Interleukin 1 Receptor Antagonist Protein: 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.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Histamine H2 Antagonists: 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.Rats, Sprague-Dawley: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Piperidines: A family of hexahydropyridines.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Dopamine Antagonists: 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.Interleukin-1beta: An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.Serotonin 5-HT2 Receptor Antagonists: 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.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Hormone Antagonists: 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.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Histamine H1 Antagonists: 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.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Muscarinic Antagonists: 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.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Sialoglycoproteins: Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Histamine Antagonists: 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.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Receptors, Serotonin: 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.Receptors, N-Methyl-D-Aspartate: 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.Serotonin 5-HT1 Receptor Antagonists: 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.Dizocilpine Maleate: 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.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.beta 2-Microglobulin: An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.Biphenyl CompoundsCells, Cultured: 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.Receptors, Interleukin-1: Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.Nicotinic Antagonists: 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.TetrazolesBenzazepines: Compounds with BENZENE fused to AZEPINES.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Interleukin-1: A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.Xanthines: Purine bases found in body tissues and fluids and in some plants.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Guinea Pigs: 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.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Peptides, Cyclic: Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Indoles: 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.Sulfonamides: A group of compounds that contain the structure SO2NH2.Pyrazoles: 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.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Receptors, Bradykinin: Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.RNA, Messenger: 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.Substance P: 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.Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Receptors, Neurokinin-1: A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.Cimetidine: 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.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.Binding, Competitive: 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.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Serotonin: 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.Integrin beta3: An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.Receptors, Cholecystokinin: Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.Neurons: 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.Signal Transduction: 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.PyrrolidinesBehavior, Animal: The observable response an animal makes to any situation.QuinoxalinesReceptors, Vasopressin: Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.PiperazinesReceptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Receptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Disease Models, Animal: 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.Bradykinin: 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.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Famotidine: A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Injections, Intraventricular: Injections into the cerebral ventricles.Adenosine: 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.Receptors, Neurokinin-2: A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.Adrenergic alpha-Antagonists: 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.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Oligopeptides: Peptides composed of between two and twelve amino acids.Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.QuinuclidinesHistamine: 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.BenzodiazepinonesCell Line: Established cell cultures that have the potential to propagate indefinitely.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Mice, Inbred C57BLAdrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.Angiotensin II: An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.Receptors, Histamine H3: 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)Calcium: 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.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.QuinolinesReceptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptor, Bradykinin B2: A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.Pyrilamine: 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.PhenylpropionatesEndothelins: 21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.Imidazoles: 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).Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Synaptic Transmission: The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Receptors, Corticotropin-Releasing Hormone: Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.Receptors, Calcitonin Gene-Related Peptide: Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Receptor, Angiotensin, Type 1: An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.Antihypertensive Agents: Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.Receptors, Tachykinin: Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Muscle Contraction: 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.Receptors, Angiotensin: Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Memantine: AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.Proglumide: A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Brain: 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.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Kinetics: The rate dynamics in chemical or physical systems.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.CHO Cells: 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.Dioxanes: 1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)Receptors, Neurotransmitter: Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.Ligands: 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)Muscle, Smooth: 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)Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.Mice, Knockout: 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.Receptors, Serotonin, 5-HT3: A subclass of serotonin receptors that form cation channels and mediate signal transduction by depolarizing the cell membrane. The cation channels are formed from 5 receptor subunits. When stimulated the receptors allow the selective passage of SODIUM; POTASSIUM; and CALCIUM.Tachykinins: A family of biologically active peptides sharing a common conserved C-terminal sequence, -Phe-X-Gly-Leu-Met-NH2, where X is either an aromatic or a branched aliphatic amino acid. Members of this family have been found in mammals, amphibians, and mollusks. Tachykinins have diverse pharmacological actions in the central nervous system and the cardiovascular, genitourinary, respiratory, and gastrointestinal systems, as well as in glandular tissues. This diversity of activity is due to the existence of three or more subtypes of tachykinin receptors.Neurokinin A: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ B with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the BRONCHI.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.Rabbits: 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.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Morphine: The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Receptor, Angiotensin, Type 2: An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.Receptors, Histamine H2: 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)Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Receptors, Neuropeptide Y: Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.Receptors, GABA-A: Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)MorpholinesCyclic AMP: 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.Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).TriazolesBornanes8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Norepinephrine: 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.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.Integrin alpha5beta1: An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.Histamine Agonists: 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.Receptor, Bradykinin B1: A subtype of BRADYKININ RECEPTOR that is induced in response to INFLAMMATION. It may play a role in chronic inflammation and has a high specificity for KININS lacking the C-terminal ARGININE such as des-Arg(10)-kallidin and des-Arg(9)-bradykinin. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.Prostaglandin Antagonists: Compounds that inhibit the action of prostaglandins.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.

