A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
A class of histamine receptors discriminated by their pharmacology and mode of action. Most histamine H1 receptors operate through the inositol phosphate/diacylglycerol second messenger system. Among the many responses mediated by these receptors are smooth muscle contraction, increased vascular permeability, hormone release, and cerebral glyconeogenesis. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
The secretion of histamine from mast cell and basophil granules by exocytosis. This can be initiated by a number of factors, all of which involve binding of IgE, cross-linked by antigen, to the mast cell or basophil's Fc receptors. Once released, histamine binds to a number of different target cell receptors and exerts a wide variety of effects.
Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.
A histamine H2 receptor agonist that is often used to study the activity of histamine and its receptors.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
A histamine H2 receptor antagonist that is used as an anti-ulcer agent.
A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.
A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.
A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
An enzyme that catalyzes the transfer of a methyl group from S-adenosylmethionine to histamine, forming N-methylhistamine, the major metabolite of histamine in man. EC 2.1.1.8.
Drugs used for their actions on histaminergic systems. Included are drugs that act at histamine receptors, affect the life cycle of histamine, or affect the state of histaminergic cells.
A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
A family of hexahydropyridines.
An antagonist of histamine that appears to block both H2 and H3 histamine receptors. It has been used in the treatment of ulcers.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
An enzyme that catalyzes the decarboxylation of histidine to histamine and carbon dioxide. It requires pyridoxal phosphate in animal tissues, but not in microorganisms. EC 4.1.1.22.
A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment.
A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.
An undecenyl THIOUREA which may have topical anti-inflammatory activity.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat ASTHMA; HAY FEVER; URTICARIA; and RHINITIS; and also in veterinary applications. Tripelennamine is administered by various routes, including topically.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A potent mast cell degranulator. It is involved in histamine release.
A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.
Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.
Hydrochloric acid present in GASTRIC JUICE.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
Granulated cells that are found in almost all tissues, most abundantly in the skin and the gastrointestinal tract. Like the BASOPHILS, mast cells contain large amounts of HISTAMINE and HEPARIN. Unlike basophils, mast cells normally remain in the tissues and do not circulate in the blood. Mast cells, derived from the bone marrow stem cells, are regulated by the STEM CELL FACTOR.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
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.
A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
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 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.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.
A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.
A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.
Agents inhibiting the effect of narcotics on the central nervous system.
Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones.
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.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Compounds with two BENZENE rings fused to AZEPINES.
An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.
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.
A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
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.
Granular leukocytes characterized by a relatively pale-staining, lobate nucleus and cytoplasm containing coarse dark-staining granules of variable size and stainable by basic dyes.
Compounds with BENZENE fused to AZEPINES.
The liquid secretion of the stomach mucosa consisting of hydrochloric acid (GASTRIC ACID); PEPSINOGENS; INTRINSIC FACTOR; GASTRIN; MUCUS; and the bicarbonate ion (BICARBONATES). (From Best & Taylor's Physiological Basis of Medical Practice, 12th ed, p651)
A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.
Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)
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.
The distal and narrowest portion of the SMALL INTESTINE, between the JEJUNUM and the ILEOCECAL VALVE of the LARGE INTESTINE.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
An organ of digestion situated in the left upper quadrant of the abdomen between the termination of the ESOPHAGUS and the beginning of the DUODENUM.
One of the HISTAMINE H1 ANTAGONISTS with little sedative action. It is used in treatment of hay fever, rhinitis, allergic dermatoses, and pruritus.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
The cartilaginous and membranous tube descending from the larynx and branching into the right and left main bronchi.
A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
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)
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.
Elements of limited time intervals, contributing to particular results or situations.
A group of compounds that are derivatives of beta-methylacetylcholine (methacholine).
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Compounds based on a propanolamine attached via an OXYGEN atom to a phenoxy ring. The side chain is one carbon longer than PHENYLETHYLAMINES.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
The sudden, forceful, involuntary expulsion of air from the NOSE and MOUTH caused by irritation to the MUCOUS MEMBRANES of the upper RESPIRATORY TRACT.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
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.
Compounds containing phenyl-1-butanone.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
Area in the hypothalamus bounded medially by the mammillothalamic tract and the anterior column of the FORNIX (BRAIN). The medial edge of the INTERNAL CAPSULE and the subthalamic region form its lateral boundary. It contains the lateral hypothalamic nucleus, tuberomammillary nucleus, lateral tuberal nuclei, and fibers of the MEDIAL FOREBRAIN BUNDLE.
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Injections into the cerebral ventricles.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
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.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
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.
The observable response an animal makes to any situation.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Pyridines substituted in any position with an amino group. May be hydrogenated, but must retain at least one double bond.
Rounded or pyramidal cells of the GASTRIC GLANDS. They secrete HYDROCHLORIC ACID and produce gastric intrinsic factor, a glycoprotein that binds VITAMIN B12.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The larger air passages of the lungs arising from the terminal bifurcation of the TRACHEA. They include the largest two primary bronchi which branch out into secondary bronchi, and tertiary bronchi which extend into BRONCHIOLES and PULMONARY ALVEOLI.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
A subtype of enteroendocrine cells found in the gastrointestinal MUCOSA, particularly in the glands of PYLORIC ANTRUM; DUODENUM; and ILEUM. These cells secrete mainly SEROTONIN and some neuropeptides. Their secretory granules stain readily with silver (argentaffin stain).
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.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
The property of blood capillary ENDOTHELIUM that allows for the selective exchange of substances between the blood and surrounding tissues and through membranous barriers such as the BLOOD-AIR BARRIER; BLOOD-AQUEOUS BARRIER; BLOOD-BRAIN BARRIER; BLOOD-NERVE BARRIER; BLOOD-RETINAL BARRIER; and BLOOD-TESTIS BARRIER. Small lipid-soluble molecules such as carbon dioxide and oxygen move freely by diffusion. Water and water-soluble molecules cannot pass through the endothelial walls and are dependent on microscopic pores. These pores show narrow areas (TIGHT JUNCTIONS) which may limit large molecule movement.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Use of electric potential or currents to elicit biological responses.
Skin irritant and allergen used in the manufacture of polyurethane foams and other elastomers.
Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.
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.
Tests involving inhalation of allergens (nebulized or in dust form), nebulized pharmacologically active solutions (e.g., histamine, methacholine), or control solutions, followed by assessment of respiratory function. These tests are used in the diagnosis of asthma.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.
Established cell cultures that have the potential to propagate indefinitely.
A group of LEUKOTRIENES; (LTC4; LTD4; and LTE4) that is the major mediator of BRONCHOCONSTRICTION; HYPERSENSITIVITY; and other allergic reactions. Earlier studies described a "slow-reacting substance of ANAPHYLAXIS" released from lung by cobra venom or after anaphylactic shock. The relationship between SRS-A leukotrienes was established by UV which showed the presence of the conjugated triene. (From Merck Index, 11th ed)
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.
The rate dynamics in chemical or physical systems.
An immunoglobulin associated with MAST CELLS. Overexpression has been associated with allergic hypersensitivity (HYPERSENSITIVITY, IMMEDIATE).
The excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.
A chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.
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.
The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulchi. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.
Compounds with a BENZENE fused to IMIDAZOLES.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
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.
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.
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.
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.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
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.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
The physical activity of a human or an animal as a behavioral phenomenon.
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.
Narrowing of the caliber of the BRONCHI, physiologically or as a result of pharmacological intervention.
An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in URINARY INCONTINENCE, in MOTION SICKNESS, as an antispasmodic, and as a mydriatic and cycloplegic.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
A condition characterized by inactivity, decreased responsiveness to stimuli, and a tendency to maintain an immobile posture. The limbs tend to remain in whatever position they are placed (waxy flexibility). Catalepsy may be associated with PSYCHOTIC DISORDERS (e.g., SCHIZOPHRENIA, CATATONIC), nervous system drug toxicity, and other conditions.
The action of a drug in promoting or enhancing the effectiveness of another drug.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
The outer covering of the body that protects it from the environment. It is composed of the DERMIS and the EPIDERMIS.
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)
A group of compounds that contain the structure SO2NH2.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.
A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)
Compounds that inhibit the action of prostaglandins.
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.
The mucous lining of the NASAL CAVITY, including lining of the nostril (vestibule) and the OLFACTORY MUCOSA. Nasal mucosa consists of ciliated cells, GOBLET CELLS, brush cells, small granule cells, basal cells (STEM CELLS) and glands containing both mucous and serous cells.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A group of enzymes including those oxidizing primary monoamines, diamines, and histamine. They are copper proteins, and, as their action depends on a carbonyl group, they are sensitive to inhibition by semicarbazide.
Inflammation of the mucous membrane of the nose similar to that found in hay fever except that symptoms persist throughout the year. The causes are usually air-borne allergens, particularly dusts, feathers, molds, animal fur, etc.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)
Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.
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.
Seven membered heterocyclic rings containing a NITROGEN atom.
Purine bases found in body tissues and fluids and in some plants.
The giving of drugs, chemicals, or other substances by mouth.
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.
Compounds that contain a BENZENE ring fused to a furan ring.
A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.

