Cannabinoid receptor modulators. Medical search

A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.

Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.

A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.

A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.

Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.

A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)

Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.

Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.

Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS.

Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.

OXAZINES with a fused BENZENE ring.

A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.

Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.

Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.

A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

A family of hexahydropyridines.

Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.

Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.

GLYCEROL esterified with FATTY ACIDS.

Pregnadienes which have undergone ring contractions or are lacking carbon-18 or carbon-19.

Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.

Compound isolated from Cannabis sativa extract.

An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.

One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.

Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.

Compounds capable of relieving pain without the loss of CONSCIOUSNESS.

The relationship between the dose of an administered drug and the response of the organism to the drug.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

A physiologically inactive constituent of Cannabis sativa L.

Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.

A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)

The plant genus in the Cannabaceae plant family, Urticales order, Hamamelidae subclass. The flowering tops are called many slang terms including pot, marijuana, hashish, bhang, and ganja. The stem is an important source of hemp fiber.

Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations.

Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.

One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. Its expression and function differs from, and in some ways opposes, ESTROGEN RECEPTOR BETA.

The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.

Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important.

The surgical removal of one or both ovaries.

A subfamily of lysophospholipid receptors with specificity for LYSOSPHINGOLIPIDS such as sphingosine-1-phosphate and sphingosine phosphorylcholine.

The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.

A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.

Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.

Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.

Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.

Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.

The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.

A class of drugs that act by selective inhibition of calcium influx through cellular membranes.

Compounds that contain a BENZENE ring fused to a furan ring.

The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.

Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.

Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.

Compounds based on benzene fused to oxole. They can be formed from methylated CATECHOLS such as EUGENOL.

One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.

Phenomena and pharmaceutics of compounds that bind to the same receptor binding-site as an agonist (DRUG AGONISM) for that receptor but exerts the opposite pharmacological effect.

The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.

Unsaturated derivatives of the ESTRANES with methyl groups at carbon-13, with no carbon at carbon-10, and with no more than one carbon at carbon-17. They must contain one or more double bonds.

Tumors or cancer of the UTERUS.

CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.

Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.

These compounds stimulate anabolism and inhibit catabolism. They stimulate the development of muscle mass, strength, and power.

Phenols substituted in any position by an amino group.

The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.

A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.

Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.

The hollow thick-walled muscular organ in the female PELVIS. It consists of the fundus (the body) which is the site of EMBRYO IMPLANTATION and FETAL DEVELOPMENT. Beyond the isthmus at the perineal end of fundus, is CERVIX UTERI (the neck) opening into VAGINA. Beyond the isthmi at the upper abdominal end of fundus, are the FALLOPIAN TUBES.

The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.

AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives.

The excessive use of marijuana with associated psychological symptoms and impairment in social or occupational functioning.

Blocking the process leading to OVULATION. Various factors are known to inhibit ovulation, such as neuroendocrine, psychological, and pharmacological agents.

The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.

A plant species in the PIPERACEAE plant family. It is a common spice on foods and is used medicinally to increase gastrointestinal assimilation of other supplements and drugs. Piperine is a key component. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water.

Six-carbon alicyclic hydrocarbons.

The observable response an animal makes to any situation.

The most common inhibitory neurotransmitter in the central nervous system.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.

The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.

The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo.

A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.

An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.

The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.

Tumors or cancer of the human BREAST.

Established cell cultures that have the potential to propagate indefinitely.

Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.

Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.

Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations, and other alterations of mood and thinking. Despite the name, the feature that distinguishes these agents from other classes of drugs is their capacity to induce states of altered perception, thought, and feeling that are not experienced otherwise.

An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.

Elements of limited time intervals, contributing to particular results or situations.

A cell line derived from cultured tumor cells.

The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.

The modification of the reactivity of ENZYMES by the binding of effectors to sites (ALLOSTERIC SITES) on the enzymes other than the substrate BINDING SITES.

Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS.

The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.

Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)

One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.

An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.

An increased sensation of pain or discomfort produced by mimimally noxious stimuli due to damage to soft tissue containing NOCICEPTORS or injury to a peripheral nerve.

Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079)

Steroids containing the fundamental tetracyclic unit with no methyl groups at C-10 and C-13 and with no side chain at C-17. The concept includes both saturated and unsaturated derivatives.

Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.

A group of 16-carbon fatty acids that contain no double bonds.

A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.

The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)

Compounds which inhibit or antagonize the biosynthesis or actions of androgens.

Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.

The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.

The surgical removal of one or both testicles.

A type I keratin that is found associated with the KERATIN-4 in the internal stratified EPITHELIUM. Defects in gene for keratin 13 cause HEREDITARY MUCOSAL LEUKOKERATOSIS.

Histochemical localization of immunoreactive substances using labeled antibodies as reagents.

Chemical substances or agents with contraceptive activity in males. Use for male contraceptive agents in general or for which there is no specific heading.

Product of the CANNABIS plant, CANNABINOIDS, or synthetic derivatives thereof, used in the treatment of a wide range of clinical symptoms.

An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

An amino alcohol with a long unsaturated hydrocarbon chain. Sphingosine and its derivative sphinganine are the major bases of the sphingolipids in mammals. (Dorland, 28th ed)

Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.

A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.

The function of opposing or restraining the excitation of neurons or their target excitable cells.

An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.

A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.

A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.

A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.

All of the processes involved in increasing CELL NUMBER including CELL DIVISION.

Steroidal compounds related to ESTRADIOL, the major mammalian female sex hormone. Estradiol congeners include important estradiol precursors in the biosynthetic pathways, metabolites, derivatives, and synthetic steroids with estrogenic activities.

Heterocyclic compounds of a ring with SULFUR and two NITROGEN atoms fused to a BENZENE ring. Members inhibit SODIUM-POTASSIUM-CHLORIDE SYMPORTERS and are used as DIURETICS.

Inhaling and exhaling the smoke from CANNABIS.

A loosely defined grouping of drugs that have effects on psychological function. Here the psychotropic agents include the antidepressive agents, hallucinogens, and tranquilizing agents (including the antipsychotics and anti-anxiety agents).

A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring.

Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.

A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.

The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life.

Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.

Drugs designed and synthesized, often for illegal street use, by modification of existing drug structures (e.g., amphetamines). Of special interest are MPTP (a reverse ester of meperidine), MDA (3,4-methylenedioxyamphetamine), and MDMA (3,4-methylenedioxymethamphetamine). Many drugs act on the aminergic system, the physiologically active biogenic amines.

The physical activity of a human or an animal as a behavioral phenomenon.

A group of compounds that are derivatives of methoxybenzene and contain the general formula R-C7H7O.

Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.

Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.

2-, 3-, or 4-Pyridinecarboxylic acids. Pyridine derivatives substituted with a carboxy group at the 2-, 3-, or 4-position. The 3-carboxy derivative (NIACIN) is active as a vitamin.

Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.

Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.

Alkaloids extracted from various species of Cinchona.

One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.

Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.

Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

Characteristic restricted to a particular organ of the body, such as a cell type, metabolic response or expression of a particular protein or antigen.

Neurons whose primary neurotransmitter is GAMMA-AMINOBUTYRIC ACID.

The characteristic three-dimensional shape of a molecule.

Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies.

The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.

Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.

A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.

Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.

The process of finding chemicals for potential therapeutic use.

The third type of glial cell, along with astrocytes and oligodendrocytes (which together form the macroglia). Microglia vary in appearance depending on developmental stage, functional state, and anatomical location; subtype terms include ramified, perivascular, ameboid, resting, and activated. Microglia clearly are capable of phagocytosis and play an important role in a wide spectrum of neuropathologies. They have also been suggested to act in several other roles including in secretion (e.g., of cytokines and neural growth factors), in immunological processing (e.g., antigen presentation), and in central nervous system development and remodeling.

A set of forebrain structures common to all mammals that is defined functionally and anatomically. It is implicated in the higher integration of visceral, olfactory, and somatic information as well as homeostatic responses including fundamental survival behaviors (feeding, mating, emotion). For most authors, it includes the AMYGDALA; EPITHALAMUS; GYRUS CINGULI; hippocampal formation (see HIPPOCAMPUS); HYPOTHALAMUS; PARAHIPPOCAMPAL GYRUS; SEPTAL NUCLEI; anterior nuclear group of thalamus, and portions of the basal ganglia. (Parent, Carpenter's Human Neuroanatomy, 9th ed, p744; NeuroNames, http://rprcsgi.rprc.washington.edu/neuronames/index.html (September 2, 1998)).

Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.

The parts of a macromolecule that directly participate in its specific combination with another molecule.

The smooth muscle coat of the uterus, which forms the main mass of the organ.

The use of hormonal agents with estrogen-like activity in postmenopausal or other estrogen-deficient women to alleviate effects of hormone deficiency, such as vasomotor symptoms, DYSPAREUNIA, and progressive development of OSTEOPOROSIS. This may also include the use of progestational agents in combination therapy.

PLANT EXTRACTS and compounds, primarily ISOFLAVONES, that mimic or modulate endogenous estrogens, usually by binding to ESTROGEN RECEPTORS.

Hyperpolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during NEUROTRANSMISSION. They are local changes which diminish responsiveness to excitatory signals.

Use of electric potential or currents to elicit biological responses.

A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.

A specialized CONNECTIVE TISSUE that is the main constituent of the SKELETON. The principle cellular component of bone is comprised of OSTEOBLASTS; OSTEOCYTES; and OSTEOCLASTS, while FIBRILLAR COLLAGENS and hydroxyapatite crystals form the BONE MATRIX.

A genus of ascomycetous fungi in the family Trichocomaceae, order EUROTIALES. Health effects, allergenicity, and toxicity of Eurotium are closely related to its anamorph ASPERGILLUS.

Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.

BENZOIC ACID amides.

Most generally any NEURONS which are not motor or sensory. Interneurons may also refer to neurons whose AXONS remain within a particular brain region in contrast to projection neurons, which have axons projecting to other brain regions.

Almond-shaped group of basal nuclei anterior to the INFERIOR HORN OF THE LATERAL VENTRICLE of the TEMPORAL LOBE. The amygdala is part of the limbic system.

The motor activity of the GASTROINTESTINAL TRACT.

The measurement of an organ in volume, mass, or heaviness.

An antiandrogen with about the same potency as cyproterone in rodent and canine species.

Agents that reduce the frequency or rate of spontaneous or induced tumors independently of the mechanism involved.

A plant genus of the family RUTACEAE. Some members of Zanthoxylum are reclassified from ELEUTHEROCOCCUS, Melicope, and EVODIA. The twigs are used as dental brushing sticks (TOOTHBRUSHING). Most plants that are called Fagara have been reclassified as Zanthoxylum, however some Fagara were reclassified to MELICOPE (also in the Rutacea family) or to GLEDITSIA (a genus in the FABACEAE family).

A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.

The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.

Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).

A group of fatty acids that contain 18 carbon atoms and a double bond at the omega 9 carbon.

An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.

The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.

Biosynthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in circulating and tumoral macrophages. (1/954)

The stimulus-induced biosynthesis of the endocannabinoid 2-arachidonoylglycerol (2-AG) in intact mouse J774 macrophages and the inactivation of 2-AG by the same cells or by rat circulating macrophages was studied. By using gas chromatography-mass spectrometry, we found that ionomycin (5 microM) and lipopolysaccharide (LPS, 200 microg x mL-1) cause a 24-fold and 2.5-fold stimulation of 2-AG levels in J774 cells, respectively, thus providing unprecedented evidence that this cannabimimetic metabolite can be synthesized by macrophages. In J774 cells, LPS also induced a 7.8-fold increase of the levels of the other endocannabinoid, anandamide, and, in rat circulating macrophages, an almost twofold increase of 2-AG levels. Extracellular [3H]2-AG was cleared from the medium of intact J774 macrophages (t1/2 = 19-28 min) and esterified to phospholipids, diacylglycerols and triglycerides or hydrolyzed to [3H]arachidonic acid and glycerol. These catabolic processes were attenuated differentially by various enzyme inhibitors. Rat circulating macrophages were shown to contain enzymatic activities for the hydrolysis of 2-AG, including: (a) fatty acid amide hydrolase (FAAH), the enzyme responsible for anandamide breakdown and previously shown to catalyse also 2-AG hydrolysis, and (b) a 2-AG hydrolase activity different from FAAH and down-regulated by LPS. High levels of FAAH mRNA were found in circulating macrophages but not platelets, which, however, contain a 2-AG hydrolase. Both platelets and macrophages were shown to express the mRNA for the CB1 cannabinoid receptor. A macrophage 2-AG hydrolase with apparent Km = 110 microM and Vmax = 7.9 nmol x min-1 x (mg protein)-1 was partially characterized in J774 cells and found to exhibit an optimal pH of 6-7 and little or no sensitivity to typical FAAH inhibitors. These findings demonstrate for the first time that macrophages participate in the homeostasis of the hypotensive and immunomodulatory endocannabinoid 2-AG through metabolic mechanisms that are subject to regulation. (+info)

The endothelial component of cannabinoid-induced relaxation in rabbit mesenteric artery depends on gap junctional communication. (2/954)