*Falintolol

... is a beta-adrenergic receptor antagonist. Conti, P; Dallanoce, C; De Amici, M; De Micheli, C; Klotz, KN (1998). " ... "Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor ... antagonists". Bioorganic & Medicinal Chemistry. 6 (4): 401-8. doi:10.1016/s0968-0896(97)10051-7. PMID 9597184. ...

*Flestolol

... is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... 1. Novel .beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/ ...

*Beta-3 adrenergic antagonist

... is an adrenergic antagonist which blocks the Beta-3 adrenergic receptors of cells, with either high specificity (an antagonist ... "Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... SR 59230A Carvedilol Betablocker Beta-3 adrenergic receptor Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, ... A Beta-3 adrenergic antagonist (β3-adrenoceptor antagonist) ... an antagonist for β3 and for β1 or β2 adrenoceptors) like the ...

*Beta-3 adrenergic receptor

"Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta Blocker GRCh38: Ensembl release 89: ...

*Beta-2 adrenergic antagonist

... β2-adrenoceptor antagonist) is an adrenergic antagonist which blocks the beta-2 adrenergic receptors of cells, with either high ... ICI-118,551 Butaxamine Propranolol Betablocker Beta-2 adrenergic receptor Beta2-adrenergic agonist Bilski, AJ; Halliday, SE; ... an antagonist for β2 and for β1 or β3 adrenoceptors) like the non-selective betablocker Propranolol. ... Fitzgerald, JD; Wale, JL (1983). "The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)". J Cardiovasc ...

*Three-finger toxin

... causes decreased heart rate and are thought to function as beta blockers, antagonists for the beta-1 and beta-2 adrenergic ... of Three-Finger Fold Toxins Creates Ligands with Original Pharmacological Profiles for Muscarinic and Adrenergic Receptors". ... a family of G-protein-coupled receptors. Muscarinic toxins can be either receptor agonists or receptor antagonists, and in some ... Novel Antagonists of Nicotinic Acetylcholine Receptors from Snake Venom". ACS Chemical Biology. 10 (12): 2805-2815. doi:10.1021 ...

*Alpha-2A adrenergic receptor

... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ... ADRA2A adrenergic, alpha-2A-, receptor". "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union ...

*Tiprenolol

... is a beta adrenergic receptor antagonist. Allen, JD; Shanks, RG (1974). "Effects of tiprenolol, practolol and ... 51 (2): 179-85. doi:10.1111/j.1476-5381.1974.tb09645.x. PMC 1776753 . PMID 4155971. ...

*Primary polydipsia

... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ... 157 (2): 569-593. doi:10.1111/j.1749-6632.1969.tb12908.x. ISSN 1749-6632. Siegler EL, Tamres D, Berlin JA, Allen-Taylor L, ...

*Tolamolol

... is a beta adrenergic receptor antagonist. Curtis-Prior, PB; Gadd, AL (1990). "Beta-adrenoceptor antagonists and human ... 42 (3): 220-2. doi:10.1111/j.2042-7158.1990.tb05395.x. PMID 1974626. ...

*Glaucoma medication

... a beta-adrenergic receptor antagonist Glaucoma Basic and clinical science course (2011-2012). Glaucoma. American Academy of ... Adrenergic antagonists (nonselective and selective Beta1-antagonists) Alpha 2 agonists Hyperosmotic agents Fotil is a ...

*Sulfinalol

... is a beta adrenergic receptor antagonist. The methyl group on a sulfoxide is sufficiently acidic to substitute for ... "Studies on the mechanism of the acute antihypertensive and vasodilator actions of several beta-adrenoceptor antagonists". J. ... Bromination followed by condensation with 4-(4-methoxyphenyl)butan-2-amine (not PMA) gives the aminoketone 3. Successive ...

*Adrenergic receptor

"Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Molecular ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ... ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ...