Cimetidine transport in brush-border membrane vesicles from rat small intestine. (1/694)

In previous studies, sulfoxide metabolite was observed in animal and human intestinal perfusions of cimetidine and other H2-antagonists. A sequence of follow-up studies is ongoing to assess the intestinal contributions of drug metabolism and drug and metabolite transport to variable drug absorption. An evaluation of these contributions to absorption variability is carried out in isolated fractions of the absorptive cells to uncouple the processes involved. In this report, data is presented on the drug entry step from a study on [3H]cimetidine uptake into isolated brush-border membrane vesicles from rat small intestine. A saturable component for cimetidine uptake was characterized with a Vmax and Km (mean +/- S.E.M.) of 6.1 +/- 1.5 nmol/30s/mg protein and 8.4 +/- 2.0 mM, respectively. Initial binding, and possibly intravesicular uptake, was inhibited by other cationic compounds including ranitidine, procainamide, imipramine, erythromycin, and cysteamine but not by TEA or by the organic anion, probenecid. Initial uptake was not inhibited by amino acids methionine, cysteine, or histidine, by the metabolite cimetidine sulfoxide, or by inhibitors of cimetidine sulfoxidation, methimazole, and diisothiocyanostilbene-2,2'-disulfonic acid. Equilibrium uptake was inhibited by ranitidine, procainamide, and cysteamine but not by erythromycin or imipramine. Initial cimetidine uptake was stimulated by an outwardly directed H+ gradient, and efflux was enhanced by an inwardly directed H+ gradient. Collapse of the H+ gradient as well as voltage-clamping potential difference to zero significantly reduced initial cimetidine uptake. The data is supportive of both a cimetidine/H+ exchange mechanism and a driving-force contribution from an inside negative proton or cation diffusion potential.  (+info)

Helicobacter pylori eradication with proton pump inhibitor-based triple therapies and re-treatment with ranitidine bismuth citrate-based triple therapy. (2/694)

BACKGROUND: It has been suggested that short-term triple therapy comprising a proton pump inhibitor, plus clarithromycin and amoxycillin be used as first choice in treating H. pylori infection, while eradication failure patients should be further treated with a quadruple therapy. Nevertheless, conflicting results have been reported using these treatment regimens in different countries. METHODS: A total of 278 patients with H. pylori infection were randomised to receive one-week triple therapy, comprising clarithromycin 500 mg b.d., amoxycillin 1 g b.d., and either omeprazole 20 mg b.d. (OAC; 90 patients), or pantoprazole 40 mg b.d. (PAC; 95 patients), or lansoprazole 30 mg b.d. (LAC; 93 patients). H. pylori infection at entry, and eradication 4-6 weeks after therapy had ended, were assessed by rapid urease test and histology on biopsies from the antrum and the corpus. When eradication did not occur, patients were given a 2-week treatment comprising ranitidine bismuth citrate 400 mg b.d., tetracycline 500 mg t.d.s. and tinidazole 500 mg b.d. (RBTT). Eradication in these patients was assessed 4-6 weeks after conclusion of treatment by a further endoscopy. RESULTS: Six patients were lost to the follow-up. At the end of the first course of treatment, the overall H. pylori eradication rate was 78% (95% CI: 73-83) and 79% (95% CI: 75-84) at 'intention-to-treat' (ITT) and 'per protocol' (PP) analysis, respectively, without any statistically significant difference between treatment regimens, although a trend for better results with the omeprazole combination was observed. Moreover, H. pylori eradication was achieved in 82% (95% CI: 75-97) (ITT) and 86% (95% CI: 69-94) (PP) of 38 patients re-treated with RBTT regimen. CONCLUSIONS: Our data found that this short-term triple therapy is not a satisfactory treatment (< 80% eradication rate) for H. pylori infection. The 2-week triple therapy used as re-treatment in eradication failure patients yielded more promising results.  (+info)

Effect of Helicobacter pylori eradication on the natural history of duodenal ulcer disease. (3/694)

BACKGROUND: Duodenal ulcer disease is strongly associated with Helicobacter pylori infection of the gastric mucosa. Eradication of H pylori from the gastric mucosa in adults is associated with long term healing of ulcers. AIMS: To follow a cohort of children with duodenal ulcer disease for a minimum of two years after the eradication of H pylori. PATIENTS AND METHODS: Over a three year period, all children diagnosed with duodenal ulcer disease had their symptoms documented and their H pylori status evaluated. The histories of these children were carefully screened to determine previous symptoms and to document previous treatment regimens. RESULTS: Sixteen children were diagnosed with ulcers and 15 were available for treatment and long term follow up. The median age at which symptoms first occurred was 10.5 years (range, 6-14) and the median duration of symptoms was 24 months (range, 2-60). Ten of the children had been treated with H2 receptor antagonists for a median of 3.5 months (range, 1-60). Duodenal ulcers healed in all children after eradication of H pylori and all children have remained asymptomatic for a median of 37 months (range, 26-62). No child has required subsequent admission to hospital. CONCLUSION: Eradication of H pylori is very effective in the long term healing of duodenal ulcer disease. H pylori eradication should be the standard treatment for all infected children who present with duodenal ulcer disease.  (+info)

An evaluation of increasing doses of ranitidine for treatment of heartburn. (4/694)

BACKGROUND: This was a randomized, double-blind, placebo-controlled, multicentre, parallel group, dose-ranging trial of ranitidine tablets for relief of episodic heartburn. Adult out-patients who reported heartburn relieved by antacids at least seven times per week were eligible. METHODS: Patients who successfully completed a 1-week single-blind placebo run-in phase and who did not achieve adequate relief in more than 50% of heartburn episodes were randomized to a 1-week, double-blind treatment phase during which they received ranitidine doses of 25, 75 or 125 mg, or placebo. RESULTS: Of 577 patients randomized, 566 had at least one evaluable heartburn episode and were included in the intention-to-treat analysis. All three ranitidine doses were statistically significantly superior to placebo in providing overall episodic heartburn relief for the first episode (P < 0.002), last episode (P+info)

Effect of histamine H2-receptor antagonist on the phosphorus-binding abilities of calcium carbonate and calcium lactate in hemodialysis patients. (5/694)

The effect of histamine H2-receptor antagonist (famotidine) on the phosphorus-binding abilities of calcium carbonate and calcium lactate were examined in 13 chronic hemodialysis patients. In seven patients receiving calcium carbonate, famotidine (20 mg/d) was given because of gastroduodenal disorders, and calcium carbonate was replaced with calcium lactate as a phosphorus binder after 4 wk of treatment with famotidine. With the 4-wk administration of famotidine accompanied by calcium carbonate, the serum phosphorus level increased from 6.3+/-0.9 to 7.1+/-0.5 mg/dl (P<0.05). However, with the substitution of calcium lactate, the serum phosphorus level decreased significantly when compared to that before substitution (6.3+/-0.2 and 6.0+/-0.9 mg/dl after 4 and 8 wk of substitution, respectively), despite continued administration of famotidine. Serum calcium, creatinine, alkaline phosphatase, high sensitive parathyroid hormone, blood urea nitrogen, arterial blood pH, and bicarbonate were not significantly altered during the trial period. In six control patients treated with calcium carbonate alone, there were no statistical changes in serum calcium and phosphorus levels after substitution of calcium lactate for calcium carbonate. These results suggest that famotidine significantly affects the phosphorus-binding ability of calcium carbonate, but not that of calcium lactate. A careful observation of changes in the serum phosphorus level should be required in hemodialysis patients receiving calcium carbonate and histamine H2-receptor antagonists. Calcium lactate may be useful as a phosphorus binder in such hemodialysis patients.  (+info)