1. We have shown that the endocannabinoid anandamide and its stable analogue methanandamide relax rings of rabbit superior mesenteric artery through endothelium-dependent and -independent mechanisms that are unaffected by blockade of NO synthase and cyclooxygenase. 2. The endothelium-dependent component of the responses was attenuated by the gap junction inhibitor 18alpha-glycyrrhetinic acid (18alpha-GA; 50 microM), and a synthetic connexin-mimetic peptide homologous to the extracellular Gap 27 sequence of connexin 43 (43Gap 27, SRPTEKTIFII; 300 microM). By contrast, the corresponding connexin 40 peptide (40Gap 27, SRPTEKNVFIV) was inactive. 3. The cannabinoid CB1 receptor antagonist SR141716A (10 microM) also attenuated endothelium-dependent relaxations but this inhibition was not observed with the CB1 receptor antagonist LY320135 (10 microM). Furthermore, SR141716A mimicked the effects of 43Gap 27 peptide in blocking Lucifer Yellow dye transfer between coupled COS-7 cells (a monkey fibroblast cell line), whereas LY320135 was without effect, thus suggesting that the action of SR141716A was directly attributable to effects on gap junctions. 4. The endothelium-dependent component of cannabinoid-induced relaxation was also attenuated by AM404 (10 microM), an inhibitor of the high-affinity anandamide transporter, which was without effect on dye transfer. 5. Taken together, the findings suggest that cannabinoids derived from arachidonic acid gain access to the endothelial cytosol via a transporter mechanism and subsequently stimulate relaxation by promoting diffusion of an to adjacent smooth muscle cells via gap junctions. 6. Relaxations of endothelium-denuded preparations to anandamide and methanandamide were unaffected by 43Gap 27 peptide, 18alpha-GA, SR141716A, AM404 and indomethacin and their genesis remains to be established. (+info)

Comparison of novel cannabinoid partial agonists and SR141716A in the guinea-pig small intestine. (3/954)

The controversial nature of the CB(1) receptor antagonist, SR141716A, in the guinea-pig small intestine was investigated by comparing it with four analogues of Delta(8)-tetrahydrocannabinol (Delta(8)-THC): O-1184, O-1238, O-584 and O-1315. These compounds (10 - 1000 nM) inhibited the electrically-evoked contractions with a rank order of potency of O-1238>O-1184>O-584>O-1315. Log concentration-response curves for O-1238, O-1184 and O-1315 were significantly shifted to the right by SR141716A and the maxima were significantly less than that of the CB(1) agonist, WIN55212-2, an indication of partial agonism. Partial saturation of the triple bond in O-1184 to a cis double bond (O-1238) increased its potency as an agonist (pEC(50) from 6.42 to 7.63) and as an antagonist of WIN55212-2, (pK(B), from 8.36 to 9.49). Substitution of the terminal azide group by an ethyl group (O-584) or removal of the phenolic hydroxyl group (O-1315) had no significant effect on the agonist or antagonist potency. None of these analogues increased the twitch response in a manner resembling that of SR141716A. O-1184 (10 and 100 nM) shifted the log concentration-response curve of WIN55212-2 for inhibition of the twitch responses to the right with pK(B) values of 8.29 and 8.38, respectively. We conclude that these Delta(8)-THC analogues behave as partial agonists rather than silent antagonists at CB(1) binding sites in this tissue. There was no evidence of antagonism of endocannabinoids thus supporting the hypothesis that, in this tissue, SR141716A is an inverse agonist of constitutively active CB(1) receptors. (+info)

Reversal of dopamine D(2) receptor responses by an anandamide transport inhibitor. (4/954)

We characterized the pharmacological properties of the anandamide transport inhibitor N-(4-hydroxyphenyl)-arachidonamide (AM404) in rats and investigated the effects of this drug on behavioral responses associated with activation of dopamine D(2) family receptors. Rat brain slices accumulated [(3)H]anandamide via a high-affinity transport mechanism that was blocked by AM404. When administered alone in vivo, AM404 caused a mild and slow-developing hypokinesia that was significant 60 min after intracerebroventricular injection of the drug and was reversed by the CB1 cannabinoid receptor antagonist SR141716A. AM404 produced no significant catalepsy or analgesia, two typical effects of direct-acting cannabinoid agonists. However, AM404 prevented the stereotypic yawning produced by systemic administration of a low dose of apomorphine, an effect that was dose-dependent and blocked by SR141716A. Furthermore, AM404 reduced the stimulation of motor behaviors elicited by the selective D(2) family receptor agonist quinpirole. Finally, AM404 reduced hyperactivity in juvenile spontaneously hypertensive rats, a putative model of attention deficit hyperactivity disorder. The results support a primary role of the endocannabinoid system in the regulation of psychomotor activity and point to anandamide transport as a potential target for neuropsychiatric medicines. (+info)

Endocannabinoid 2-arachidonyl glycerol is a full agonist through human type 2 cannabinoid receptor: antagonism by anandamide. (5/954)

The endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG) bind to G protein-coupled central and peripheral cannabinoid receptors CB1 and CB2, respectively. Due to the relatively high expression of the CB2 isotype on peripheral immune cells, it has been hypothesized that this receptor mediates the immunosuppressive effects of cannabinoids. Unfortunately, there was a dearth of pharmacological studies with the endocannabinoids and human CB2 (hCB2). These studies compare and contrast the potency and efficacy of anandamide, 2-AG, and the synthetic cannabinoid HU210 at hCB2. Using [(35)S]guanosine-5'-O-(3-thio)triphosphate (GTPgammaS) and radioligand bindings in insect Sf9-hCB2 membranes, we showed that both endocannabinoids bound hCB2 with similar affinity and that the cannabinoids acted as full agonists in stimulating [(35)S]GTPgammaS exchange, although 2-AG was 3-fold more potent than anandamide (EC(50) = 38.9 +/- 3.1 and 121 +/- 29 nM, respectively). In a mammalian expression system (Chinese hamster ovary-hCB2 cells), HU210 and 2-AG maximally inhibited forskolin-stimulated cAMP synthesis (IC(50) = 1.61 +/- 0.42 nM and 1.30 +/- 0.37 microM, respectively) although anandamide was ineffective. In Chinese hamster ovary-hCB2 membranes, HU210 and 2-AG were also full agonists in stimulating [(35)S]GTPgammaS binding (EC(50) = 1.96 +/- 0.35 and 122 +/- 17 nM, respectively), but anandamide was a weak partial agonist (EC(50) = 261 +/- 91 nM; 34 +/- 4% of maximum). Due to its low intrinsic activity, coincubation with anandamide effectively attenuated the functional activity of 2-AG at hCB2. Collectively, the data showed that both endocannabinoids bound hCB2 with similar affinity, but only 2-AG functioned as a full agonist. Moreover, the agonistic activity of 2-AG was attenuated by anandamide. (+info)

Are anandamide and cannabinoid receptors involved in ethanol tolerance? A review of the evidence. (6/954)

There have been significant developments towards the elucidation of molecular and cellular changes in neuronal second messenger pathways involved in the development of tolerance to and dependence on ethanol (EtOH). The long-term exposure to EtOH has been shown to affect several aspects of neuronal signal transduction as well as ligand-gated ion channels and receptor systems, including the receptors that are coupled to the superfamily of GTP binding regulatory proteins (G-proteins). The recent identification of a G-protein coupled receptor that was activated by delta-9-tetrahydrocannabinol (THC), the major psychoactive component of marijuana, led to the discovery of endogenous agonists. One such agonist found to exist in mammalian brain was characterized to be an arachidonic acid (AA) metabolite and was named anandamide (AnNH). AnNH has been shown to bind specifically to the cannabinoid receptor (CB(1)) and mimic many of the pharmacological and behavioural effects of THC including tolerance development. The role of endocannabinoids and the CB(1) receptor signal transduction system in tolerance development to drugs of abuse has not been explored until recently. The findings presented in this review provide evidence for the first time that some of the pharmacological actions of EtOH including tolerance development may be mediated through participation of the endocannabinoid-CB(1) receptor signal transduction system. Recent studies have shown that chronic EtOH exposure produces downregulation of CB(1) receptors and an inhibition of CB(1) receptor agonist-stimulated GTPgammaS binding in mouse brain synaptic plasma membranes (SPM). The observed receptor downregulation results from the persistent stimulation of the receptors by the endogenous CB(1) receptor agonist AnNH, the synthesis of which is increased by chronic EtOH exposure. Further, the CB(1) receptor antagonist SR-141716A has been shown to block voluntary EtOH intake in rats and mice. Based on these studies, a hypothesis is presented to explain the possible involvement of the endocannabinoid system in the pharmacological and behavioural effects of EtOH. (+info)

Down-regulation of anandamide hydrolase in mouse uterus by sex hormones. (7/954)

Endocannabinoids are an emerging class of lipid mediators, which mimic several effects of cannabinoids. Anandamide (arachidonoylethanolamide) is a major endocannabinoid, which has been shown to impair pregnancy and embryo development. The activity of anandamide is controlled by cellular uptake through a specific transporter and intracellular degradation by the enzyme anandamide hydrolase (fatty acid amide hydrolase, FAAH). We characterized FAAH in mouse uterus by radiochromatographic and immunochemical techniques, showing that the enzyme is confined to the epithelium and its activity decreases appreciably during pregnancy or pseudopregnancy because of lower gene expression at the translational level. Ovariectomy prevented the decrease in FAAH, and both progesterone and estrogen further reduced its basal levels, suggesting hormonal control of the enzyme. Anandamide was shown to induce programmed cell death in mouse blastocysts, through a pathway independent of type-1 cannabinoid receptor. Blastocysts, however, have a specific anandamide transporter and FAAH, which scavenge this lipid. Taken together, these results provide evidence of an interplay between endocannabinoids and sex hormones in pregnancy. These findings may also be relevant for human fertility, as epithelial cells from healthy human uterus showed FAAH activity and expression, which in adenocarcinoma cells was increased fivefold. (+info)

Age dependent accumulation of N-acyl-ethanolamine phospholipids in ischemic rat brain. A (31)P NMR and enzyme activity study. (8/954)

N-acyl-ethanolamine phospholipids (NAPE) can be formed as a stress response during neuronal injury, and they are precursors for N-acyl-ethanolamines (NAE), some of which are endocannabinoids. The levels of NAPE accumulated during post-decapitative ischemia (6 h at 37 degrees C) were studied in rat brains of various age (1, 6, 12, 19, 30, and approximately 70 days) by the use of (31)P NMR spectroscopy of lipid extracts. This ability to accumulate NAPE was compared with the activity of N-acyltransferase and of NAPE-hydrolyzing phospholipase D (NAPE-PLD) in brain microsomes. These two enzymes are involved in the formation and degradation of NAPE, respectively. The results showed that 1) the ability to accumulate NAPE during post-decapitative ischemia is especially high in the youngest rats and is markedly reduced in older brains [in 1-day-old rat brains NAPE accumulated to 1.5% of total phospholipids, while in 30-day-old rat brains NAPE accumulation could not be detected (detection limit 0.09%)] and 2) this age pattern of accumulation can be explained by a combination of the decreased activity of N-acyltransferase and the increased activity of NAPE-PLD during development. These results point out that it would be advantageous to investigate a potential cytoprotective role of NAPE in the brains of very young rats. (+info)

Leiomyomas are the most common type of gynecologic tumor and affect up to 80% of women at some point in their lifetime. They are more common in women who have a family history of leiomyomas or who are obese.

There are several different types of leiomyomas, including:

1. Submucosal leiomyomas: These tumors grow into the uterine cavity and can cause bleeding and other symptoms.
2. Intramural leiomyomas: These tumors grow within the muscle of the uterus and can cause pelvic pain and heavy menstrual bleeding.
3. Pedunculated leiomyomas: These tumors are attached to the uterine wall by a stalk-like structure and can be felt during a pelvic exam.
4. Broad ligament leiomyomas: These tumors grow on the broad ligament, which is a band of tissue that connects the uterus to the pelvis.

Leiomyomas are typically diagnosed through a combination of pelvic examination, ultrasound, and hysteroscopy (a procedure in which a small camera is inserted into the uterus to examine the inside of the organ). Treatment options for leiomyomas depend on the size and location of the tumors, as well as the severity of symptoms. Treatment may include watchful waiting, medications to regulate hormones or shrink the tumors, or surgery to remove the tumors.

In some cases, leiomyomas can be associated with other conditions such as endometriosis or adenomyosis, and it is important for women with these tumors to receive ongoing care from a healthcare provider to monitor for any changes in their condition.

1. Endometrial carcinoma (cancer that starts in the lining of the uterus)
2. Uterine papillary serous carcinoma (cancer that starts in the muscle layer of the uterus)
3. Leiomyosarcoma (cancer that starts in the smooth muscle of the uterus)
4. Adenocarcinoma (cancer that starts in the glands of the endometrium)
5. Clear cell carcinoma (cancer that starts in the cells that resemble the lining of the uterus)
6. Sarcoma (cancer that starts in the connective tissue of the uterus)
7. Mixed tumors (cancers that have features of more than one type of uterine cancer)

These types of cancers can affect women of all ages and are more common in postmenopausal women. Risk factors for developing uterine neoplasms include obesity, tamoxifen use, and a history of endometrial hyperplasia (thickening of the lining of the uterus).