*Dopexamine

Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ... It is not an α-adrenergic agonist, does not cause vasoconstriction, and is not a pressor agent. As of 2004 there was some ... Dopexamine stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ...

*Tienoxolol

... is a beta adrenergic receptor antagonist. Mahé, N; Do, B; Nicolaï, B; Rietveld, IB; Barrio, M; Tamarit, JL; Céolin, ...

*Toliprolol

... is a beta adrenergic receptor antagonist. Stephenson, KA; Wilson, AA; Meyer, JH; Houle, S; Vasdev, N (2008). "Facile ... Synthesis, radiolabeling, and ex vivo biodistribution of 18F-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ...

*List of veterinary drugs

... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists benazepril ... clavulanic acid - Adjunct to penicillin-derived antibiotics used to overcome resistance in bacteria that secrete beta-lactamase ... Crosses blood-brain barrier, useful in treatment of meningitis cimetidine - H2 antagonist used to reduce GI acid production ... Ineffective against species that produce beta-lactamase. apomorphine - emetic (used to induce vomiting) artificial tears - ...

*Chlorprothixene

Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Chlorprothixene is an antagonist of the following receptors: 5-HT2: antipsychotic effects, anxiolysis, weight gain D1, D2, D3: ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ...

*List of MeSH codes (D12.776.476)

... beta-adrenergic receptor kinase MeSH D12.776.476.250.067.249 -- cdc2 protein kinase MeSH D12.776.476.250.067.500 -- cdc28 ... tnf receptor-associated factor 1 MeSH D12.776.476.024.500.750 -- tnf receptor-associated factor 2 MeSH D12.776.476.024.500.875 ... tnf receptor-associated factor 3 MeSH D12.776.476.024.500.937 -- tnf receptor-associated factor 5 MeSH D12.776.476.024.500.968 ... receptor-regulated MeSH D12.776.476.024.417.500.100 -- smad1 protein MeSH D12.776.476.024.417.500.200 -- smad2 protein MeSH ...

*Adrenergic antagonist

Alpha blocker Beta blocker Adrenergic Receptor Antagonist Sympathetic nervous system Propanolol Beta-blockers and the treatment ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group ... The α-adrenergic antagonists have different effects from the β-adrenergic antagonists. Adrenergic ligands are endogenous ...

*Allium neapolitanum

... seems to have beta-adrenergic antagonist properties. The Plant List "BSBI List 2007". Botanical Society of ... Nencini C, Franchi GG, Micheli L (June 2010). "Cardiovascular receptor binding affinity of aqueous extracts from Allium species ... It produces round bulbs up to 2 cm across. Scape is up to 25 cm tall, round in cross-section but sometimes has wings toward the ...

*Cocaine intoxication

"Death temporally related to the use of a Beta adrenergic receptor antagonist in cocaine associated myocardial infarction". ... "Reflections on beta-adrenergic receptor blockers and cocaine use. A case in point". Revista Española De Cardiología. 62 (4): ... Schurr, James W.; Gitman, Brenda; Belchikov, Yuly (2014-12-01). "Controversial therapeutics: the β-adrenergic antagonist and ... "Potentiation of Cocaine-Induced Coronary Vasoconstriction by Beta-Adrenergic Blockade". Annals of Internal Medicine. 112 (12): ...

*History of hypertension

Black JW, Crowther AF, Shanks RG, Smith LH, Dornhorst AC (May 1964). "A new adrenergic beta receptor antagonist". Lancet. 1 ( ... February 1996). "Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy". J. Med. Chem ... The first member was verapamil, a derivative of papaverine that was initially thought to be a beta blocker and used for angina ... More recently angiotensin receptor blockers and renin inhibitors have also been introduced as antihypertensive agents. Esunge ...

*ICI-118,551

"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ...