Alcohol-histamine interactions. (6/694)

Alcohol and histamine metabolic pathways in the body have the common enzymes aldehyde dehydrogenase and aldehyde oxidase. The metabolite of ethanol, acetaldehyde, can effectively compete with the metabolites of histamine, methylimidazole acetaldehyde, and imidazole acetaldehyde. At the periphery, alcohol and acetaldehyde liberate histamine from its store in mast cells and depress histamine elimination by inhibiting diamine oxidase, resulting in elevated histamine levels in tissues. Histamine mediates alcohol-induced gastric and intestinal damage and bronchial asthma as well as flushing in Orientals. On the other hand, alcohol provokes food-induced histaminosis and histamine intolerance, which is an epidemiological problem. There are many controversial reports concerning the effect of H2 receptor antagonists on ethanol metabolism and the activity of alcohol dehydrogenase in the stomach. In addition, alcohol affects histamine levels in the brain by modulating histamine synthesis, release, and turnover. Histamine receptor antagonists can affect ethanol metabolism and change the sensitivity of animals to the hypnotic effects of alcohol. In contrast to other neurotransmitters, the involvement of the brain histamine system in the mechanisms of the central actions of alcohol and in the pathogenesis of alcoholism is poorly studied and understood.  (+info)

L-365,260 inhibits in vitro acid secretion by interacting with a PKA pathway. (7/694)

The aim of this study was to analyse the antisecretory mechanism of L-365,260 in vitro in isolated rabbit gastric glands. We showed that compound L-365,260, described as a non-peptide specific competitive CCK-B receptor antagonist, was able to dose-dependently inhibit [14C]-aminopyrine accumulation induced by histamine (10(-4) M), carbachol (5x10(-5) M), 3-isobutyl-1-methyl-xanthine (IBMX) (5x10(-6) M) and forskolin (5x10(-7) M) with similar IC50 values respectively of 1.1+/-0.6x10(-7) M, 1.9+/-1.2x10(-7) M, 4.2+/-2.0x10(-7) M and 4.0+/-2.8x10(-7) M. We showed that L-365,260 acted beyond receptor activation and production of intracellular second messengers and that it had no action on the H+/K+ -ATPase. We found that L-365,260 inhibited cyclic AMP-induced [14C]-aminopyrine accumulation in digitonin-permeabilized rabbit gastric glands, suggesting that this compound acted, at least in part, as an inhibitor of the cyclic AMP-dependent protein kinase (PKA) pathway.  (+info)

Efficacy of omeprazole versus ranitidine for symptomatic treatment of poorly responsive acid reflux disease-a prospective, controlled trial. (8/694)

BACKGROUND: H2-receptor antagonists are widely used in patients with gastro-oesophageal reflux disease (GERD) and are frequently continued when symptoms persist. AIM: To compare the efficacy of omeprazole 20 mg once daily with that of ranitidine 150 mg twice daily in relieving GERD symptoms, in patients who remained symptomatic following a 6-week course of ranitidine therapy. METHODS: Patients with heartburn on at least 4 days/week but who did not have endoscopy to assess oesophageal mucosa could participate. This two-phase, prospective trial included a 6-week open-label phase (phase I), followed by an 8-week double-blind phase (phase II). Patients still symptomatic following treatment with ranitidine 150 mg twice daily (phase I) were randomized to double-blind treatment (phase II) with either omeprazole 20 mg once daily or ranitidine 150 mg twice daily. The primary efficacy variable was the proportion of patients with heartburn resolution during weeks 4 and 8 of phase II. RESULTS: Of the 533 patients with GERD who received ranitidine in phase I, 348 patients (65%) were still symptomatic. A total of 317 patients (59%) were randomized to double-blind treatment (phase II). At week 8, a significantly (P < 0.0004) greater proportion of omeprazole-treated patients (70%) experienced no more than mild heartburn compared with ranitidine-treated patients (49%). Complete resolution of heartburn also occurred in a significantly (P < 0. 00001) greater proportion of omeprazole-treated patients (46% vs. 16% of the ranitidine group at week 8). CONCLUSIONS: After 6 weeks of ranitidine treatment, the majority of patients with GERD were still experiencing moderate to severe heartburn. Omeprazole was significantly more effective than ranitidine in resolving heartburn in this group of patients.  (+info)