Symptoms of uterine neoplasms can include:

1. Abnormal vaginal bleeding (heavy or prolonged menstrual bleeding, spotting, or postmenopausal bleeding)
2. Postmenopausal bleeding
3. Pelvic pain or discomfort
4. Vaginal discharge
5. Weakness and fatigue
6. Weight loss
7. Pain during sex
8. Increased urination or frequency of urination
9. Abnormal Pap test results (abnormal cells found on the cervix)

If you have any of these symptoms, it is essential to consult your healthcare provider for proper evaluation and treatment. A diagnosis of uterine neoplasms can be made through several methods, including:

1. Endometrial biopsy (a small sample of tissue is removed from the lining of the uterus)
2. Dilation and curettage (D&C; a surgical procedure to remove tissue from the inside of the uterus)
3. Hysteroscopy (a thin, lighted tube with a camera is inserted through the cervix to view the inside of the uterus)
4. Imaging tests (such as ultrasound or MRI)

Treatment for uterine neoplasms depends on the type and stage of cancer. Common treatments include:

1. Hysterectomy (removal of the uterus)
2. Radiation therapy (uses high-energy rays to kill cancer cells)
3. Chemotherapy (uses drugs to kill cancer cells)
4. Targeted therapy (uses drugs to target specific cancer cells)
5. Clinical trials (research studies to test new treatments)

It is essential for women to be aware of their bodies and any changes that occur, particularly after menopause. Regular pelvic exams and screenings can help detect uterine neoplasms at an early stage, when they are more treatable. If you experience any symptoms or have concerns about your health, talk to your healthcare provider. They can help determine the cause of your symptoms and recommend appropriate treatment.

During menopause, the levels of estrogen in the body decrease significantly, which can lead to a loss of bone density and an increased risk of developing osteoporosis. Other risk factors for postmenopausal osteoporosis include:

* Family history of osteoporosis
* Early menopause (before age 45)
* Poor diet or inadequate calcium and vitamin D intake
* Sedentary lifestyle or lack of exercise
* Certain medications, such as glucocorticoids and anticonvulsants
* Other medical conditions, such as rheumatoid arthritis and liver or kidney disease.

Postmenopausal osteoporosis can be diagnosed through a variety of tests, including bone mineral density (BMD) measurements, which can determine the density of bones and detect any loss of bone mass. Treatment options for postmenopausal osteoporosis typically involve a combination of medications and lifestyle changes, such as:

* Bisphosphonates, which help to slow down bone loss and reduce the risk of fractures
* Hormone replacement therapy (HRT), which can help to replace the estrogen that is lost during menopause and improve bone density
* Selective estrogen receptor modulators (SERMs), which mimic the effects of estrogen on bone density but have fewer risks than HRT
* RANK ligand inhibitors, which can help to slow down bone loss and reduce the risk of fractures
* Parathyroid hormone (PTH) analogues, which can help to increase bone density and improve bone quality.

It is important for women to discuss their individual risks and benefits with their healthcare provider when determining the best course of treatment for postmenopausal osteoporosis. Additionally, lifestyle changes such as regular exercise, a balanced diet, and avoiding substances that can harm bone health (such as smoking and excessive alcohol consumption) can also help to manage the condition.

1) They share similarities with humans: Many animal species share similar biological and physiological characteristics with humans, making them useful for studying human diseases. For example, mice and rats are often used to study diseases such as diabetes, heart disease, and cancer because they have similar metabolic and cardiovascular systems to humans.

2) They can be genetically manipulated: Animal disease models can be genetically engineered to develop specific diseases or to model human genetic disorders. This allows researchers to study the progression of the disease and test potential treatments in a controlled environment.

3) They can be used to test drugs and therapies: Before new drugs or therapies are tested in humans, they are often first tested in animal models of disease. This allows researchers to assess the safety and efficacy of the treatment before moving on to human clinical trials.

4) They can provide insights into disease mechanisms: Studying disease models in animals can provide valuable insights into the underlying mechanisms of a particular disease. This information can then be used to develop new treatments or improve existing ones.

5) Reduces the need for human testing: Using animal disease models reduces the need for human testing, which can be time-consuming, expensive, and ethically challenging. However, it is important to note that animal models are not perfect substitutes for human subjects, and results obtained from animal studies may not always translate to humans.

6) They can be used to study infectious diseases: Animal disease models can be used to study infectious diseases such as HIV, TB, and malaria. These models allow researchers to understand how the disease is transmitted, how it progresses, and how it responds to treatment.

7) They can be used to study complex diseases: Animal disease models can be used to study complex diseases such as cancer, diabetes, and heart disease. These models allow researchers to understand the underlying mechanisms of the disease and test potential treatments.

8) They are cost-effective: Animal disease models are often less expensive than human clinical trials, making them a cost-effective way to conduct research.

9) They can be used to study drug delivery: Animal disease models can be used to study drug delivery and pharmacokinetics, which is important for developing new drugs and drug delivery systems.

10) They can be used to study aging: Animal disease models can be used to study the aging process and age-related diseases such as Alzheimer's and Parkinson's. This allows researchers to understand how aging contributes to disease and develop potential treatments.

The DSM-5 defines marijuana abuse as:

1. Taking marijuana in larger amounts or for a longer period than intended.
2. Desire or unsuccessful efforts to cut down or control use.
3. Spending a lot of time obtaining, using, or recovering from the effects of use.
4. Craving or strong desire to use marijuana.
5. Interference with work, school, or home responsibilities due to use.
6. Continuing to use despite social or personal problems caused by use.
7. Giving up important activities in order to use.
8. Using marijuana in hazardous situations, such as while driving or operating machinery.
9. Continued use despite physical or psychological problems caused or worsened by use.
10. Developing tolerance (needing to use more to achieve the desired effect).
11. Experiencing withdrawal symptoms when stopping or reducing use.

Marijuana abuse can lead to a range of negative consequences, including:

* Addiction: Marijuana can be addictive, and long-term use can lead to dependence and withdrawal symptoms when trying to stop.
* Mental Health Problems: Marijuana use has been linked to an increased risk of depression, anxiety, psychosis, and other mental health issues.
* Respiratory Problems: Smoking marijuana can irritate the lungs and increase the risk of respiratory problems, such as bronchitis and lung infections.
* Cognitive Impairment: Marijuana use can impair memory, attention, and decision-making skills.
* Impaired Coordination and Judgment: Marijuana use can impair coordination and judgment, which can increase the risk of accidents and injuries.

If you or someone you know is struggling with marijuana abuse, it is important to seek professional help as soon as possible. Treatment options may include counseling, medication, and support groups. With the right treatment and support, it is possible to overcome marijuana abuse and achieve a healthier, happier life.

There are different types of Breast Neoplasms such as:

1. Fibroadenomas: These are benign tumors that are made up of glandular and fibrous tissues. They are usually small and round, with a smooth surface, and can be moved easily under the skin.

2. Cysts: These are fluid-filled sacs that can develop in both breast tissue and milk ducts. They are usually benign and can disappear on their own or be drained surgically.

3. Ductal Carcinoma In Situ (DCIS): This is a precancerous condition where abnormal cells grow inside the milk ducts. If left untreated, it can progress to invasive breast cancer.

4. Invasive Ductal Carcinoma (IDC): This is the most common type of breast cancer and starts in the milk ducts but grows out of them and invades surrounding tissue.

5. Invasive Lobular Carcinoma (ILC): It originates in the milk-producing glands (lobules) and grows out of them, invading nearby tissue.

Breast Neoplasms can cause various symptoms such as a lump or thickening in the breast or underarm area, skin changes like redness or dimpling, change in size or shape of one or both breasts, discharge from the nipple, and changes in the texture or color of the skin.

Treatment options for Breast Neoplasms may include surgery such as lumpectomy, mastectomy, or breast-conserving surgery, radiation therapy which uses high-energy beams to kill cancer cells, chemotherapy using drugs to kill cancer cells, targeted therapy which uses drugs or other substances to identify and attack cancer cells while minimizing harm to normal cells, hormone therapy, immunotherapy, and clinical trials.

It is important to note that not all Breast Neoplasms are cancerous; some are benign (non-cancerous) tumors that do not spread or grow.

There are several different types of pain, including:

1. Acute pain: This type of pain is sudden and severe, and it usually lasts for a short period of time. It can be caused by injuries, surgery, or other forms of tissue damage.
2. Chronic pain: This type of pain persists over a long period of time, often lasting more than 3 months. It can be caused by conditions such as arthritis, fibromyalgia, or nerve damage.
3. Neuropathic pain: This type of pain results from damage to the nervous system, and it can be characterized by burning, shooting, or stabbing sensations.
4. Visceral pain: This type of pain originates in the internal organs, and it can be difficult to localize.
5. Psychogenic pain: This type of pain is caused by psychological factors such as stress, anxiety, or depression.

The medical field uses a range of methods to assess and manage pain, including:

1. Pain rating scales: These are numerical scales that patients use to rate the intensity of their pain.
2. Pain diaries: These are records that patients keep to track their pain over time.
3. Clinical interviews: Healthcare providers use these to gather information about the patient's pain experience and other relevant symptoms.
4. Physical examination: This can help healthcare providers identify any underlying causes of pain, such as injuries or inflammation.
5. Imaging studies: These can be used to visualize the body and identify any structural abnormalities that may be contributing to the patient's pain.
6. Medications: There are a wide range of medications available to treat pain, including analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs), and muscle relaxants.
7. Alternative therapies: These can include acupuncture, massage, and physical therapy.
8. Interventional procedures: These are minimally invasive procedures that can be used to treat pain, such as nerve blocks and spinal cord stimulation.

It is important for healthcare providers to approach pain management with a multi-modal approach, using a combination of these methods to address the physical, emotional, and social aspects of pain. By doing so, they can help improve the patient's quality of life and reduce their suffering.

Hyperalgesia is often seen in people with chronic pain conditions, such as fibromyalgia, and it can also be a side effect of certain medications or medical procedures. Treatment options for hyperalgesia depend on the underlying cause of the condition, but may include pain management techniques, physical therapy, and medication adjustments.

In clinical settings, hyperalgesia is often assessed using a pinprick test or other pain tolerance tests to determine the patient's sensitivity to different types of stimuli. The goal of treatment is to reduce the patient's pain and improve their quality of life.

There are several types of osteoporosis, including:

1. Postmenopausal osteoporosis: This type of osteoporosis is caused by hormonal changes that occur during menopause. It is the most common form of osteoporosis and affects women more than men.
2. Senile osteoporosis: This type of osteoporosis is caused by aging and is the most common form of osteoporosis in older adults.
3. Juvenile osteoporosis: This type of osteoporosis affects children and young adults and can be caused by a variety of genetic disorders or other medical conditions.
4. secondary osteoporosis: This type of osteoporosis is caused by other medical conditions, such as rheumatoid arthritis, Crohn's disease, or ulcerative colitis.

The symptoms of osteoporosis can be subtle and may not appear until a fracture has occurred. They can include:

1. Back pain or loss of height
2. A stooped posture
3. Fractures, especially in the spine, hips, or wrists
4. Loss of bone density, as determined by a bone density test

The diagnosis of osteoporosis is typically made through a combination of physical examination, medical history, and imaging tests, such as X-rays or bone density tests. Treatment for osteoporosis can include medications, such as bisphosphonates, hormone therapy, or rANK ligand inhibitors, as well as lifestyle changes, such as regular exercise and a balanced diet.

Preventing osteoporosis is important, as it can help to reduce the risk of fractures and other complications. To prevent osteoporosis, individuals can:

1. Get enough calcium and vitamin D throughout their lives
2. Exercise regularly, especially weight-bearing activities such as walking or running
3. Avoid smoking and excessive alcohol consumption
4. Maintain a healthy body weight
5. Consider taking medications to prevent osteoporosis, such as bisphosphonates, if recommended by a healthcare provider.

Neuralgia is often difficult to diagnose and treat, as the underlying cause can be challenging to identify. However, various medications and therapies can help manage the pain and other symptoms associated with this condition. These may include pain relievers, anticonvulsants, antidepressants, and muscle relaxants, as well as alternative therapies such as acupuncture or physical therapy.

Some common forms of neuralgia include:

1. Trigeminal neuralgia: This is a condition that affects the trigeminal nerve, which carries sensation from the face to the brain. It is characterized by sudden, intense pain in the face, typically on one side.
2. Postherpetic neuralgia (PHN): This is a condition that occurs after a shingles infection, and is characterized by persistent pain in the affected area.
3. Occipital neuralgia: This is a condition that affects the nerves in the back of the head and neck, and can cause pain in the back of the head, neck, and face.
4. Geniculate neuralgia: This is a rare condition that affects the nerves in the jaw and ear, and can cause pain in the jaw, face, and ear.

Overall, neuralgia is a complex and debilitating condition that can significantly impact an individual's quality of life. It is important for individuals experiencing symptoms of neuralgia to seek medical attention to determine the underlying cause and develop an appropriate treatment plan.