*SR 59230A

... is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 ... "Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... Bellantuono V, Cassano G, Lippe C (August 2008). "The adrenergic receptor subtypes present in frog (Rana esculenta) skin". Comp ...
Neonatal-onset multisystem inflammatory disease (abbreviated NOMID, also known as chronic infantile neurologic cutaneous and articular syndrome, or CINCA) is a rare genetic periodic fever syndrome which causes uncontrolled inflammation in multiple parts of the body starting in the newborn period. Symptoms include skin rashes, severe arthritis, and chronic meningitis leading to neurologic damage. It is one of the cryopyrin-associated periodic syndromes. NOMID can result from a mutation in the CIAS1 gene (also known as NLRP3 gene), which helps control inflammation. Mutations in this gene also cause familial cold urticaria and Muckle-Wells syndrome. NOMID has been successfully treated with the drug anakinra. This syndrome is also known as the Prieur-Griscelli syndrome as it was first described by these authors in 1981. The age of onset is almost always before 3 months of age. Many infants are born preterm (1/3 cases) and dysmature. The babies are frequently small for dates. The placenta may be ...
The approval for Kineret was based on the results received from a Phase III open label and uncontrolled study. The study enrolled 43 NOMID patients who were aged between 0.7 and 46 years.. The patients were initially administered with Kineret dose of one to 2.4mg/kg body weight. The dose was adjusted by 0.5 to 1mg/kg increments, according to the specified protocol, up to a maximum of 10mg/kg daily. The maximum dose administered in the study was 7.6mg/kg/day. The average maintenance dose was three to 4mg/kg daily. Kineret was administered once-daily in some patients, and twice-daily in others.. The NOMID symptoms were measured using disease-specific Diary Symptom Sum Score (DSSS). The main disease symptoms were fever, rash, joint pain, vomiting and headache. The patients were treated for more than 60 months.. The results of the study were consistent in all subgroups. The improvements occurred in all individual disease symptoms comprising the DSSS. Common side effects found during the clinical ...
BACKGROUND: Mevalonate kinase deficiency (MKD) is a hereditary autoinflammatory syndrome marked by recurrent attacks of fever and inflammation. Severe enzyme deficiency results in mevalonic aciduria (MA) and milder deficiency in hyperimmunoglobulin D syndrome (HIDS). Treatment remains a challenge. OBJECTIVE: To observe the effect of the recombinant interleukin-1 receptor antagonist anakinra in patients with MKD. METHODS: A prospective observational study was undertaken. Two patients with MA started continuous treatment with anakinra (1-2 mg/kg/day) and nine patients with HIDS chose between continuous treatment and on-demand treatment (starting at first symptoms of attack, 100 mg/day or 1 mg/kg/day for 5-7 days). RESULTS: Anakinra induced partial remission in one patient with MA but there was no response in the other patient with MA. In one patient with HIDS continuous treatment induced complete remission for 7 months but was stopped because of side effects. Eight patients ...
Chronic infantile neurological cutaneous articular (CINCA) syndrome, also known as neonatal-onset multisystem inflammatory disease, is a rare congenital inflammatory disease characterised by cardinal signs including a variable congenital maculopapular urticarial rash, chronic non-inflammatory arthropathy with abnormal cartilage proliferation, and chronic meningitis with progressive neurological impairment associated with polymorphonuclear and occasionally eosinophilic infiltration.1 The CINCA syndrome is associated with childhood uveitis and papillitis with chronic disc swelling.2 It may occur as a result of mutations of the CIAS1 gene that encodes cryopyrin, which results in reduced apoptosis of the inflammatory cells with up regulation of interleukin 1 (IL1).3-5 Consequently, the CINCA syndrome responds poorly to immunosuppressives including steroids, and treatment has been limited until recent reports of successful treatment with the recombinant human IL1 receptor ...
Several studies indicate that local immunoregulation and associated cytokines have a putative role in the development of cancer. There is evidence that pro-inflammatory cytokines such as interleukin-1 (IL-1) are critically involved with tumour progression. IL-1 receptor antagonist (IL-1Ra) is known to down regulate and limit the inflammatory response. Therefore we attempted to examine the influence of the known polymorphism of the IL-1Ra gene on the development of human colorectal cancer (CRC). The study included 125 patients with CRC and 134 controls. Variable number tandem repeat (VNTR) polymorphism in intron 2 of the IL-Ra gene was analysed by the polymerase chain reaction method. There was a significant difference in genotype distribution between CRC patients and controls (P=0.025) and also in allelic frequencies (P=0.012). In detail the carriage rate of allele 3 in CRC patients was significantly increased compared with controls (P=0.007). We also found that the allelic ...