Histamine2 H2 - receptor antagonists are widely prescribed for a variety of acid-mediated gastrointestinal disorders. The objective of the present study was to quantify the frequency of inappropriate H2-receptor antagonist use and its economic impact in patients who were admitted to a critical care bed at our hospital and followed as...
Antisecretory effects of two new histamine H2-receptor antagonists.: N-(3-[3-(1-Piperidinylmethyl)phenoxy]propyl)acetoxyaceta mide hydrochloride (Hoe 760) and N
Results showed that PPI use correlated with elevated risk of GC (hazard ratio, 2.44; 95% confidence interval, 1.42 to 4.2), while histamine-2 receptor antagonist use was not associated with increased risk (hazard ratio, 0.72; 95% confidence interval, 0.48 to 1.07).
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TY - JOUR. T1 - Histamine H2-Receptor Antagonist Use Is Associated with Lower Prevalence of Nonalcoholic Fatty Liver Disease A Population-based Study from the National Health and Nutrition Examination Survey, 2001-2006. AU - Shen, Huafeng. AU - Liangpunsakul, Suthat. PY - 2016/8/1. Y1 - 2016/8/1. N2 - Background and Aim: Recent basic mechanistic studies found that proton-pump inhibitors (PPIs) or histamine antagonists inhibited multiple pathways involved in nonalcoholic fatty liver disease (NAFLD) development. The aim of this study was to investigate an association between PPIs or H1/H2-receptor antagonist (H1RA/ H2RA) use and NAFLD prevalence in the general US population. Methods: We conducted a cross-sectional analysis of data from the National Health and Nutrition Examination Survey, 2001-2006. We included 10,398 adults aged 20 to 74 years who had alanine aminotransferase data; of those, 2058 were identified as having NAFLD and 8340 as controls. PPI or H1RA/H2RA use was defined as use of ...
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Proton pump inhibitors (PPI) and histamine 2 receptor antagonists (H2RA) have been widely used as stress ulcer prophylaxis (SUP) in critically ill patients, however, its efficacy and safety remain unclear. This study aimed to assess the effect of SUP on clinical outcomes in critically ill adults. Literature search was conducted in PubMed, EMBASE, Web of Science, and the Cochrane database of clinical trials for randomized controlled trials (RCTs) that investigated SUP, with PPI or H2RA, versus placebo or no prophylaxis in critically ill patients from database inception through 1 June 2019. Study selection, data extraction and quality assessment were performed in duplicate. The primary outcomes were clinically important gastrointestinal (GI) bleeding and overt GI bleeding. Conventional meta-analysis with random-effects model and trial sequential analysis (TSA) were performed. Twenty-nine RCTs were identified, of which four RCTs were judged as low risk of bias. Overall, SUP could reduce the incident of
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Define nizatidine. nizatidine synonyms, nizatidine pronunciation, nizatidine translation, English dictionary definition of nizatidine. n. A histamine receptor antagonist, C12H21N5O2S2, that inhibits the secretion of gastric acid and is used to treat duodenal and gastric ulcers and...
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The involvement of immunological reactivity to ranitidine base R-b and ranitidine hydrochloride R-HCl in the development of occupationally related symptomatology was analyzed in 40 subjects employed in a pharmaceutical plant producing ranitidine and in 33 nonexposed controls, using a specific dose-response lymphocyte proliferative test...
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PreRX=pretreatment; ULN=upper limit of normal. Neutrophils, (absolute), low (10*3 c/uL): ,0.85*PreRx, if PreRx ,1.5; ,1.5 if PreRx ≥1.5. Alanine aminotransferase, high (U/L): ,1.25*PreRx if PreRx ,ULN; ,1.25*ULN if PreRx ≤ULN. Bilirubin, direct (mg/dL), high: ,1.1*ULN if PreRx ≤ULN;, 1.1*ULN if PreRx is missing; ,1.25*PreRx if PreRx ,ULN. Bilirubin, total (mg/dL), high: ,1.1*ULN if PreRx ≤ULN;, 1.1*ULN if PreRx is missing; ,1.25*PreRx if PreRx ,ULN ...
PreRX=pretreatment; ULN=upper limit of normal. Neutrophils, (absolute), low (10*3 c/uL): ,0.85*PreRx, if PreRx ,1.5; ,1.5 if PreRx ≥1.5. Alanine aminotransferase, high (U/L): ,1.25*PreRx if PreRx ,ULN; ,1.25*ULN if PreRx ≤ULN. Bilirubin, direct (mg/dL), high: ,1.1*ULN if PreRx ≤ULN;, 1.1*ULN if PreRx is missing; ,1.25*PreRx if PreRx ,ULN. Bilirubin, total (mg/dL), high: ,1.1*ULN if PreRx ≤ULN;, 1.1*ULN if PreRx is missing; ,1.25*PreRx if PreRx ,ULN ...
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The PEPTIC multi-center RCT compared histamine-2 receptor blockers (H2RBs) versus proton pump inhibitors (PPIs) for stress ulcer prophylaxis among
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Compounds of formula (I) 1 are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the his
Title: MedicineNet cimetidine Specialty, Description: MedicineNet cimetidine Specialty, By: Feedage Forager, ID: 331221, Grade: 93, Type: RSS20
... is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate ... Durant, G. J.; Emmett, J. C.; Ganellin, C. R.; Roe, A. M.; Slater, R. A. (1976). "Potential histamine H2-receptor antagonists. ... ISBN 978-0-19-850346-0. "Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. ... "Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine". Journal of ...
Fedorowicz, Zbys; van Zuuren, Esther J; Hu, Nianfang (2012-03-14). "Histamine H2-receptor antagonists for urticaria". Cochrane ... H2-receptor antagonists are sometimes used in addition to H1-antagonists to treat urticaria, but there is limited evidence for ... Histamine and other proinflammatory substances are released from mast cells in the skin and tissues in response to the binding ... Ingestion of free histamine released by bacterial decay in fish flesh may result in a rapid-onset, allergic-type symptom ...
"Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. American Chemical Society. ... California Discovery of histamine H2-receptor antagonists and the introduction of Tagamet by scientists at Smith Kline and ...
... is an antagonist at the H2 and H3 histamine receptors. It is largely inactive as an H2 antagonist at physiological ... ISBN 978-0-19-850346-0. "Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. ... in their intent to develop a histamine antagonist for the treatment of peptic ulcers. The discovery of burimamide ultimately ...
The mechanism of action of cimetidine as an antacid is as a histamine H2 receptor antagonist. It has been found to bind to the ... the first H2 receptor antagonist. Burimamide, a specific competitive antagonist at the H2 receptor, 100 times more potent than ... Sivelle PC, Underwood AH, Jelly JA (March 1982). "The effects of histamine H2 receptor antagonists on androgen action in vivo ... Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid ...
Force R. W., Nahata M. C. (1992). "Effect of histamine H2-receptor antagonists on vitamin B12 absorption". The Annals of ... Fedorowicz, Z; van Zuuren, EJ; Hu, N (14 March 2012). "Histamine H2-receptor antagonists for urticaria". The Cochrane Database ... Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid ... Ranitidine and other histamine H2 receptor antagonists may increase the risk of pneumonia in hospitalized patients.[26] They ...
... is a histamine antagonist selective for the H2 subtype. It was studied as a treatment for excessive gastric ... Palasciano, G; Maggi, V; Portincasa, P (1990). "The effect of the H2-antagonist niperotidine on intragastric acidity in healthy ...
It is a histamine H2 receptor antagonist. Famotidine was patented in 1979 and came into medical use in 1985. It is available as ... Famotidine, an H2 antagonist, blocks the action of histamine on the parietal cells, ultimately reducing acid secretion into the ... Famotidine, sold under the brand name Pepcid among others, is an histamine H2 receptor antagonist medication that decreases ... April 1985). "Famotidine, a new, potent, long-acting histamine H2-receptor antagonist: comparison with cimetidine and ...
Tsai BS, Yellin TO (1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic antidepressants ... Kanba S, Richelson E (1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain ... It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ... ISBN 0-89603-121-7. Tran VT, Chang RS, Snyder SH (1978). "Histamine H1 receptors identified in mammalian brain membranes with [ ...
Treatment with histamine H2 antagonists in acute upper gastrointestinal hemorrhage. Implications of randomized trials. „N Engl ... Meta-analysis: the efficacy of intravenous H2-receptor antagonists in bleeding peptic ulcer. „Aliment Pharmacol Ther". 16 (6), ...
Subdivisions of histamine antagonists include H1 receptor antagonists, H2 receptor antagonists, and H3 receptor antagonists. ... Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). ... Histaminergic means "working on the histamine system", and histaminic means "related to histamine". A histaminergic agent (or ... drug) is a chemical which functions to directly modulate the histamine system in the body or brain. ...
... is an H2 histamine receptor receptor antagonist. Willson RA, Hall T, Hart J (June 1988). "Oxmetidine (H2 receptor antagonist) ...
"Histamine H2-receptor antagonists for urticaria". Cochrane Database of Systematic Reviews. doi:10.1002/14651858.CD008596.pub2. ... H2-receptor antagonists are sometimes used in addition to H1-antagonists to treat urticaria, but there is limited evidence for ... Leukotriene-receptor antagonistsEdit. Leukotrienes are released from mast cells along with histamine. The medications, ... Dietary histamine poisoningEdit. This is termed scombroid food poisoning. Ingestion of free histamine released by bacterial ...