* Anxiety
* Depression
* Fatigue
* Insomnia
* Muscle and bone pain
* Nausea and vomiting
* Seizures (in severe cases)
* Sweating
* Tremors

The specific symptoms of substance withdrawal syndrome can vary depending on the substance being withdrawn from, but some common symptoms include:

* Alcohol: tremors, anxiety, insomnia, nausea and vomiting, headaches, and seizures
* Opioids: withdrawal symptoms can include anxiety, muscle aches, sweating, nausea and vomiting, diarrhea, and depression
* Benzodiazepines: withdrawal symptoms can include anxiety, insomnia, tremors, and seizures

The diagnosis of substance withdrawal syndrome is typically made based on the patient's history of substance use and the presence of withdrawal symptoms. A healthcare provider may also order laboratory tests to rule out other conditions that may be causing the symptoms. Treatment for substance withdrawal syndrome usually involves supportive care, such as rest, hydration, and pain management, as well as medication to manage withdrawal symptoms. In some cases, medical professionals may also recommend a gradual tapering of the substance over a period of time to minimize withdrawal symptoms.

It is important for individuals who are experiencing withdrawal symptoms to seek medical attention as soon as possible, as untreated withdrawal can lead to serious complications, such as seizures and dehydration. With appropriate treatment, most individuals with substance withdrawal syndrome can recover fully and successfully overcome their addiction.

Gliosis is made up of glial cells, which are non-neuronal cells that provide support and protection to neurons. When neural tissue is damaged, glial cells proliferate and form a scar-like tissue to fill in the gap and repair the damage. This scar tissue can be made up of astrocytes, oligodendrocytes, or microglia, depending on the type of injury and the location of the damage.

Gliosis can have both beneficial and harmful effects on the brain. On one hand, it can help to prevent further damage by providing a physical barrier against invading substances and protecting the surrounding neural tissue. It can also promote healing by bringing in immune cells and growth factors that aid in the repair process.

On the other hand, gliosis can also have negative effects on brain function. The scar tissue can disrupt normal communication between neurons, leading to impaired cognitive and motor function. In addition, if the scar tissue is too extensive or severe, it can compress or displaces surrounding neural tissue, leading to long-term neurological deficits or even death.

There are several ways to diagnose gliosis, including magnetic resonance imaging (MRI), positron emission tomography (PET), and histopathology. Treatment options for gliosis depend on the underlying cause of the condition and can include medications, surgery, or a combination of both.

In summary, gliosis is a type of scar tissue that forms in the brain and spinal cord as a result of damage to neural tissue. It can have both beneficial and harmful effects on brain function, and diagnosis and treatment options vary depending on the underlying cause of the condition.

There are several key features of inflammation:

1. Increased blood flow: Blood vessels in the affected area dilate, allowing more blood to flow into the tissue and bringing with it immune cells, nutrients, and other signaling molecules.
2. Leukocyte migration: White blood cells, such as neutrophils and monocytes, migrate towards the site of inflammation in response to chemical signals.
3. Release of mediators: Inflammatory mediators, such as cytokines and chemokines, are released by immune cells and other cells in the affected tissue. These molecules help to coordinate the immune response and attract more immune cells to the site of inflammation.
4. Activation of immune cells: Immune cells, such as macrophages and T cells, become activated and start to phagocytose (engulf) pathogens or damaged tissue.
5. Increased heat production: Inflammation can cause an increase in metabolic activity in the affected tissue, leading to increased heat production.
6. Redness and swelling: Increased blood flow and leakiness of blood vessels can cause redness and swelling in the affected area.
7. Pain: Inflammation can cause pain through the activation of nociceptors (pain-sensing neurons) and the release of pro-inflammatory mediators.

Inflammation can be acute or chronic. Acute inflammation is a short-term response to injury or infection, which helps to resolve the issue quickly. Chronic inflammation is a long-term response that can cause ongoing damage and diseases such as arthritis, asthma, and cancer.

There are several types of inflammation, including:

1. Acute inflammation: A short-term response to injury or infection.
2. Chronic inflammation: A long-term response that can cause ongoing damage and diseases.
3. Autoimmune inflammation: An inappropriate immune response against the body's own tissues.
4. Allergic inflammation: An immune response to a harmless substance, such as pollen or dust mites.
5. Parasitic inflammation: An immune response to parasites, such as worms or fungi.
6. Bacterial inflammation: An immune response to bacteria.
7. Viral inflammation: An immune response to viruses.
8. Fungal inflammation: An immune response to fungi.

There are several ways to reduce inflammation, including:

1. Medications such as nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and disease-modifying anti-rheumatic drugs (DMARDs).
2. Lifestyle changes, such as a healthy diet, regular exercise, stress management, and getting enough sleep.
3. Alternative therapies, such as acupuncture, herbal supplements, and mind-body practices.
4. Addressing underlying conditions, such as hormonal imbalances, gut health issues, and chronic infections.
5. Using anti-inflammatory compounds found in certain foods, such as omega-3 fatty acids, turmeric, and ginger.

It's important to note that chronic inflammation can lead to a range of health problems, including:

1. Arthritis
2. Diabetes
3. Heart disease
4. Cancer
5. Alzheimer's disease
6. Parkinson's disease
7. Autoimmune disorders, such as lupus and rheumatoid arthritis.

Therefore, it's important to manage inflammation effectively to prevent these complications and improve overall health and well-being.

Body weight is an important health indicator, as it can affect an individual's risk for certain medical conditions, such as obesity, diabetes, and cardiovascular disease. Maintaining a healthy body weight is essential for overall health and well-being, and there are many ways to do so, including a balanced diet, regular exercise, and other lifestyle changes.

There are several ways to measure body weight, including:

1. Scale: This is the most common method of measuring body weight, and it involves standing on a scale that displays the individual's weight in kg or lb.
2. Body fat calipers: These are used to measure body fat percentage by pinching the skin at specific points on the body.
3. Skinfold measurements: This method involves measuring the thickness of the skin folds at specific points on the body to estimate body fat percentage.
4. Bioelectrical impedance analysis (BIA): This is a non-invasive method that uses electrical impulses to measure body fat percentage.
5. Dual-energy X-ray absorptiometry (DXA): This is a more accurate method of measuring body composition, including bone density and body fat percentage.

It's important to note that body weight can fluctuate throughout the day due to factors such as water retention, so it's best to measure body weight at the same time each day for the most accurate results. Additionally, it's important to use a reliable scale or measuring tool to ensure accurate measurements.

"Cannabinoid Receptor Modulators, Their Processes of Preparation, and use of Cannabinoid Receptor Modulators for Treating ... September 2002). "C-3 Amido-indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399- ... that acts as a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 8 nM at CB2 and 500x selectivity ... over the related CB1 receptor. It has antiinflammatory effects and inhibits release of TNF-α. A-796,260 APP-FUBINACA JWH-200 ...

https://en.wikipedia.org/wiki/BMS-F

"Cannabinoid Receptor Modulators, Their Processes of Preparation, and use of Cannabinoid Receptor Modulators for Treating ... September 2002). "C-3 Amido-indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399- ... September 2002). "C-3 Amido-indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399- ... that acts as a reasonably selective agonist of peripheral cannabinoid receptors. It has moderate affinity for CB2 receptors ...

https://en.wikipedia.org/wiki/MN-25

... is a negative allosteric modulator of the cannabinoid CB1 receptor. Org 27569 PSNCBAM-1 ZCZ-011 Kulkarni PM, Kulkarni AR ... Cannabinoids, CB1 receptor antagonists, Isothiocyanates, All stub articles, Cannabinoid stubs). ... June 2016). "Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100 ... January 2016). "Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s ...

https://en.wikipedia.org/wiki/GAT100

... which acts on the cannabinoid receptor type 1 (CB1) as a partial agonist, CBD instead is a negative allosteric modulator of CB1 ... Cannabidiol may be an antagonist of GPR55, a G protein-coupled receptor and putative cannabinoid receptor that is expressed in ... December 2007). "The orphan receptor GPR55 is a novel cannabinoid receptor". British Journal of Pharmacology. 152 (7): 1092- ... "Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor". British Journal of Pharmacology. 20 (172): ...

https://en.wikipedia.org/wiki/Cannabidiol

"Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor". British Journal of Pharmacology. 172 (20): ... later it was found that the most important receptors are the PPAR-alpha receptor, the TRPV receptor and the GPR55 receptor. ... The cannabinoid receptors CB1 and CB2, two G protein-coupled receptors that are located in the central and peripheral nervous ... Cannabinoid receptors are G-protein coupled receptors located on the pre-synaptic membrane. While there have been some papers ...

https://en.wikipedia.org/wiki/Endocannabinoid_system

"Are cannabidiol and Δ9-tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review". British ... cannabinoid receptor 1 (CB1) and 2 (CB2). Both receptors are 7-transmembrane G-protein coupled receptors (GPCRs) which inhibit ... A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of ... The endogenous cannabinoid system includes cannabinoid receptors, their endogenous ligands (endocannabinoids) and enzymes for ...

https://en.wikipedia.org/wiki/Cannabinoid_receptor_antagonist

Nickols HH, Conn PJ (January 2014). "Development of allosteric modulators of GPCRs for treatment of CNS disorders". ... Cannabinoid receptor type 1 (CB1), also known as cannabinoid receptor 1, is a G protein-coupled cannabinoid receptor that in ... Discovery and development of Cannabinoid Receptor 1 Antagonists Cannabinoid receptor Cannabinoid receptor type 2 (CB2) GRCh38: ... Selective CB1 agonists may be used to isolate the effects of the receptor from the CB2 receptor, as most cannabinoids and ...

https://en.wikipedia.org/wiki/Cannabinoid_receptor_type_1

"Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor". British Journal of Pharmacology. 172 (20): ... "The pharmacology of cannabinoid receptors and their ligands: an overview". International Journal of Obesity. 30 (S1): S13-S18. ... Cannabis and cannabinoids : pharmacology, toxicology, and therapeutic potential. Grotenhermen, Franjo., Russo, Ethan. New York ... κ-opioid receptor agonist), the active constituent of Salvia divinorum sage Salvinorin B methoxymethyl ether†, a semi-synthetic ...

https://en.wikipedia.org/wiki/List_of_psychedelic_drugs

December 2015). "A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No ... ZCZ-011 is a positive allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 PSNCBAM-1 Poklis JL, Clay DJ, ... June 2015). "HPLC-MS-MS Determination of ZCZ-011, A Novel Pharmacological Tool for Investigation of the Cannabinoid Receptor in ... Cannabinoids, Tryptamines, All stub articles, Cannabinoid stubs). ...

https://en.wikipedia.org/wiki/ZCZ-011

... is a negative allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 ZCZ-011 German N, Decker AM, ... "Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure-Activity Relationship Studies on 1-(4- ... Cannabinoids, CB1 receptor antagonists, Aminopyridines, All stub articles, Cannabinoid stubs). ... a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats". British Journal of Pharmacology. ...

https://en.wikipedia.org/wiki/PSNCBAM-1

Foster MD (2011). Computational study of RTI-371, a positive allosteric modulator of the cannabinoid CB1 receptor (PDF) (MSc ... "Positive allosteric modulation of the human cannabinoid (CB) receptor by RTI-371, a selective inhibitor of the dopamine ... It may be caused by lack of BBB penetration, or interactions at alternative receptor sites. List of cocaine analogues List of ...

https://en.wikipedia.org/wiki/RTI-371

Additionally, indometacin has recently been found to be a positive allosteric modulator (PAM) of the CB1 cannabinoid receptor. ... 2019-10-18). "Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling". Frontiers in Molecular Neuroscience. 12: 257. doi: ... By enhancing the binding and signalling of endogenous cannabinoids such as anandamide, PAMs may elicit increased cannabinergic ...

https://en.wikipedia.org/wiki/Indometacin

Cannabinoids (e.g., nabilone, tetrahydrocannabinol (THC)/cannabis) - cannabinoid receptor modulators NMDA receptor modulators ( ... dopamine receptor agonist, serotonin receptor modulator, adrenergic receptor modulator, and serotonin reuptake inhibitor [19] ... glutamate modulator [2] Cannabis extracts (various) - cannabinoid receptor modulators [3] 4'-Fluorocannabidiol (4'-F-CBD; ... cannabinoid receptor modulator, other actions [4] AbbVie/Rugen research programme - unspecified mechanism of action [5] ...

https://en.wikipedia.org/wiki/List_of_investigational_obsessive–compulsive_disorder_drugs

September 2002). "C-3 Amido-indole cannabinoid receptor modulators". Bioorganic & Medicinal Chemistry Letters. 12 (17): 2399- ... AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2, with ... May 2010). "Brain cannabinoid CB2 receptor in schizophrenia". Biological Psychiatry. 67 (10): 974-82. doi:10.1016/j.biopsych. ... Morgan NH, Stanford IM, Woodhall GL (September 2009). "Functional CB2 type cannabinoid receptors at CNS synapses". ...

https://en.wikipedia.org/wiki/AM-630

... is a drug which acts as a potent and selective negative allosteric modulator of the cannabinoid CB1 receptor. Studies ... Cannabinoids, CB1 receptor antagonists, All stub articles, Cannabinoid stubs). ... "Allosteric modulation of the cannabinoid CB1 receptor". Molecular Pharmacology. 68 (5): 1484-95. doi:10.1124/mol.105.016162. ... However while Org 27569 increases the ability of CB1 agonists to bind to the receptor, it decreases their efficacy at ...

https://en.wikipedia.org/wiki/Org_27569

It is shown that pepcan-12 opposite acts as a potent CB2 cannabinoid receptor positive allosteric modulator (PAM). This peptide ... shown to act as negative allosteric modulators (NAM) of cannabinoid CB1 receptors. ... Recently it was shown that RVD-Hpα (also called Pepcan-12) is a potent negative allosteric modulator at CB1 receptors, together ... is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage". ...

https://en.wikipedia.org/wiki/RVD-Hpα

GABAA receptor positive allosteric modulators, Cannabinoids, Biphenyls, Lignans, Phenols, Allyl compounds). ... It is known to act on the GABAA receptors in rat cells in vitro as well as having antifungal properties. Magnolol has a number ... Magnolol is also binding in dimeric mode to PPARγ, acting as an agonist of this nuclear receptor. Magnolol at Sigma-Aldrich Lee ... Ai, Jinglu; Wang, Xiaomei; Nielsen, Mogens (2001). "Honokiol and Magnolol Selectively Interact with GABAA Receptor Subtypes in ...

https://en.wikipedia.org/wiki/Magnolol

"Cannabinoid Receptor Modulators, Their Processes of Preparation, and Use of Cannabinoid Receptor Modulators in Treating ... A comparatively safe new synthetic cannabinoid receptor agonist entering the NPS market?". Drug Testing and Analysis. 11 (2): ... A review of the chemistry and pharmacology of newly emerging heterocyclic synthetic cannabinoid receptor agonists". Drug ... Cannabinoids, Designer drugs, Gamma-Carbolines, All stub articles, Cannabinoid stubs). ...

https://en.wikipedia.org/wiki/CUMYL-PEGACLONE

... to be at least contributing in part by being a non competitive negative allosteric modulator of the Cannabinoid receptor type 1 ...

https://en.wikipedia.org/wiki/7-Hydroxycannabidiol

Cannabinoids, GABAA receptor positive allosteric modulators). ... 4-O-Methylhonokiol is a CB2 receptor ligand (Ki = 50 nM), ... Gertsch, Anavi-Goffer (2012). "Methylhonokiol attenuates neuroinflammation: a role for cannabinoid receptors?". Journal of ... "Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists". ... 4-O-Methylhonokiol activates CB2 receptors and also inhibits the oxygenation of the major endocannabinoid 2-AG via COX-2 in a ...

https://en.wikipedia.org/wiki/4-O-Methylhonokiol

GABAA receptor positive allosteric modulators, Cannabinoids, Biphenyls, Allyl compounds). ... Honokiol is a weak cannabinoid CB2 receptor ligand but the naturally occurring derivative 4-O-methylhonokiol was shown to be a ... "Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB2 Receptor Inverse Agonists". ... GABAA receptors control ligand-gated Cl− channels that can help increase seizure thresholds through the influx of chloride ...

https://en.wikipedia.org/wiki/Honokiol

... cannabinoid receptor modulator and gabapentinoid [30] Ciforadenant (CPI-444, V-81444) - adenosine A2A receptor antagonist [31] ... cannabinoid receptor modulators [56] Norepinephrine reuptake inhibitors / adrenergic receptor antagonists [Pfizer] (NRI-022, ... dopamine D2 receptor antagonist and serotonin receptor modulator (e.g., serotonin 5-HT2B and 5-HT2A receptor antagonist) - ... AMPA receptor modulator [71] CX-1739 - ampakine / AMPA receptor modulator [72] Donepezil (Aricept, Aricept D, Aricept Dry Syrup ...

https://en.wikipedia.org/wiki/List_of_investigational_attention_deficit_hyperactivity_disorder_drugs

In 2018, a study showed that perrottetinene is moderately psychoactive through activation of the cannabinoid receptor 1. The ... are they new cannabinoidergic modulators? Planta. 2019 Jun;249(6):1681-1694. doi:10.1007/s00425-019-03138-x PMID 30877436 ... Cannabinoids, Benzochromenes, Phenols, All stub articles, Cannabinoid stubs). ... Perrottetinene is a naturally occurring cannabinoid compound found in liverworts from the genus Radula native to Japan, New ...

https://en.wikipedia.org/wiki/Perrottetinene

CBD also acts as an allosteric modulator of the μ- and δ-opioid receptors. THC also potentiates the effects of the glycine ... Xiong W, Cheng K, Cui T, Godlewski G, Rice KC, Xu Y, Zhang L (May 2011). "Cannabinoid potentiation of glycine receptors ... the CB1 receptor and the CB2 receptor, both of which are G protein-coupled receptors. The CB1 receptor is found primarily in ... Researchers confirmed that THC exerts its most prominent effects via its actions on two types of cannabinoid receptors, ...

https://en.wikipedia.org/wiki/Cannabis_(drug)

... cannabinoid receptor modulator [24] CMX-020 - TRPV1 modulator as well as CB1 and CB2 receptor modulator [25] Dronabinol (Δ9-THC ... Cebranopadol (GRT-6005) - non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid ... TRPV1 modulator as well as CB1 and CB2 receptor modulator [12] DWP-05195 (TR-1) - TRPV1 antagonist [13] GRC-6211 - TRPV1 ... LNGF receptor (p75NTR) fusion protein and decoy receptor for nerve growth factor [36] NRD135S-E1 - tyrosine kinase modulator[37 ...

https://en.wikipedia.org/wiki/List_of_investigational_analgesics

For example, SSRIs, SNRIs and tricyclic antidepressants acting on serotonin, norepinephrine, dopamine and cannabinoid receptors ... including opioids and cannabinoids), COX inhibitors, acetylcholine modulators, melatonin analogs (such as Ramelton), adenosine ... by which cannabinoid CB1 receptors modulate the excitability of dorsal raphe serotonin neurons. Data suggest that the ... vanilloid-receptor agonists, catecholamine modulators, ion-channel blockers, anticonvulsants, GABA agonists ( ...

https://en.wikipedia.org/wiki/Psychoneuroimmunology

... and ghrelin receptor agonist Anabolic catabolic transforming agents such as MT-102 Selective androgen receptor modulators ... Appetite stimulants include glucocorticoids, cannabinoids, or progestins such as megestrol acetate. Anti-emetics such as 5-HT3 ... NF-κB is a known regulator of the genes that encode cytokines and cytokine receptors. The increased production of cytokines ... Thalidomide Cytokine antagonists Cannabinoids Omega-3 fatty acids, including eicosapentaenoic acid (EPA) Non-steroidal anti- ...

https://en.wikipedia.org/wiki/Cachexia

... transmitters and modulators involved in their complex response at molecular and cellular level. The control and regulation ... were discovered to exist in the brain and have specific receptors in it, by investigations on the mechanism of action of ... Endorphins Dynorphin Bradykinin Prostaglandins Angiotensin Secretin Gastrin Cholecystokinin Histamine Cannabinoids Substance P ... The main scientific criterion for an autopharmacological agent is the discovery of specific membrane receptors for it and, ...

https://en.wikipedia.org/wiki/Autopharmacology

It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors. Longer forms of hemopressin containing 2-3 ... recently been shown to be a negative allosteric modulator of CB1 receptors and positive allosteric modulator of CB2 receptors [ ... May 2010). "The peptide hemopressin acts through CB1 cannabinoid receptors to reduce food intake in rats and mice". J. Neurosci ... December 2007). "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proc. Natl. Acad. Sci. U.S.A. 104 (51): 20588 ...

https://en.wikipedia.org/wiki/Hemopressin

... which are believed to relate to the inhibition of the constitutive activity of the cannabinoid receptor. The GABAA receptor has ... Allosteric modulators: They do not bind to the agonist-binding site of the receptor but instead on specific allosteric binding ... The insulin receptor is an example. Type 4: Nuclear receptors - While they are called nuclear receptors, they are actually ... Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule ...

https://en.wikipedia.org/wiki/Receptor_(biochemistry)

2016: The marijuana receptor-human Cannabinoid receptor type 1 (CB1) and the human C-C chemokine receptor type 2 (CCR2) 2017: ... "Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators" Nature 546, 312-315 (2017). (not NIH ... the human cannabinoid receptor CB2, the human neurokinin 1 receptor, and the melatonin receptors MT1 and MT2 2020:The human ... 2013: Serotonin receptors 5-HT1B and 5-HT2B, the second HIV co-receptor, C-C chemokine receptor type 5 (CCR5) and the first ...

https://en.wikipedia.org/wiki/Raymond_C._Stevens

MENT Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor ligands. They are intended to ... "A new cannabinoid receptor 1 selective agonist evading the 2021 'China ban': ADB-FUBIATA". Drug Testing and Analysis. 14 (9): ... Zhang X, Sui Z (February 2013). "Deciphering the selective androgen receptor modulators paradigm". Expert Opinion on Drug ... APP-CHMINACA SDB-005 THJ-018 THJ-2201 Indole containing cannabinoid receptor agonists include: 4-HTMPIPO 4F-MDMB-BICA 5C-MN-24 ...

https://en.wikipedia.org/wiki/List_of_designer_drugs

"The Endocrine Disruptor Monoethyl-hexyl-phthalate Is a Selective Peroxisome Proliferator-activated Receptor γ Modulator That ... additionally mimic lipid activators of the cannabinoid system and inhibit AMPK activity. Endocannaboid levels are high in those ... the PPAR receptors must heterodimerize with another receptor known as the 9-cis retinoic acid receptor (RXR). The RXR receptor ... Often the function of these receptors overlaps with metabolism regulation, such as that of the H1 receptor which when activated ...

https://en.wikipedia.org/wiki/Obesogen

Other targets that are affected by alcohol include cannabinoid, opioid and dopamine receptors, although it is unclear whether ... At low or moderate doses, alcohol acts primarily as a positive allosteric modulator of GABAA. Alcohol binds to several ... Alteration of NMDA receptor numbers in chronic alcoholics is likely to be responsible for some of the symptoms seen in delirium ... NMDA receptors become unresponsive, slowing areas of the brain for which they are responsible. Contributing to this effect is ...

https://en.wikipedia.org/wiki/Short-term_effects_of_alcohol_consumption

Hotamisligil GS (June 1999). "The role of TNFalpha and TNF receptors in obesity and insulin resistance". Journal of Internal ... Turcotte C, Chouinard F, Lefebvre JS, Flamand N (June 2015). "Regulation of inflammation by cannabinoids, the endocannabinoids ... signaling system plays a critical role in motivational homeostasis as a conduit for reward stimuli and a positive modulator of ... Endocannabinoid-system hyperactivity through CB1 receptor transmission is considered contributory to a range of appetitive ...

https://en.wikipedia.org/wiki/Metabolic_syndrome

"Cannabinoid receptors couple to NMDA receptors to reduce the production of NO and the mobilization of zinc induced by glutamate ... Allosteric receptor binding sites for zinc, proteins and the polyamines spermidine and spermine are also modulators for the ... The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA and kainate receptors. ... The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in ...

https://en.wikipedia.org/wiki/NMDA_receptor

CB1 receptor agonists, GABAA receptor positive allosteric modulators, Monoamine oxidase inhibitors). ... It has been shown to possess binding affinity for the cannabinoid receptor CB1 (Ki = 0.72 μM), and selectivity vs. the CB2 ... The CB1 receptor affinity of yangonin suggests that the endocannabinoid system might contribute to the complex human ... The plant-derived yangonin is a novel CB1 receptor ligand". Pharmacological Research. 66 (2): 163-169. doi:10.1016/j.phrs. ...

https://en.wikipedia.org/wiki/Yangonin

... cannabinoid receptor modulator, antioxidant, other actions Basmisanil (RG-1662, RO-5186582) - GABAA receptor α5 subunit- ... NMDA receptor glycine-site positive allosteric modulator PF-4958242 - AMPA receptor positive allosteric modulator Pomaglumetad ... D2 receptor partial agonist, 5-HT2A receptor antagonist, other actions) F-17464 - D3 receptor antagonist, 5-HT1A receptor ... cannabinoid receptor modulator (phytocannabinoid-based chewing gum) Cannabidiol (CBD; GW-42003, GWP-42003, GWP-42003-P, ECP- ...

https://en.wikipedia.org/wiki/List_of_investigational_antipsychotics

Progesterone receptor modulators like mifepristone and gestrinone have the potential (based on only one RCT each) to be used as ... an IL-1 receptor antagonist. Promising preclinical outcomes is pushing clinical trials into testing cannabinoid extracts, ... Fu J, Song H, Zhou M, Zhu H, Wang Y, Chen H, Huang W (July 2017). "Progesterone receptor modulators for endometriosis". The ... A 2010 Cochrane review found that GnRH modulators were more effective for pain relief in endometriosis than no treatment or ...

https://en.wikipedia.org/wiki/Endometriosis

US 20180200225, Attala MN, Diaz P, "Hydrazone modulators of cannabinoid receptors", published 19 July 2018, assigned to ... in human cannabinoid receptors but functions differently in rat cannabinoid receptors binding to rat cannabinoid CB2 receptors ... The pharmacology of MDA-19 in rat cannabinoid receptors have been demonstrated to function differently than human cannabinoid ... MDA-19 (also known as BZO-HEXOXIZID) is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB2, ...

https://en.wikipedia.org/wiki/MDA-19

"Adenosine-cannabinoid receptor interactions. Implications for striatal function". Br. J. Pharmacol. 160 (3): 443-453. doi: ... Cherasse Y, Urade Y (November 2017). "Dietary Zinc Acts as a Sleep Modulator". International Journal of Molecular Sciences. 18 ... It has been demonstrated that D1 receptors form the hetero-oligomer with D2 receptors, and that the D1-D2 receptor hetero- ... Glucocorticoids and dopamine: Glucocorticoid receptors are the only corticosteroid receptors in the nucleus accumbens shell. L- ...