... is a brain-penetrating selective histamine H2 receptor (HRH2) antagonist developed by Smith, Kline & French, with ... January 1988). "Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist". British ... It is a benzthiazole derivative with a 30-fold higher potency for H2 receptors than other peripheral and central receptors. ...
Treatments proposed include cromolyn sodium and prednisone, as well as histamine (H2) receptor antagonists or proton pump ...
3. 2012). "Histamine H2-receptor antagonists for urticaria.". The Cochrane database of systematic reviews 3: CD008596. PMID ... "Effect of histamine H2-receptor antagonists on vitamin B12 absorption." The Annals of Pharmacotherapy 26.10 (1992): 1283-1286. ... 1994). "Recent treatment with H2-antagonists and antibiotics and gastric surgery as risk factors for Salmonella infection". Br ... "The association between histamine 2 receptor antagonist use and Clostridium difficile infection: a systematic review and meta- ...
... is a histamine H2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment ... Nizatidine proved to be the last new histamine H2 receptor antagonist introduced prior to the advent of proton pump inhibitors ... another popular H2 receptor antagonist Romero M, Franzosi MG (1989). "[Nizatidine]". Medicina (Florence, Italy) (in Italian). 9 ...
Tsai BS, Yellin TO (November 1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic ... The TCAs also have varying but typically high affinity for antagonising the H1 and H2 histamine receptors, as well as the ... through interfering with the reuptake of serotonin and acting as antagonists to SHAM (serotonin, histamine, alpha, muscarinic) ... "Tricyclic antidepressant drugs block histamine H2 receptor in brain". Nature. 269 (5624): 163-5. Bibcode:1977Natur.269..163G. ...
Histamine H2 receptor antagonists like cimetidine and ranitidine may reduce the efficacy of cefalexin by delaying its ...
An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ... They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system ... Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR ...
... exist as inverse agonists and neutral antagonists. They act on H2 histamine receptors found mainly in the parietal cells of the ... histamine acts on H2 to stimulate acid secretion; drugs that inhibit H2 signaling thus reduce the secretion of gastric acid. H2 ... H2-antihistamines bind to histamine H2 receptors in the upper gastrointestinal tract, primarily in the stomach. Antihistamines ... Research into these drugs led to the discovery that they were H1 antagonists and also to the development of H2 antagonists, ...
Proton pump inhibitors (such as omeprazole and lansoprazole) and histamine H2-receptor antagonists (such as famotidine and ...
... (INN) is a second generation histamine H2 receptor antagonist having multimodal mechanism of action and used to ... Like other H2 receptor antagonists, lafutidine acts by preventing the secretion of gastric acid. It also activates calcitonin ...
The Discovery of Histamine H1 and H2 Antagonists". Clinical pharmacology in drug development. 5 (1): 5-12. doi:10.1002/cpdd.236 ... Research into these drugs led to the discovery that they were H1 antagonists and also to the development of H2 antagonists, ... Histamine receptors exhibit constitutive activity, so antihistamines can function as either a neutral receptor antagonist or an ... H2-antihistamines, like H1-antihistamines, occur as inverse agonists and neutral antagonists. They act on H2 histamine ...
Avoiding rapid infusion of protamine sulfate and pre-treating at-risk patients with histamine receptor antagonists (H1 and H2) ...
... is a specific and competitive histamine H2 receptor antagonist drug that is used to treat gastric ulcers, ...
French company during the time when Black was leading the team that developed the histamine receptor antagonists, H2 ... "H2-receptor antagonists". British National Formulary. Retrieved 30 January 2017. CS1 maint: discouraged parameter (link) Paton ... Clark took this much further and extended it to examine the actions of antagonists. The data he gathered on the exact ... Rather than looking at the depression by antagonist of the response to a fixed agonist concentration, he measured the dose- ...
... and omeprazole was quickly shown to be clinically superior to the histamine H2 receptor antagonists, and was launched in 1988 ... sodium with other anti-secretory drugs showed that it was significantly more effective than H2-receptor antagonists and either ... Therefore, a new class of PPIs, potassium-competitive acid blockers (P-CABs) or acid pump antagonists (APAs), have been under ... of histamine, acetylcholine, or other yet to be discovered stimulants. In addition, their mechanism of action involves covalent ...
... when the overwhelming success of the histamine H2 receptor antagonists Tagamet (cimetidine) and Zantac (ranitidine ... the second H2 receptor antagonist, marketed as Zantac by Glaxo. Other pharmaceutical and agrochemical companies gradually ...
H2,66,82)(H2,67,83)(H2,68,85)(H,72,86)(H,73,84)(H,74,89)(H,75,87)(H,76,91)(H,77,92)(H,78,90)(H,79,88)(H4,69,70,71)/t40-,41-,42 ... by drugs known as neurokinin type 1 antagonists (also termed: SP antagonists, or tachykinin antagonists.) One such drug is ... histamine, dopamine, serotonin, and opioids. Their activation stimulates the vomiting reflex. Different emetic pathways exist, ... H2,66,82)(H2,67,83)(H2,68,85)(H,72,86)(H,73,84)(H,74,89)(H,75,87)(H,76,91)(H,77,92)(H,78,90)(H,79,88)(H4,69,70,71)/t40-,41-,42 ...
Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor antagonist)) ... InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3/t9-/m0/s1 ... 組織胺受體激動劑(英語:Histamine agonist) ... 血清素受體拮抗劑(英語:Serotonin antagonist) (5-HT3(英語:5-HT3 antagonist)) ... Cannabinoid receptor antagonist(英語:Cannabinoid receptor antagonist). *Endocannabinoid enhancer
"Purification and molecular cloning of a secreted, Frizzled-related antagonist of Wnt action". Proc. Natl. Acad. Sci. U.S.A. 94 ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
"Tagamet®: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. American Chemical Society. ... prvega zaviralca histaminskega receptorja H2. Burimamid je specifičen kompetitivni antagonist s 100-krat večjo jakostjo od Nα- ... InChI=1S/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14) ... Cimetidin velja za prototipsko učinkovino iz skupine zaviralcev histaminskega receptorja H2, iz katere so kasneje razvili ...
Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z. The histamine H3 receptor antagonist clobenpropit enhances ... InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19) Y. Key ... Klobenpropit je histaminski antagonist H3 receptora.[5] On ima neuroprotektivno dejstvo, koje ostvaruje putem stimulacije ... Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in ...
"Proton pump inhibitors versus histamine 2 receptor antagonists for stress ulcer prophylaxis in critically ill patients: a ... In case of severe hemorrhagic or erosive gastritis and stress ulcers, a combination of antacids and H2-blockers may stop active ... Possible agents include antacids, H2-receptor blockers, sucralfate, and proton pump inhibitors (PPIs). Tentative evidence ... supports that PPIs may be better than H2 blockers. Concerns with the use of stress ulcer prophylaxis agents include increased ...
Agonists and antagonists[edit]. Specific antagonists include istradefylline (KW-6002) and SCH-58261, while specific agonists ... Specific antagonists include MRS1191, MRS1523 and MRE3008F20, while specific agonists include Cl-IB-MECA and MRS3558.[19] ... Adenosine antagonists are widely used in neonatal medicine; A reduction in A1 expression appears to prevent hypoxia-induced ... Xanthine derivatives such as caffeine and theophylline act as non-selective antagonists at A1 and A2A receptors in both heart ...
乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺(英语:Dopamine receptor) (D1, D2, D3, D4, D5) · 组织胺(英语:Histamine receptor) (H1, H2, H3, H4) · 褪黑素( ... GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. British Journal of Pharmacology. January 1994 ...
Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
Force R. W., Nahata M. C. (1992). "Effect of histamine H2-receptor antagonists on vitamin B12 absorption". The Annals of ... Fedorowicz, Z; van Zuuren, EJ; Hu, N (14 March 2012). "Histamine H2-receptor antagonists for urticaria". The Cochrane Database ... Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid ... Ranitidine and other histamine H2 receptor antagonists may increase the risk of pneumonia in hospitalized patients.[27] They ...
... drugs which are selective receptor antagonists of CysLTR1 but not CysLTR2.[20][21][22][23] Models of allergic reactions in ... a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma". Journal of Medicinal Chemistry. 58 (15): 6093-113. doi: ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... and development asthma and that drugs targeting CYSLTR2 may work in a manner that differs from those of CYSLTR1 antagonists.[9] ...
H2,45,57)(H2,46,58)(H2,47,59)(H,48,61)(H,49,66)(H,50,60)(H,51,62)(H,52,65)(H,53,63)(H,54,64)/t22-,25-,26-,27-,28-,29-,30-,31-, ... Maternal behavior: Female rats given oxytocin antagonists after giving birth do not exhibit typical maternal behavior.[59] By ... "Inhibition of post-partum maternal behaviour in the rat by injecting an oxytocin antagonist into the cerebral ventricles". The ... The antidepressant-like effects of oxytocin are not blocked by a selective antagonist of the oxytocin receptor, suggesting that ...