https://en.wikipedia.org/wiki/Nucleus_accumbens

In humans, the only post-synaptic receptor at which amphetamine is known to bind is the 5-HT1A receptor, where it acts as an ... Bozdag M, Altamimi AA, Vullo D, Supuran CT, Carta F (2019). "State of the Art on Carbonic Anhydrase Modulators for Biomedical ... It has been implicated in addictions to alcohol, cannabinoids, cocaine, methylphenidate, nicotine, opioids, phencyclidine, ... Amphetamine addiction is largely mediated through increased activation of dopamine receptors and co-localized NMDA receptors in ...

https://en.wikipedia.org/wiki/Amphetamine

Russell R, Gori I, Pellegrini C, Kumar R, Achtari C, Canny GO (Dec 2011). "Lipoxin A4 is a novel estrogen receptor modulator". ... It is found that the anti-inflammatory lipid lipoxin A4 is an endogenous allosteric enhancer of the CB1 cannabinoid receptor. ... FPR2, which is now termed the ALX, ALX/FPR, or ALX/FPR2 receptor, is a G protein coupled receptor initially identified as a ... LXA4 and 15-epi-LXA4 are high affinity receptor ligands for and activators of the FPR2 receptor. ...

https://en.wikipedia.org/wiki/Lipoxin

New Jersey specializing in positive allosteric modulators of the AMPA receptor known as Ampakines. In February 2005, Cortex ... a synthetic cannabinoid, also known as Δ9-tetrahydrocannabinol or Δ9-THC. News: Today's Orange County business briefs - ...

https://en.wikipedia.org/wiki/RespireRx

PEA cannot strictly be considered a classic endocannabinoid because it lacks affinity for the cannabinoid receptors CB1 and CB2 ... Palmitoylethanolamide (PEA) is an endogenous fatty acid amide, and lipid modulator PEA has been studied in in vitro and in vivo ... Phan NQ, Siepmann D, Gralow I, Ständer S (February 2010). "Adjuvant topical therapy with a cannabinoid receptor agonist in ... O'Sullivan SE, Kendall DA (August 2010). "Cannabinoid activation of peroxisome proliferator-activated receptors: potential for ...

https://en.wikipedia.org/wiki/Palmitoylethanolamide

... which indicates that prejunctional CB1 receptors mediate the sympatho-inhibitory action. Thus cannabinoids can inhibit both the ... September 2017). "Neurotransmitters: The Critical Modulators Regulating Gut-Brain Axis". Journal of Cellular Physiology. 232 (9 ... known as alpha and beta adrenergic receptors. Alpha receptors are divided into subtypes α1 and α2; beta receptors into subtypes ... depending on whether they primarily block alpha-1 receptors, alpha-2 receptors, or both. Alpha-2 receptors, as described ...

https://en.wikipedia.org/wiki/Norepinephrine

Cannabinoid Receptor Agonists. Cannabinoid Receptor Antagonists. Cannabinoid Receptor Modulators. Caspase Inhibitors. ... New Cannabinoid Receptors Modulator terms were created. The term Endocannabinoids was removed from the D27 category (Hormones, ... Receptors, Artificial. RNA, Long Untranslated. Single-Domain Antibodies. Sodium Channel Agonists. Tight Junction Proteins. ...

https://www.nlm.nih.gov/pubs/techbull/nd12/nd12_medline_data_changes_2013.html

Cannabinoid Receptor Modulators--physiology. Cerebellum--physiology. Synaptic Transmission--physiology. Publication Types: ...

https://videocast.nih.gov/watch=4361

MeSH Terms: Adult; Alcohol Drinking/prevention & control*; Cannabinoid Receptor Modulators/administration & dosage*; Female; ...

https://tools.niehs.nih.gov/portfolio/index.cfm?do=portfolio.publicationDetail&id=3912281

Examples of interest include: effectors of opioid, glutamate, GABA, cannabinoid, and adenosine receptors, modulators of ... Some examples are: a) target-based biochemical or cellular assays that measure activities of enzymes, receptor-ligand bindings ... Alcohol dependence is a complex disorder involving many neurotransmitter receptors and transporters, ion channels, ... and modulators of neuroimmune and neuroinflammatory pathways. In case a screening campaign yields promising bioactive hits, ...

https://grants.nih.gov/grants/guide/pa-files/PAR-14-279.html

Seven-transmembrane receptors signal via G-protein- and β-arrestin-dependent pathways. We describe a peripheral CB,sub,1,/sub,R ... The hepatic cannabinoid 1 receptor as a modulator of hepatic energy state and food intake. Cooper ME, Regnell SE. Cooper ME, et ... Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB1R) Antagonist Ziyi Liu 1 , Malliga R Iyer 1 , Grzegorz Godlewski ... Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB1R) Antagonist Ziyi Liu et al. ACS Pharmacol Transl Sci. 2021. . ...

https://www.ncbi.nlm.nih.gov/pubmed/?term=34151207

... bind to a recently discovered site on a cannabinoid brain receptor called CB1, but they do not bind to the typical THC receptor ... Hohmanns compounds, called positive allosteric modulators, or PAMs, ... THC stimulates cannabinoid receptors in the brain to release endocannabinoids, natural pain-relieving molecules. ... Researchers in recent years have attempted to create drug compounds that can target pain receptors in the brain but not affect ...

https://www.livescience.com/56876-marijuana-like-drugs-may-relieve-pain-without-addiction-risk.html

... cannabinoid, and adenosine receptors, modulators of neuropeptide systems (NPY, CRF, substance P), and agents that alter signal ... neurokinin receptors: NK1, NK2, NK3; heteromeric neuronal nicotinic receptor subunits; NMDA subunits; opioid receptors: mu, ... Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRF R1, CRF R2; ... G-protein coupled receptors, such as the dopamine receptor, an indirect site of action for cocaine and amphetamine, or ligand ...

https://grants.nih.gov/grants/guide/pa-files/PAR-13-087.html

Allosteric Targeting of Cannabinoid CB1 Receptor to Develop Non-Addictive Small Molecule Analgesics. LU, DAI. TEXAS A&M ... Novel mGlu5 negative allosteric modulators as first-in-class non-addictive analgesic therapeutics. ROOK, JERRI MICHELLE. ... Development of MRGPRX1 positive allosteric modulators as non-addictive therapies for neuropathic pain. TSUKAMOTO, TAKASHI JOHNS ... thrombin receptor antagonist), and Zetia® (ezetimibe). Prior to joining industry in 1987, he was Associate Professor of ...

https://www.ninds.nih.gov/current-research/trans-agency-activities/ninds-role-heal-initiative/pain-therapeutics-development-program-ptdp

Cannabinoid Receptor Modulators (2004-2012). Cannabinoids (1992-2003). Public MeSH Note. 2013. History Note. 2013(2004). Date ... They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR ... They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR ... Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. ...

https://meshb.nlm.nih.gov/record/ui?ui=D063388

Cannabinoid Receptor Modulators [D27.505.696.399.472.188] * Cannabinoid Receptor Agonists [D27.505.696.399.472.188.500] ... Cannabinoid Receptor Modulators [D27.505.519.625.085] * Cannabinoid Receptor Agonists [D27.505.519.625.085.500] ... Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS.. Terms. Cannabinoid Receptor Modulators ... Cannabinoid Receptor Modulators. Tree Number(s). D27.505.519.625.085. D27.505.696.399.472.188. Unique ID. D063385. RDF Unique ...

https://meshb-prev.nlm.nih.gov/record/ui?ui=D063385

Cannabinoid Receptor Modulators (2004-2012). Cannabinoids (1992-2003). Public MeSH Note:. 2013. ... They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR ... They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR ... Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. ...

https://decs.bvsalud.org/en/ths/resource/?id=38329&filter=ths_exact_term&q=ENDOCANABINOIDES

See also: Cannabinoid receptor modulators (cannabinoids by pharmacology). *List of: AM cannabinoids ... RCS-8 (also known as 1-(2-cyclohexylethyl)-3-(2-methoxyphenylacetyl)indole, SR-18, and BTM-8) is a synthetic cannabinoid that ... CB1 & CB2 receptors role in Cancer Texas Health Co-op is a subsidiary, in name reservation only, of Good Acts LLC. read more » ... Clinical Application of Cannabinoids and Terpenes , M. Gordon,. April 18, 2017. The complexity of medical cannabis stems from ...

https://thcscience.wiki/term/cannabaceae/cannabis/cannabis-ruderalis/?rdp_we_resource=https%3A%2F%2Fen.wikipedia.org%2Fwiki%2FRCS-8

A Cannabinoid CB 1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects. ...

https://abdn.pure.elsevier.com/en/publications/?ordering=title&descending=false&showAdvanced=false&allConcepts=true&inferConcepts=true&publicationYear=2019&author=6b3900ce-ef7e-44f2-93bf-e1791f86fc46&format=&nofollow=true&page=16

Cannabinoid Receptor Modulators, Their Processes Of Preparation, And Use Of Cannabinoid Receptor Modulators For Treating ... Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is ... Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation ... partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor. ...

https://clubset.com/profile/John-Tokarski-EPGYCw

Cannabinoid receptor 1 positive allosteric modulator (GAT229) attenuates cisplatin-induced neuropathic pain in mice. ... Activating the cannabinoid receptor type 1 (CB1) by orthosteric agonists has shown promising results in alleviating the pain ... The CB1 receptor antagonist/inverse agonist AM251 blocked GAT229-mediated beneficial effects. According to our data, we suggest ... Unlike the CB1 orthosteric agonists, CB1 positive allosteric modulators (PAMs) dont produce any psychoactive effects, ...

https://pesquisa.bvsalud.org/portal/?lang=pt&q=au:Rasheed,+A

Cholesterol as a modulator of cannabinoid CB2 Yeliseev, A.; Iyer, M. R.; Joseph, T.T.; Coffey, N. J.; Cinar, R.; Zoubak. L.; ... Cannabinoid Receptor Mediating Compounds. Inventors: Kunos, G.; Iyer M R.; Cinar, R.; Rice, K. C Patent number: 9765031 ... Crystal Structure of Human Cannabinoid Receptor CB2. Li, X.; Hua, T.; Vemuri, K.; Ho, Jo-Hao.; Wu, Y.; Wu, L.; Katrich, V.; ... Pyrazole Derivatives and their Use as Cannabinoid Receptor Mediators. Inventors: Kunos, G.; Iyer M R.; Cinar, R.; Rice, K. C ...

https://www.niaaa.nih.gov/research/intramural-research/labs/section-medicinal-chemistry

Cannabinoid Receptor Meditating Compounds for Metabolic Disease *Read more about Cannabinoid Receptor Meditating Compounds for ... Treatment for Wolfram Syndrome and Other Endoplasmic Reticulum Stress Disorders with Endoplasmic Reticulum Calcium Modulators * ... There is evidence that the metabolic effects of endocannabinoids are mediated by CB1 receptors in peripheral tissues. While ... inventors at NIH have discovered compounds that block CB1 receptors with reduced brain penetrance. In addition, some of these ...

https://www.techtransfer.nih.gov/taxonomy/term/199?page=1

Cholesterol as a modulator of cannabinoid receptor CB(2) signaling. Sci Rep. 2021;11(1):3706. ... Cannabinoformins: Designing Biguanide-Embedded, Orally Available, Peripherally Selective Cannabinoid-1 Receptor Antagonists for ... Kenner Rice at NIDA studying the medicinal chemistry of opioid receptors and sigma receptors in substance use disorders towards ... Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB(1)R) Receptor with Reduced Lipophilicity. J Med Chem. 2022;65(3):2374-2387. ...

https://irp.nih.gov/pi/malliga-iyer

Munro, S., Thomas, K. L. & Abu-Shaar, M. (1993). Molecular characterization of a peripheral receptor for cannabinoids. Nature, ... Endogenous cannabinoid system as a modulator of food intake. Int J Obes, 27, 289-301. [ Links ]. ... Di Marzo, V., Melck, D., Bisogno, T. & De Petrocellis, L. (1998). Endocannabinoid: endogenous cannabinoid receptor ligands with ... Elevated cannabinoid 1 receptor mRNA is linked to eating disorder related behavior and attitudes in females with eating ...

http://pepsic.bvsalud.org/scielo.php?script=sci_arttext&pid=S0103-56652012000100011

... we have focused on the role of the type-1 cannabinoid receptor (CB1R), a highly abundant G-protein coupled receptor (GPCR) in ... ATP, via purinergic P2X receptors, acts as a neurotransmitter and modulator in both the central and peripheral nervous systems ... Cannabinoid Receptors Modulate Neuronal Morphology and AnkyrinG Density at the Axon Initial Segment. ... Of these, the P2X7 receptor was the only functional receptor, as its activation induced intracellular calcium increments ...

https://pesquisa.bvsalud.org/brasil/?lang=pt&q=au:Del+Puerto,+Ana

G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacological Reviews. Molecular Medicine. Pharmacology ... Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2. Pharmacological Reviews. Molecular Medicine. Pharmacology. ...

https://research.amanote.com/publication/search?category=Pharmacology&page=1

8. The use of selective estrogen receptor modulators and selective estrogen receptor down-regulators in breast cancer.. Howell ... 6. Tamoxifen Isomers and Metabolites Exhibit Distinct Affinity and Activity at Cannabinoid Receptors: Potential Scaffold for ... 4. Regulation of aryl hydrocarbon receptor function by selective estrogen receptor modulators.. DuSell CD; Nelson ER; Wittmann ... MiRNA-27a sensitizes breast cancer cells to treatment with Selective Estrogen Receptor Modulators.. Ljepoja B; García-Roman J; ...

https://pubmedhh.nlm.nih.gov/biomarkers/search.php?id=37369286&mod=related&page=1&from=&outid=&proj=

3 ?Endocannabinoid Modulators The endocannabinoid system is a group of cannabinoid receptors located in the brain and ... solventfree CO2 extraction process All of FABs products are superclean and are loaded with beneficial cannabinoids and ...

https://www.velveta.cz/Paste/Fd6b70_Cbd-Cure/Oil-Gold-Paste

Development of selective cannabinoid receptor 2 agonists for treatment of addiction. Substance Use Disorder. Shamloo, Mehrdad. ... Development of a splicing modulator compound for familial dysautonomia. Familial Dysautonomia. Slaugenhaupt, Susan A. ...

https://neuroscienceblueprint.nih.gov/neurotherapeutics/blueprint-neurotherapeutics-network-bpn-small-molecules/drug-development-projects

Effects of mixed cannabinoid CB1/CB2 agonists, CB2-selective agonists, and modulators of the endocannabinoid system (i.e. ... Effects of genetic disruption of cannabinoid receptors or enzymes controlling endocannabinoid degradation on neuropathic ... STUDY: Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside. Written By. Cannabis Advisory ... Cannabinoids, drugs that share the same target as Δ9-tetrahydrocannabinol (Δ9-THC), the psychoactive ingredient in cannabis, ...

https://www.thecannabisadvisory.com/clinical-studies/health_condition/diabetes/study-cannabinoids-as-pharmacotherapies-for-neuropathic-pain-from-the-bench-to-the-bedside/

Compounds that inhibit or block the activity of CANNABINOID RECEPTORS. HN - 2013 MH - Cannabinoid Receptor Modulators UI - ... HN - 2013 FX - Cannabinoids FX - Endocannabinoids FX - Receptors, Cannabinoid MH - Cannabinoid Receptor Antagonists UI - ... They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR ... Cannabinoid Receptor Agonists UI - D063386 MN - D27.505.519.625.85.500 MN - D27.505.696.399.472.188.500 MS - Compounds that ...

https://nlmpubs.nlm.nih.gov/projects/mesh/.newterms/mshnew2013.old.txt

Specific topics of interest vary among Institutes, Centers, and Offices, but overall the research portfolio includes studies investigating the whole or parts of the Cannabis sativa plant, cannabis extracts or enriched extracts, cannabinoid compounds extracted and derived from cannabis extracts, non-cannabinoid constituents of cannabis, synthetic cannabinoids, and the components of the endocannabinoid system (the signaling pathways in the body activated by cannabinoids). (nih.gov)
as well as the physiological systems affected by cannabis (e.g., endocannabinoid system) and modulators thereof (e.g., fatty acid amide hydrolase [FAAH] inhibitors). (nih.gov)
The laboratory aims to exploit and maximize the therapeutic potential of the endocannabinoid system central and peripheral receptors with unique small molecule-based approaches. (nih.gov)
3 ?Endocannabinoid Modulators The endocannabinoid system is a group of cannabinoid receptors located in the brain and throughout the nervous system. (velveta.cz)
Effects of mixed cannabinoid CB 1 /CB 2 agonists, CB 2 -selective agonists, and modulators of the endocannabinoid system (i.e. inhibitors of transport or degradation) are compared. (thecannabisadvisory.com)
Here, you can learn about medicinal cannabis in general, including scientific information about cannabinoids and the body's endocannabinoid system. (wecare-medicalcannabis.com)
The endocannabinoid system (ECS) is a complex network of cell receptors , endocannabinoids, and enzymes that work together to regulate a variety of physiological processes in the body. (thehappycampers.com)
The endocannabinoid system (ECS) is a complex network of receptors, endocannabinoids (cannabinoids produced naturally by the body), and enzymes that work together to maintain balance in various physiological processes, including mood, appetite, pain, and inflammation. (thehappycampers.com)
When it comes to cannabis, we're talking about more than 100 cool cannabinoids that know how to party with the ECS (Endocannabinoid System) in all sorts of funky ways. (thehappycampers.com)
CBD is a modulator of the endocannabinoid system that controls the work of the other systems of our body. (verdeskin.co)
These receptors make up the body's endocannabinoid system. (verdeskin.co)

They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS . (nih.gov)
Disclosed are the coordinates for the crystal structure, and methods for determining agonists, partial agonists, antagonists, partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor. (clubset.com)
Gurgle HE, White K, McAdam-Marx C. SGLT2 inhibitors or GLP-1 receptor agonists as second-line therapy in type 2 diabetes: patient selection and perspectives. (uams.edu)
Cannabinoid agonists stimulate G protein-coupled receptors (GPCRs) by binding to an "orthosteric" site on the receptor, which initiates a series of micro-conformational changes in the receptor structure, that ultimately leads to G-activation. (lipocanna.com)

THC stimulates cannabinoid receptors in the brain to release endocannabinoids, natural pain-relieving molecules. (livescience.com)
Therapeutic Cannabinoid Research - This subset of the Cannabinoid Research category (above) reports all NIH projects examining the therapeutic properties of all classes of cannabinoids (endocannabinoids, phytocannabinoids, and synthetic). (nih.gov)
There is evidence that the metabolic effects of endocannabinoids are mediated by CB1 receptors in peripheral tissues. (nih.gov)
Vertebrates also produce their own cannabinoid-like substances called endocannabinoids, including anandamide and 2-arachidonoylglyceral. (medicalmarijuana411.com)
It works by speaking with receptors, blocking reuptake of the body endocannabinoids. (irelandoffline.com)
It's got three main players: endocannabinoids, receptors, and enzymes. (thehappycampers.com)
Endocannabinoids are like these natural superheroes that your body makes, and they're all about getting cozy with those ECS receptors. (thehappycampers.com)

Hohmann's compounds, called positive allosteric modulators, or PAMs, bind to a recently discovered site on a cannabinoid brain receptor called CB1, but they do not bind to the typical THC receptor or the opioid receptor. (livescience.com)
Here, we find that, unlike the phytocannabinoid Δ 9 -tetrahydrocannabinol, the indole-moiety containing SCs, AM2201 and JWH-018, act as positive allosteric modulators (PAMs) at the 5-HT 1A receptor (5-HT 1A R). This suggests that some biological effects of SCs might involve allosteric interactions with 5-HT 1A Rs. (nih.gov)
Here, we find that, unlike the phytocannabinoid Δ9-tetrahydrocannabinol, the indole-moiety containing SCs, AM2201 and JWH-018, act as positive allosteric modulators (PAMs) at the 5-HT1A receptor (5-HT1AR). (nih.gov)

Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB(1)R) Receptor with Reduced Lipophilicity. (nih.gov)
Cannabinoid antagonists block activation of G proteins by binding to an "allosteric" site on the receptor that is involved in the G protein activation process, thereby precluding the ability of the orthosteric agonist-mediated conformational stimulus to execute activation. (lipocanna.com)

The plant also contains more than 500 other chemicals, including more than 100 compounds that are chemically related to THC, called cannabinoids . (nih.gov)
Researchers in recent years have attempted to create drug compounds that can target pain receptors in the brain but not affect opioid receptors, the source for opioid addiction. (livescience.com)
Unlike marijuana or prescription opioids , the PAM compounds "do not hit every receptor everywhere," she added. (livescience.com)
Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS . (nih.gov)
The present invention provides compounds of formula IThe formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. (clubset.com)
The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors. (clubset.com)
While prior attempts at generating CB1 receptor blockers have had serious neuropsychiatric side effects, inventors at NIH have discovered compounds that block CB1 receptors with reduced brain penetrance. (nih.gov)
2. Characterization of new estrogen receptor destabilizing compounds: effects on estrogen-sensitive and tamoxifen-resistant breast cancer. (nih.gov)

16. Potential of endogenous estrogen receptor beta to influence the selective ER modulator ERbeta complex. (nih.gov)

Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide ( CGRP ) receptor antagonist with a K i of 0.027 nM and an IC 50 of 0.14 nM for hCGRP receptor [1] . (medchemexpress.com)
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC 50 of 0.03 nM and K i of 14.4 pM for human CGRP [1] [2] . (medchemexpress.com)
Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist. (medchemexpress.com)
CGRP antagonist 2 is a CGRP receptor antagonist. (medchemexpress.com)
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide ( CGRP ) receptor in the hindlimb vascular bed of the cat [1] [2] . (medchemexpress.com)
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH 2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. (medchemexpress.com)
International essential tremor in mainstream and movement, no studies appear to change in cannabinoid cb1 receptor antagonist, vogel z. (amanovaraonlus.it)

Cannabidiol Research - This subset of the Cannabinoid Research category (above) reports all NIH projects examining basic, preclinical, and therapeutic properties of cannabidiol (CBD). (nih.gov)
Our previous studies showed that the non-psychoactive cannabinoid, cannabidiol (CBD), ameliorates the clinical symptoms in mouse myelin oligodendrocyte glycoprotein (MOG)35-55-induced experimental autoimmune encephalomyelitis model of multiple sclerosis (MS) as well as decreases the memory MOG35-55-specific T cell (TMOG) proliferation and cytokine secretion including IL-17, a key autoimmune factor. (nih.gov)
Evidence that pre-cannabidiol is a powerful plant antibiotic was obtained and more recent investigations have demonstrated, to various degrees, antibacterial activity for the nonpsychotropic cannabinoids cannabichromene (CBC), cannabigerol (CBG), cannabidiol (CBD) and tetrahydrocannabidiol (THC). (medicalmarijuana411.com)
Cannabidiol CBD and furthermore its sister compound tetrahydrocannabinol are both cannabinoids in cannabis. (irelandoffline.com)
4 The two most researched and most used cannabinoids are Δ 9 -tetrahydrocannabinol (THC) and cannabidiol (CBD). (wecare-medicalcannabis.com)
CBD (or cannabidiol) is the second most studied cannabinoid. (wecare-medicalcannabis.com)

Design, Synthesis and Biological Evaluation of Novel Non-Brain Penetrant Hybrid Cannabinoid CB 1 R inverse agonist/inducible nitric oxide synthase (iNOS) inhibitors for the treatment of liver fibrosis. (nih.gov)
This differentiates these cannabinoids from cyclooxygenase-2 inhibitors that suppress the synthesis of eicosanoids that promote the induction of the inflammatory process. (medicalmarijuana411.com)

Today's findings reveal a better understanding of the body's cannabinoid system and how to modulate it," said Margaret Haney, a drug-abuse expert at Columbia University in New York who was not associated with either research project. (livescience.com)

She trained as a postdoctoral fellow with Dr. Kenner Rice at NIDA studying the medicinal chemistry of opioid receptors and sigma receptors in substance use disorders towards developing non-addicting pharmacotherapies. (nih.gov)

CBD is also a receptor modulator, supporting it can improve or forestall the transmission of signs between cell receptors. (irelandoffline.com)

CBD's activation of serotonin receptors allows your body to make use of already existing serotonin molecules more efficiently. (onlinesrs.co)

RCS-8 (also known as 1-(2-cyclohexylethyl)-3-(2-methoxyphenylacetyl)indole , SR-18 , and BTM-8 ) is a synthetic cannabinoid that has been found as an ingredient of "herbal" synthetic cannabis blends. (thcscience.wiki)
The nonmedical (i.e., recreational) misuse of synthetic cannabinoids (SCs) is a worldwide public health problem. (nih.gov)

1. Evaluation of a polymeric topical formulation of Endoxifen in an estrogen receptor positive breast cancer murine model. (nih.gov)
3. Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model. (nih.gov)
4. Regulation of aryl hydrocarbon receptor function by selective estrogen receptor modulators. (nih.gov)
5. Effectiveness of Selective Estrogen Receptor Modulators in Breast Cancer Therapy: An Update. (nih.gov)
8. The use of selective estrogen receptor modulators and selective estrogen receptor down-regulators in breast cancer. (nih.gov)
10. MiRNA-27a sensitizes breast cancer cells to treatment with Selective Estrogen Receptor Modulators. (nih.gov)
11. Acquired resistance to selective estrogen receptor modulators (SERMs) in clinical practice (tamoxifen & raloxifene) by selection pressure in breast cancer cell populations. (nih.gov)
13. Effects of SERM (selective estrogen receptor modulator) treatment on growth and proliferation in the rat uterus. (nih.gov)