CCL18 has been identified as an endogenous antagonist of the GPER.[16] ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... "In vivo effects of a GPR30 antagonist". Nat. Chem. Biol. 5 (6): 421-7. doi:10.1038/nchembio.168. PMC 2864230. PMID 19430488 ...
Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): ... SB-222,200 - potent and selective antagonist, Ki = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, ... Advenier C, Lagente V, Boichot E (Aug 1997). "The role of tachykinin receptor antagonists in the prevention of bronchial ... NK3 receptor antagonists are being investigated as treatments for various indications.[7] ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ... Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, ...
Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
H2-receptor antagonists and prokinetics for gastro-oesophageal reflux disease-like symptoms and endoscopy negative reflux ... "Proton pump inhibitors versus histamine 2 receptor antagonists for stress ulcer prophylaxis in critically ill patients: a ... of magnesium can be found in people on PPI therapy and these can be reversed when they are switched to H2-receptor antagonist ... results in a class of drugs that are significantly more effective than H2 antagonists and reduce gastric acid secretion by up ...
... β1 antagonist): 6.09 μM; ICI-118,551 (β2 antagonist): 3.58 μM; SR-5923A (β3 antagonist): 17 μM.[73] ... Furthermore, the marked brocho-constriction produced by injections of histamine was not reversed by either l-synephrine or d,l- ... InChI=1S/C9H13NO2/c1-10-6-9(12)7-2-4-8(11)5-3-7/h2-5,9-12H,6H2,1H3 Y ... a standard α1 antagonist) and ketanserin,[o] with prazosin being the more potent antagonist (pA2 = 9.38, vs pA2 = 8.23 for ...
response to histamine. • behavioral fear response. • dopamine receptor signaling pathway. • G-protein coupled receptor ... Apomorphine - D4 selective but also D2 and D3 agonist, α-adrenergic and serotonergic weak antagonist ... Lanig H, Utz W, Gmeiner P (April 2001). "Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[ ... an antagonist with high affinity and selectivity for the human dopamine D4 receptor". Journal of Medicinal Chemistry. 39 (10): ...
Category:Dopamine antagonists. References[edit]. *^ Girault JA, Greengard P (2004). "The neurobiology of dopamine signaling". ... antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine ... unless blocked by a receptor antagonist or a synthetic partial agonist.[8] ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
Ramatroban, vidupiprant, and Bay U3405 are non-selective (i.e. known to influence other receptors) antagonists of DP2.[9] ... PDP2 receptor antagonists have been shown to allergic reactions induced in the airways mice and sheep as well as the airways ... The following compounds are selective receptor antagonists of and thereby inhibit the activation of DP2: fevipiprant, ... Setipiprant (ACT-129968), a selective, orally active antagonist of the (DP2) receptor, proved to be well-tolerated and ...
InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3 Y. Key: ... Ciproheptadin deluje kao antagonist (ili inverzni agonist u zavisnosti od aktivnog mesta) na sledećim receptorima: *H1 (~0,05 ... "Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the ... 1997). "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology 36 (4-5): 621-9. PMID ...
H2) পাকস্থলীর পাচক অ্যাসিড নিঃসব্রণ নিয়ন্ত্রণ করে।[২] ... Histamine. *HTMT. *UR-AK49. *Antagonists: First-generation: 4-Methyldiphenhydramine. *Alimemazine. *Antazoline. *Azatadine ...
Lapa GB, Mathews TA, Harp J, Budygin EA, Jones SR: Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant ... InChI=1S/C19H23NO/c1-20-14-12-18(13-15-20)21-19(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18-19H,12-15H2,1H3. Key: OWQUZNMMYNAXSL ...
... was first isolated by German physician Albrecht Kossel and Sven Hedin in 1896.[4] It is also a precursor to histamine ... InChI=1S/C6H9N3O2/c7-5(6(10)11)1-4-2-8-3-9-4/h2-3,5H,1,7H2,(H,8,9)(H,10,11)/t5-/m0/s1 Y ... The histidine amino acid is a precursor for histamine, an amine produced in the body necessary for inflammation.[22] ... InChI=1S/C6H9N3O2/c7-5(6(10)11)1-4-2-8-3-9-4/h2-3,5H,1,7H2,(H,8,9)(H,10,11)/t5-/m0/s1 ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... InChI=1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9- ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ...
Haematological adverse effects of histamine H2-receptor antagonists.. Aymard JP1, Aymard B, Netter P, Bannwarth B, Trechot P, ... Histamine H2-receptor antagonists are widely used in the treatment of gastrointestinal diseases related to gastric acid ... This is of no clinical importance in short term treatment, but long term use of H2-receptor antagonists may theoretically ... appear to be of particular clinical importance in cases of impaired renal elimination of H2-receptor antagonists. Cimetidine ...
Histamine H2-receptor antagonists are widely used in the treatment of gastrointestinal diseases related to gastric acid ... The effects of histamine H2-receptor antagonists on PHA induced lymphocyte proliferation. Agents and Actions 15: 242-248, 1984 ... Histamine H2-receptor antagonists are widely used in the treatment of gastrointestinal diseases related to gastric acid ... Histamine H2-antagonist drug interactions in perspective: mechanistic concepts and clinical implications. American Journal of ...
SEARCH RESULTS for: Histamine H2 Receptor Antagonists [Drug Class] (640 results) * Share : JavaScript needed for Sharing tools ...
2 Abstracts with Histamine H2 Antagonists Research. Filter by Study Type. In Vitro Study. ... Histamine H2 Antagonists is a Sub of the following Topic. *Acid Blockers ... Curcumin protects against gastric ulcers by blocking H2 histamine receptors.Dec 01, 2005. ...
Histamine H2-Receptor Antagonists. Class Summary. These agents are usually given in addition to H1 blockers. ... Ranitidine is an H2 antagonist that, when combined with the H1 type, may be useful in treating allergic reactions that do not ... The H2-receptor antagonist ranitidine and others may aid in treatment when an H1 blocker is not effective on its own. ... This agent inhibits histamine at H2 receptors of gastric parietal cells, which results in reduced gastric acid secretion, ...
Histamine H2 Antagonists. Class Summary. Like antacids, these agents do not reduce the frequency of reflux but do decrease the ... Nizatidine competitively inhibits histamine at the H2 receptor of the gastric parietal cells, resulting in reductions in ... Cimetidine inhibits histamine at the H2 receptors of gastric parietal cells, causing reductions in gastric acid secretion, ... Ranitidine inhibits histamine stimulation of the H2 receptor in gastric parietal cells, reducing gastric acid secretion, ...
1 Abstracts with Histamine H2-Receptor Antagonist Alternatives Research. Filter by Study Type. Animal Study. ... 2 Pharmacological Actions Researched for Histamine H2-Receptor Antagonist Alternatives Name. AC. CK. Focus. ... Additional Keywords : Drug: Ranitidine, Histamine H2-Receptor Antagonist Alternatives, Natural Substances Versus Drugs, Plant ... 4 Diseases Researched for Histamine H2-Receptor Antagonist Alternatives Name. AC. CK. Focus. ...
Histamine, histamine H2-receptor antagonists, gastric acid secretion and ulcers: an overview.. Pattichis K1, Louca LL. ... Histamine actions are mediated by more than one type of receptor. The discovery, development and mode of action of H2- ... Histamine, a biogenic amine, is involved in allergic reactions and asthma. The involvement of histamine in peptide ulcers is ... of the four currently used H2-antagonists (cimetidine, ranitidine, nizatidine and famotidine) is given. Furthermore, due to ...
Detailed drug Information for histamine h2 antagonist Oral, Injection, Intravenous. Includes common brand names, drug ... Histamine h2 antagonist. Class Name: histamine h2 antagonist (Oral route, Injection route, Intravenous route) ... Histamine H2-receptor antagonists, also known as H2-blockers, are used to treat duodenal ulcers and prevent their return. They ... Drinking alcoholic beverages while taking an H2-receptor antagonist has been reported to increase the blood levels of alcohol. ...
Zantac is a histamine H2-receptor antagonist -.... Zantac is a histamine H2-receptor antagonist - onlinegenericpills. by Martin ... Ranitidine is known as an H2 histamine blocker. It acts by reducing the quantity of acid in the stomach. This helps to cure and ... Before taking ranitidine, tell your doctor or pharmacist if you are allergic to it; or to other H2 histamine blockers (e.g., ...
Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs.. T M ... Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs.. T M ... Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs.. T M ... Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. ...
Metformin With Either Histamine H2-Receptor Antagonists or Proton Pump Inhibitors: A Polypharmacy Recipe for Neuropathy via ... Metformin With Either Histamine H2-Receptor Antagonists or Proton Pump Inhibitors: A Polypharmacy Recipe for Neuropathy via ... Metformin With Either Histamine H2-Receptor Antagonists or Proton Pump Inhibitors: A Polypharmacy Recipe for Neuropathy via ... Metformin With Either Histamine H2-Receptor Antagonists or Proton Pump Inhibitors: A Polypharmacy Recipe for Neuropathy via ...