Recently, the orphan G protein-coupled receptor 55 (GPR55) was proposed to be an atypical cannabinoid receptor. (medicalmarijuana411.com)
CGRP receptor is a heterodimer formed by calcitonin-receptor-like receptor (CRLR), a type II (family B) G-protein-coupled receptor, and receptor-activity-modifying protein 1 (RAMP1), a single-membrane-pass protein. (medchemexpress.com)
7 Beyond its activity at the CB 1 and CB 2 receptors, THC may also interact with other receptors, including TRPA 1 (Transient Receptor Potential Cation Channel Subfamily A 11 Member 1), TRPV 2 (Transient Receptor Potential Cation Channel Subfamily V Member 2), GPR 55 (G Protein Coupled Receptor 55), 5-HT 3A (5-Hydroxytryptamine Receptor Type 3 Subunit A), and other receptors. (wecare-medicalcannabis.com)
7 CBD interacts with a range of receptors to elicit these properties, including TRPV 1 (Transient Receptor Potential Cation Channel Subfamily V Member 1), GPR 55 (G Protein Coupled Receptor 55), 5-HT 1A (5-Hydroxytryptamine Receptor Type 1 Subunit A), 5-HT 2A (5-Hydroxytryptamine Receptor Type 2 Subunit A), adenosine receptors A 1 & A 2 , TNFα (Tumor Necrosis Factor Alpha), and other receptors. (wecare-medicalcannabis.com)

Both end cannabinoids in our own bodies are additionally 2-arachidonoylglycerol and anandamide. (irelandoffline.com)

Cannabinoids, drugs that share the same target as Δ 9 -tetrahydrocannabinol (Δ 9 -THC), the psychoactive ingredient in cannabis, have the potential to address this unmet need. (thecannabisadvisory.com)
THC (or Δ 9 -tetrahydrocannabinol) is the primary psychoactive cannabinoid. (wecare-medicalcannabis.com)

First up, we've got delta-9-tetrahydrocannabinol (THC), the rockstar of cannabinoids. (thehappycampers.com)

Cannabinoid Research - This category reports the total NIH investment in all cannabinoid research including basic research, animal and human preclinical studies, and clinical research. (nih.gov)
Here, we review studies evaluating cannabinoids for neuropathic pain management in the clinical and preclinical literature. (thecannabisadvisory.com)
Clinical studies largely affirm that neuropathic pain patients derive benefits from cannabinoid treatment. (thecannabisadvisory.com)
Despite the ongoing political debate regarding the legality of medical marijuana, clinical investigations of the therapeutic use of cannabinoids are now more prevalent than at any time in history. (medicalmarijuana411.com)
5 These other cannabinoids, including cannabidiravin (CBDV), cannabigerol (CBG) or cannabichromene (CBC), have shown pharmacological activity at a pre-clinical level. (wecare-medicalcannabis.com)
5 Much of our knowledge about these cannabinoids is derived from in vitro and in vivo studies and a limited number of well-conducted, rigorous clinical studies. (wecare-medicalcannabis.com)

In 1995, researchers (Mechoulam et.al) discovered that the two receptors (now deemed the CB1 and CB2 receptors) were found not only in rats, but within thousands of other species (including humans). (lipocanna.com)

solventfree CO2 extraction process All of FABs products are superclean and are loaded with beneficial cannabinoids and healthboosting terpenes. (velveta.cz)

However, safe medicines based on cannabinoid chemicals derived from the marijuana plant have been available for decades and more are being developed. (nih.gov)
Cannabinoids, the active ingredients in marijuana, have dramatic effects on various organ systems. (medicalmarijuana411.com)

Another group of researchers, led by Jason Clapper, a scientist at Abide Therapeutics in San Diego, took a different approach and developed a compound that indirectly increased the amount of natural cannabinoids in the brains of rats, which relieved the animals' chronic pain symptoms . (livescience.com)
Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. (clubset.com)

6. Tamoxifen Isomers and Metabolites Exhibit Distinct Affinity and Activity at Cannabinoid Receptors: Potential Scaffold for Drug Development. (nih.gov)
Cannabis brings up to 1% delta-8 THC and as much as 20% CBD Delta-8 is an analog of delta-9 THC, indicating it has a similar molecular structure and affinity with your cannabinoid receptors (causes a blissful high). (onlinesrs.co)

Furthermore, CBD enhanced the transcription of oxidative stress modulators with potent anti-inflammatory activity that are controlled by Nfe2l2/Nrf2 (Mt1, Mt2a, Slc30a1, Hmox1). (nih.gov)

Cholesterol as a modulator of cannabinoid CB 2 Yeliseev, A. (nih.gov)

Finally, limitations of cannabinoid pharmacotherapies are discussed together with directions for future research. (thecannabisadvisory.com)

In 2015, NIH developed three reporting categories to describe and account for the research efforts underway to examine the chemical, physiological, and therapeutic properties of cannabinoids and the physiological systems they affect. (nih.gov)

Effects of genetic disruption of cannabinoid receptors or enzymes controlling endocannabinoid degradation on neuropathic nociception are described. (thecannabisadvisory.com)
The ECS was discovered in 1992, by Raphael Mechoulam (Hebrew University of Jerusalem), who observed that the ECS facilitates homeostasis through an elaborate, interactive, signaling scheme , involving cannabinoids, receptors and their regulatory enzymes. (lipocanna.com)

Desde la segunda quincena de marzo de 2020, se observó un 64,2 % de disminución en la aplicación de vacunas. (bvsalud.org)

The complexity of medical cannabis stems from the millions of combinations of doses and cannabinoid/terpene profiles. (thcscience.wiki)

Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS . (nih.gov)

We found that both 5-HT 1A R effects were potentiated by AM2201, suggesting that PAM activity at 5-HT 1A R may represent a novel noncannabinoid receptor mechanism underlying the complex profile of effects for certain SCs. (nih.gov)
By demonstrating that these "knock out" rats could did not get "high", they proved that "binding to CB1 receptors" is the mechanism by which THC works. (lipocanna.com)

After a research fellowship with Dr. George Kunos at NIAAA, she led a Medicinal Chemistry Core Program at NIAAA to develop translational approaches targeting the peripheral CB1 receptors. (nih.gov)
CB1 receptors are all up in your brain and central nervous system, while CB2 receptors are like the popular kids, hanging out in your immune system and peripheral tissues. (thehappycampers.com)

When the cannabis plant is mature, it produces an oil containing chemicals called cannabinoids. (wecare-medicalcannabis.com)
Just like these plant-derived medicines, the term 'cannabis-based medicines' refers to any medicine that is based on cannabinoids extracted from the cannabis plant. (wecare-medicalcannabis.com)
Cannabinoids are a group of chemicals produced by the cannabis plant. (wecare-medicalcannabis.com)
The cannabis plant contains over 100 cannabinoids. (wecare-medicalcannabis.com)
4 Other cannabinoids, which are normally present at low or very low concentrations in the cannabis plant, are being actively studied. (wecare-medicalcannabis.com)
The ECS is also the target of cannabinoids found in the cannabis plant, such as THC and CBD, which can interact with the ECS to produce various effects. (thehappycampers.com)

9. ERK/MAPK regulates ERRγ expression, transcriptional activity and receptor-mediated tamoxifen resistance in ER+ breast cancer. (nih.gov)
β-CGRP, human (Human β-CGRP) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC 50 s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells [1] . (medchemexpress.com)
It's more of a modulator, tweaking the activity of those receptors and keeping them on their toes. (thehappycampers.com)

partial agonist) receptors, 7 while its psychotropic effects are typically mediated by CB 2 . (wecare-medicalcannabis.com)

Delta-8 https://optimisticmommy.com/can-hhc-gummies-be-bad-for-your-health/ and CBD are both naturally occurring cannabinoids present in cannabis (hemp and cannabis). (onlinesrs.co)

They exert their effects through two receptor types: CB1, primarily located in the brain, and CB2, primarily located in the immune system. (medicalmarijuana411.com)
This bad boy goes straight for the CB1 receptors in your brain and nervous system, giving you that trippy, mind-altering experience we all know and love. (thehappycampers.com)
Think of your brain as an ocean, an ecosystem inhabited by numerous species of fish-like neurotransmitters and their receptors, with currents of electricity connecting and delicately balancing all the different components. (ultimatehealthreport.com)
In 1988, Allyn Howlett and William Devane (Johns Hopkins University) discovered the first cannabinoid receptor in the brain of a rat. (lipocanna.com)
in 1990, Lisa Matsuda (National Institute of Mental Health) mapped the DNA sequence responsible for the expression of THC-sensitive receptors in a rat's brain. (lipocanna.com)

Dual Inhibition of CB1 Receptors and iNOS as a Potential Novel Approach to the Pharmacological Management of Acute and Long COVID-19. (nih.gov)
MINNESOTA - A University of Minnesota Medical School research team led by Kalpna Gupta, Ph.D., has discovered that cannabinoids offer a novel approach to ease the chronic and acute pain caused by sickle cell disease (SCD). (medicalmarijuana411.com)

To test this hypothesis, we examined effects of AM2201 on 5-HT 1A R agonist-activated G protein-coupled inwardly rectifying potassium channel currents in neurons in vitro and on the hypothermic response to 5-HT 1A R stimulation in mice lacking the cannabinoid receptor 1. (nih.gov)
Four hundred and nine people with a specified condition of insomnia completed 1056 medical cannabis administration sessions using the Releaf App TM educational software during which they recorded real-time ratings of self-perceived insomnia severity levels prior to and following consumption, experienced side effects, and product characteristics, including combustion method, cannabis subtypes, and/or major cannabinoid contents of cannabis consumed. (mdpi.com)

This is because CBD interacts with the CB1 and CB2 receptors. (verdeskin.co)

The cannabinoids are found to have particular application as neuroprotectants, for example in limiting neurological damage following ischemic insults, such as stroke and trauma, or in the treatment of neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease and HIV dementia. (medicalmarijuana411.com)

1 These cannabinoids have a range of medicinal properties. (wecare-medicalcannabis.com)
4 Medicinal cannabis products may contain primarily THC (THC-dominant), primarily CBD (CBD-dominant), or a balance of the two cannabinoids (balanced). (wecare-medicalcannabis.com)

produced in post-synaptic neurons, then travel backwards to pre-synaptic neurons in the CB1 receptor (retrograde signaling) to inhibit neurotransmitter release, which influences other chemical reactions, producing a cascade effect. (lipocanna.com)

They were able to alter the genetics of rats, producing "knock out" rats that lacked CB1 receptors. (lipocanna.com)

Cannabinoids in CBD help regulate emotions and appetite. (verdeskin.co)

Seven-transmembrane receptors signal via G-protein- and β-arrestin-dependent pathways. (nih.gov)

Anatomy27

Organisms12

Diseases14

Chemicals and Drugs123

Analytical, Diagnostic and Therapeutic Techniques and Equipment30

Psychiatry and Psychology8

Phenomena and Processes37

Disciplines and Occupations3

Information Science1

Health Care2

Biosynthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in circulating and tumoral macrophages. (1/954)

The endothelial component of cannabinoid-induced relaxation in rabbit mesenteric artery depends on gap junctional communication. (2/954)

Comparison of novel cannabinoid partial agonists and SR141716A in the guinea-pig small intestine. (3/954)

Reversal of dopamine D(2) receptor responses by an anandamide transport inhibitor. (4/954)

Endocannabinoid 2-arachidonyl glycerol is a full agonist through human type 2 cannabinoid receptor: antagonism by anandamide. (5/954)

Are anandamide and cannabinoid receptors involved in ethanol tolerance? A review of the evidence. (6/954)

Down-regulation of anandamide hydrolase in mouse uterus by sex hormones. (7/954)

Age dependent accumulation of N-acyl-ethanolamine phospholipids in ischemic rat brain. A (31)P NMR and enzyme activity study. (8/954)

Receptors, Cannabinoid

Cannabinoid Receptor Modulators

Receptor, Cannabinoid, CB1

Receptor, Cannabinoid, CB2

Cannabinoid Receptor Agonists

Selective Estrogen Receptor Modulators

Cannabinoids

Cannabinoid Receptor Antagonists

Endocannabinoids

Cyclohexanols

Benzoxazines

Dronabinol

Pyrazoles

Polyunsaturated Alkamides

Raloxifene

Piperidines

Receptors, Drug

Naphthalenes

Arachidonic Acids

Morpholines

Bornanes

Glycerides

Norpregnadienes

Estrogen Receptor Modulators

Cannabidiol

Amidohydrolases

Monoacylglycerol Lipases

Tamoxifen

Estrogen Antagonists

Analgesics

Dose-Response Relationship, Drug

Rats, Sprague-Dawley

Cannabinol

GABA Modulators

Thiophenes

Ligands

Cannabis

Propylene Glycols

Indoles

Estrogen Receptor alpha

Estradiol

Receptors, Estrogen

Ovariectomy

Receptors, Lysosphingolipid

Signal Transduction

Leiomyoma

Rats, Wistar

Toremifene

Mice, Inbred C57BL

Pyrrolidines

Tetrahydronaphthalenes

Receptors, Androgen

Estrogens

Oximes

Neurons

Mice, Knockout

Carbamates

Calcium Channel Blockers

Benzofurans

Brain

Androgens

Guanosine 5'-O-(3-Thiotriphosphate)

Drug Interactions

Hippocampus

Receptors, GABA-A

Benzodioxoles

Estrogen Receptor beta

Cells, Cultured

Drug Evaluation, Preclinical

Drug Inverse Agonism

Drug Design

Estrenes

Uterine Neoplasms

CHO Cells

Osteoporosis, Postmenopausal

Anabolic Agents

Aminophenols

Binding, Competitive

TRPV Cation Channels

Disease Models, Animal