Effect of histamine H2-receptor antagonists on vitamin B12 absorption. Ann Pharmacother 1992;26:1283-1286. ... Histamine H2 Receptor Antagonist/Proton Pump Inhibitor-Induced Vitamin B12 Depletion. In general, acid suppressors including ... Metformin With Either Histamine H2-Receptor Antagonists or Proton Pump Inhibitors: A Polypharmacy Recipe for Neuropathy via ... Haematological adverse effects of histamine H2-receptor antagonists. Med Toxicol Adverse Drug Exp 1988;3:430-448. ...
Effects of H2-Receptor Antagonists Cimetidine, Ranitidine, and ICI 125,211 on Histamine-Stimulated Adenylate Cyclase Activity ... Effects of H2-Receptor Antagonists Cimetidine, Ranitidine, and ICI 125,211 on Histamine-Stimulated Adenylate Cyclase Activity ... Effects of H2-Receptor Antagonists Cimetidine, Ranitidine, and ICI 125,211 on Histamine-Stimulated Adenylate Cyclase Activity ... Effects of H2-Receptor Antagonists Cimetidine, Ranitidine, and ICI 125,211 on Histamine-Stimulated Adenylate Cyclase Activity ...
Histamine h2 antagonists. QualityTools. Over-the-Counter Medicine Interaction Cabinet 12/17/07 This interactive tool informs ...
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In conclusion radio protective effects of Histamine H2 receptor antagonists Famotidine and Ranitidine was observed on exposure ... Histamine H2 receptor antagonist are used in the clinical treatment of peptic ulcer. ,i,In vitro,/i, metaphase analysis and ... Histamine H2 receptor antagonist are used in the clinical treatment of peptic ulcer. In vitro metaphase analysis and ... Structural characteristics of histamine H2 receptor antagonists that scavenge hypochlorous acid. Eur. J. Pharm. 1994, vol. 268 ...
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  • Cimetidine inhibits histamine at the H2 receptors of gastric parietal cells, causing reductions in gastric acid secretion, gastric volume, and hydrogen ion concentrations. (medscape.com)
  • A brief comparison of the clinical profiles (dosage regimen, metabolism and drug interactions) of the four currently used H2-antagonists (cimetidine, ranitidine, nizatidine and famotidine) is given. (nih.gov)
  • It was 17.8 times as active as cimetidine on histamine (10(-5) M)-induced secretion from the isolated gastric mucosa of the bullfrog. (aspetjournals.org)
  • Against acid secretion from the vagally innervated gastric fistula and Heidenhain pouch of dogs stimulated with submaximal doses of histamine, methacholine and gastrin, nizatidine was, respectively, 6.5, 5 and 4.7 times as active as cimetidine by i.v. administration. (aspetjournals.org)
  • Nizatidine was very well absorbed from the gut and was 5 to 10 times as active as cimetidine on gastric acid secretion of dogs induced by submaximal and maximal doses of histamine when given p.o. (aspetjournals.org)
  • Pharmacological blockade of H2 receptors by cimetidine (100 μmoles/kg) and methiamide (410 μmoles/kg) largely prevented the formation of experimental ulcers and the decrease in the pepsinogen level. (springer.com)
  • Histamine H 2 receptor antagonists (e.g., cimetidine, ranitidine, famotidine, nizatidine) inhibit gastric acid secretion by antagonizing the histamine H 2 receptor on gastric parietal cells. (vin.com)
  • a) Cimetidine, the first H2-receptor antagonist approved for clinical use, reduces gastric acid secretion by about 50% (at a total daily dosage of 1000mg). (pharmainfo.net)
  • Nature, 1972, 236, 385) and the action of histamine at this receptor is blocked by drugs such as cimetidine. (patentgenius.com)
  • Cimetidine (Tagamet): An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. (wikipedia.org)
  • The H2-receptor antagonist ranitidine and others may aid in treatment when an H1 blocker is not effective on its own. (medscape.com)
  • Ranitidine is an H2 antagonist that, when combined with the H1 type, may be useful in treating allergic reactions that do not respond to H1 antagonists alone. (medscape.com)
  • Ranitidine inhibits histamine stimulation of the H2 receptor in gastric parietal cells, reducing gastric acid secretion, gastric volume, and hydrogen ion concentrations. (medscape.com)
  • Ranitidine is known as an H2 histamine blocker. (apsense.com)
  • In conclusion radio protective effects of Histamine H2 receptor antagonists Famotidine and Ranitidine was observed on exposure togamma-ray. (sciencepublishinggroup.com)
  • Ranitidine belongs to a class of drugs known as H2 blockers. (rxlist.com)
  • [1] Ranitidine is an H 2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach. (wikipedia.org)
  • Histamine H2 receptor antagonists (such as Ranitidine) block the production of stomach acid. (google.com)
  • While limited data exists in humans on the safety of histamine-type II (H-2) receptor antagonists, ranitidine (Zantac®) is the only H-2 antagonist, which has been studied specifically during pregnancy. (health.am)
  • Famotidine competitively inhibits histamine at the H2 receptors in gastric parietal cells, reducing gastric acid secretion, gastric volume, and hydrogen concentrations. (medscape.com)
  • Famotidine, a competitive histamine H 2 -receptor antagonist, is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. (pharmacycode.com)
  • Famotidine is a histamine H2-receptor antagonist or H2-blocker. (mayoclinic.org)
  • As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli. (cancer.gov)
  • Histamine-2 receptor antagonists (HRA), such as famotidine, are used clinically with little. (bioportfolio.com)
  • c) Famotidine is the most patent H2-receptor antagonist. (pharmainfo.net)
  • This agent competitively inhibits histamine at the H2 receptor of the gastric parietal cells, resulting in reduced gastric acid secretion, gastric volume, and reduced hydrogen concentrations. (medscape.com)
  • Because solar urticaria involves IgE-mediated mast cell degranulation with consequent histamine release, the first line of treatment for this disease consists of long-acting, nonsedating H1-receptor blockers. (medscape.com)
  • Histamine H2-receptor antagonists, also known as H2-blockers, are used to treat duodenal ulcers and prevent their return. (drugs.com)
  • H2-blockers may also be used for other conditions as determined by your doctor. (drugs.com)
  • H2-blockers work by decreasing the amount of acid produced by the stomach. (drugs.com)
  • H2-blockers are available both over-the-counter (OTC) and with your doctor's prescription. (drugs.com)
  • Confusion and dizziness may be especially likely to occur in elderly patients, who are usually more sensitive than younger adults to the effects of H2-blockers. (drugs.com)
  • H2-blockers have not been studied in pregnant women. (drugs.com)
  • Make sure your doctor knows if you are pregnant or if you may become pregnant before taking H2-blockers. (drugs.com)
  • It includes sixteen case studies of major pharmaceutical developments in the twentieth century, encompassing, amongst others, beta-blockers, beta-stimulants, inhaled steroids and histamine H2-antagonists. (elgaronline.com)
  • Many of these drugs can interact with other medicines and cause symptoms that may be more serious than those of H2 blockers alone. (medlineplus.gov)
  • H2 blockers are medicines that work by reducing the amount of stomach acid secreted by glands in the lining of your stomach. (medlineplus.gov)
  • There are different names and brands of H2 blockers. (medlineplus.gov)
  • H2 blockers are most often taken by mouth. (medlineplus.gov)
  • H2 blockers may be bought in lower doses at the store without a prescription. (medlineplus.gov)
  • If you have a peptic ulcer, your provider may prescribe H2 blockers along with 2 or 3 other medicines for up to 2 weeks. (medlineplus.gov)
  • Side effects from H2 blockers are rare. (medlineplus.gov)
  • H2 blockers may change the way certain drugs work. (medlineplus.gov)
  • Proton pomp inhibitors, H2 receptor blockers and anti-acids are common drugs for treating dyspepsia in emergency department. (clinicaltrials.gov)
  • Patients used anti-acid, H2 receptor blockers and proton pomp inhibitors in the last one hour. (clinicaltrials.gov)
  • Allergy to H2 receptor blockers and proton pomp inhibitors. (clinicaltrials.gov)
  • ASM = Acid Suppressant Medication, ie H2 blockers and PPIs. (google.com)
  • Please note, histamine blockers or H2 antagonists ex. (rqhealth.ca)
  • Malabsorption of dietary iron and cobalamin appears to result from inhibition of gastric secretion by the H2-receptor antagonists. (nih.gov)
  • Histamine, histamine H2-receptor antagonists, gastric acid secretion and ulcers: an overview. (nih.gov)
  • Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. (aspetjournals.org)
  • Nizatidine (LY139037), a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion. (aspetjournals.org)
  • K i = 4.57 x 10 -7 M). These results are consistent with the reported pharmacological potencies of the antagonists on guinea pig right atrium and on gastric acid secretion in vivo . (aspetjournals.org)
  • Agonist activities are reported for stimulation of histamine H1 (guinea-pig ileum) and H2 (rat gastric acid secretion) receptors. (meta.org)
  • Cholinergic antagonists inhibit acid secretion by antagonizing the muscarinic cholinergic receptor on gastric parietal cells. (vin.com)
  • Pirenzepine and telenzepine, selective M 1 cholinergic antagonists, inhibit cholinergically mediated gastric acid secretion without significant effects on other muscarinic receptors (M 2 , M 3 ) that mediate GI, airway, and urinary bladder smooth muscle contraction. (vin.com)
  • The invention relates to oxadiazole derivatives which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture and to pharmaceutical compositions containing them. (patentgenius.com)
  • This invention relates to oxadiazole derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. (patentgenius.com)
  • Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells. (pharmacycode.com)
  • By inhibiting the action of histamine on stomach cells, nizatidine reduces stomach acid production. (pharmacycode.com)
  • Effective pharmacological treatments for GERD include antacids, alginate, histamine H2 receptor antagonists, and proton pump inhibitors. (doaj.org)
  • Difference between Histamine h2 antagonists and antacids, difference between Salicylates and nonsteroidal antiinflammatories. (allnurses.com)
  • Previous studies have reported inconsistent findings regarding the association between the use of acid-suppressive drugs such as proton pump inhibitors (PPIs) and histamine 2 receptor antagonists (H(2)RAs) and fracture risk. (nih.gov)
  • Recent studies have suggested an increased risk of fractures with proton pump inhibitors (PPIs) and histamine-2 receptor antagonists (H2RAs). (nih.gov)
  • Effect of a proton pump inhibitor or an H2-receptor antagonist on prevention of bleeding from ulcer after endoscopic submucosal dissection of early gastric cancer: a prospective randomized controlled trial. (biomedsearch.com)
  • OBJECTIVES: With conventional methods of endoscopic mucosal resection for early gastric cancer (EGC), proton pump inhibitors (PPIs) and H2-receptor antagonists (H2RAs) have a similar effect on preventing bleeding from artificial ulcers. (biomedsearch.com)
  • Background and Aim: Recent basic mechanistic studies found that proton-pump inhibitors (PPIs) or histamine antagonists inhibited multiple pathways involved in nonalcoholic fatty liver disease (NAFLD) development. (elsevier.com)
  • Gastric acid suppressing drugs (that is, histamine 2 receptor antagonists and proton pump inhibitors) could affect the risk of oesophageal or gastric adenocarcinoma but few studies are available. (bmj.com)
  • Nonsteroidal androgen synthesis inhibitors like ketoconazole can also be described as "NSAAs", although the term is usually reserved to describe AR antagonists. (wikipedia.org)
  • H 2 -receptor antagonists are considered the drugs of choice for children because pediatric doses are well established and the medications are available in liquid form. (medscape.com)
  • Finally, if combination therapy is to be considered, in vitro studies of sucralfate activation and histamine H 2 receptor antagonist absorption suggest that the two drugs should be administered independently. (vin.com)
  • 1966, 27, 427) and the action of histamine at this receptor is blocked (antagnoised) by classical "antihistamine" drugs such as mepyramine. (patentgenius.com)
  • The aim of this study was to investigate an association between PPIs or H1/H2-receptor antagonist (H1RA/ H2RA) use and NAFLD prevalence in the general US population. (elsevier.com)
  • Haematological adverse effects of histamine H2-receptor antagonists. (nih.gov)
  • Ghorbani M. and Mozdarani H. In vitro radioprotective effects of histamine H2 receptor antagonists against gamma-rays induced chromosomal aberrations in human lymphocytes Iran. (sciencepublishinggroup.com)
  • Curcumin protects against gastric ulcers by blocking H2 histamine receptors. (greenmedinfo.com)
  • The involvement of histamine in peptide ulcers is reviewed here. (nih.gov)
  • H2 Antagonists are used in the treatment of stomach ulcers and heart burn. (familydoctor.co.nz)
  • H2- Antagonists are used for the treatment of stomach and duodenal ulcers, heartburn, and other related conditions which are a result of excess stomach acid production. (familydoctor.co.nz)
  • These medicines work by controlling the production of stomach acid via H2- receptor blockade, where they still allow the stomach to produce the amount of acid for digestion, but extra acid build-up that can cause problems (e.g. ulcers) does not occur. (familydoctor.co.nz)
  • Desloratadine is a long-acting tricyclic histamine antagonist selective for H1 receptors. (medscape.com)
  • They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). (wikipedia.org)
  • In this preparation, antidepressants are very potent antagonists of histamine H 1 receptors but are weak antagonists of histamine H 2 receptors. (elsevier.com)
  • In this preparation, antidepressants are very potent antagonists of histamine H1 receptors but are weak antagonists of histamine H2 receptors. (elsevier.com)
  • Combination therapy (sucralfate + histamine H 2 antagonist, or sucralfate + H + , K + - ATPase inhibitor) is frequently employed, but there is still no good evidence that combination therapy is better than component therapy in companion animal medicine. (vin.com)
  • MECHANISM OF ACTION : Histamine receptor H2 modulator. (lens.org)
  • The results indicate that endogenous histamine participates in the mechanism of formation of dystrophic gastric lesions. (springer.com)
  • Mechanisms (a) and (c) appear to be of particular clinical importance in cases of impaired renal elimination of H2-receptor antagonists. (nih.gov)
  • This is of no clinical importance in short term treatment, but long term use of H2-receptor antagonists may theoretically contribute to the occurrence of iron or cobalamin deficiency anaemia. (nih.gov)
  • Clinical review of histamine H2 receptor antagonists. (sciencepublishinggroup.com)
  • Shen, H & Liangpunsakul, S 2016, ' Histamine H2-Receptor Antagonist Use Is Associated with Lower Prevalence of Nonalcoholic Fatty Liver Disease A Population-based Study from the National Health and Nutrition Examination Survey, 2001-2006 ', Journal of Clinical Gastroenterology , vol. 50, no. 7, pp. 596-601. (elsevier.com)
  • H2 blocker / H2RA = Histamine H2 Receptor Antagonist. (google.com)
  • H2-Receptor agonist activities indicate that a methyl group is more readily accommodated at the 4 and Nalpha positions than elsewhere in the histamine molecule and that receptor binding is substantially retained with a methyl substituent in these positions. (meta.org)
  • Also antagonizes the activity of Histamine, a H 1 agonist. (hellobio.com)
  • The CellAura fluorescent H 2 antagonist [aminopotentidine] ligand was shown to antagonize the activity of the agonist, histamine, in a recombinant CHO cell line expressing the human H 2 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene, and in a similar cell line expressing the human H 3 receptor. (hellobio.com)
  • Addition of CellAura fluorescent H 2 antagonist [aminopotentidine] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent H 2 antagonist [aminopotentidine] has no intrinsic agonist activity. (hellobio.com)
  • To determine the apparent KD for CellAura fluorescent H 2 antagonist [aminopotentidine] at histamine H 2 and H 3 receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1µM CellAura fluorescent H 2 antagonist [aminopotentidine], and the cyclic AMP-induced expression of SPAP measured. (hellobio.com)
  • The apparent KD at H 2 and H 3 was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent H 2 antagonist [aminopotentidine], compared to the response curve for the agonist alone. (hellobio.com)
  • Kanba, S & Richelson, E 1983, ' Antidepressants are weak competitive antagonists of histamine H 2 receptors in dissociated brain tissue ', European Journal of Pharmacology , vol. 94, no. 3-4, pp. 313-318. (elsevier.com)
  • H2 receptor antagonists are medicines that help decrease stomach acid. (medlineplus.gov)
  • The item Histamine and H2 antagonists in inflammation and immunodeficiency, edited by Ross E. Rocklin represents a specific, individual, material embodiment of a distinct intellectual or artistic creation found in University of Missouri Libraries . (missouri.edu)
  • The latter result is contrary to data derived by others using homogenates of the guinea pig hippocampus and seems to dispel the idea that antidepressants derive their efficacy by blocking histamine H 2 receptors in brain. (elsevier.com)
  • Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR variants in prostate cancer, little or no inhibition or induction of cytochrome P450 enzymes, and little or no central nervous system distribution. (wikipedia.org)
  • Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system distribution, and no induction of seizures in animals. (wikipedia.org)
  • Guinea pig hippocampus dissociated by mechanical means into uniform clumps of cells (∼ 100 μm in diameter) contains histamine receptors (H 1 and H 2 ) which mediate the formation of cyclic AMP. (elsevier.com)
  • Metiamide is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. (wikipedia.org)
  • Histamine H2-receptor antagonists are widely used in the treatment of gastrointestinal diseases related to gastric acid hypersecretion. (nih.gov)
  • Cetirizine forms a complex with histamine for H1-receptor sites in the blood vessels, gastrointestinal (GI) tract, and respiratory tract. (medscape.com)
  • H2 receptor antagonist medicines are available over-the-counter and by prescription. (medlineplus.gov)
  • Other medicines may also contain H2 receptor antagonists. (medlineplus.gov)
  • Whether the trigger is allergic or not, a complex release of inflammatory mediators, including histamine from cutaneous mast cells, results in fluid leakage from superficial blood vessels. (wikipedia.org)

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