Anakinra (Kineret), a recombinant form of human interleukin-1 (IL-1) receptor antagonist, is approved for the treatment of rheumatoid arthritis (RA) in combination with methotrexate. Kineret is self-administered by daily subcutaneous injections in patients with active RA. The mechanism of action of anakinra is to competitively inhibit the local inflammatory effects of IL-1. Kineret is generally safe and well tolerated and the only major treatment-related side effects that appear are skin reactions at the injection site. Due to the relatively short half-life of anakinra, daily injection of the drug is required. This, in combination with the comparably high rates of injection-site reactions (ISRs) associated with the drug, can become a problem for the patient. The present review summarises published data concerning ISRs associated with Kineret and provides some explanations as to their cause. The objective is also to present some clinical experiences of how the ISRs can be ...
article{7e0a6fdc-7d33-427d-bbba-4e9f6dfd8fb7, author = {Saxne, Tore and Larsson, Lotta and Geborek, Pierre}, issn = {1529-0131}, language = {eng}, number = {9}, pages = {3049--3050}, publisher = {John Wiley & Sons}, series = {Arthritis and Rheumatism}, title = {Results of anakinra treatment in rheumatoid arthritis patients previously treated with tumor necrosis factor alpha blockade: comment on the article by Buch et al}, url = {http://dx.doi.org/10.1002/art.20640}, volume = {50}, year = {2004 ...
TY - JOUR. T1 - Combined data from two phase III trials of the NK1 antagonist aprepitant plus a 5HT3 antagonist and a corticosteroid for prevention of chemotherapy-induced nausea and vomiting. T2 - Effect of gender on treatment response. AU - Hesketh, P. J.. AU - Grunberg, S. M.. AU - Herrstedt, J.. AU - De Wit, R.. AU - Gralla, Richard J.. AU - Carides, A. D.. AU - Taylor, A.. AU - Evans, J. K.. AU - Horgan, K. J.. PY - 2006/4. Y1 - 2006/4. N2 - Goals of work: Prevention of chemotherapy-induced nausea and vomiting (CINV) with standard antiemetics has been more difficult to achieve in female patients. Data from two phase III trials of the NK1 antagonist aprepitant were assessed for potential effect of gender on treatment response. Patients and methods: 1,044 patients receiving cisplatin (≥70 mg/m 2) were randomly assigned to control regimen [ondansetron (O) 32 mg i.v. and dexamethasone (D) 20 mg p.o. on day 1; D 8 mg twice daily on days 2-4] or aprepitant (A) regimen (A 125 mg p.o. plus O 32 ...
Autosomal dominant mutations in NLRP3 in humans leads to three autoinflammatory syndromes collectively referred to as cryopyrin-associated periodic syndromes (CAPS; also called cryopyrinopathies) (48, 49, 50, 51). Gain-of-function mutations of NLRP3 cause a lowered activation threshold that leads to IL-1β secretion even in the absence of a stimulus in vitro (36, 52, 53). All CAPS are characterized by increased levels of IL-1β in the absence of infection. CAPS consist of a spectrum of diseases ranging from the mild, such as familial cold autoinflammatory syndrome (FCAS), to the intermediate, such as Muckle-Wells syndrome (MWS), to the severe, such as chronic infantile neurological, cutaneous and articular (CINCA) syndrome, also known as neonatal-onset multisystem inflammatory disease (NOMID). All three syndromes present with fever, urticaria-like rash, and varying degrees of arthropathy and neurological manifestations (4, 54, 55, 56). FCAS consists of the mildest symptoms, including ...
In the first part of this clinical trial, we reported that 13 weeks of IL-1Ra treatment with anakinra reduced A1C, improved β-cell function, and reduced inflammatory markers (16). In the present protocolled follow-up study, we show that the reduced PI/I ratio and CRP and IL-6 serum levels were maintained 39 weeks after anakinra withdrawal, indicating that at least 39 weeks of remission of these parameters were caused by 13 weeks of anakinra treatment.. Furthermore, a subgroup analysis showed that the 21 (62%) patients who experienced any reduction in A1C after 13 weeks of IL-1Ra treatment with anakinra (responders) maintained their anakinra-induced improved β-cell function assessed by both the PI/I ratio and stimulatory testing 39 weeks after anakinra withdrawal, whereas the β-cell function of the patients treated with placebo and those unresponsive to anakinra treatment further deteriorated after cessation of placebo and anakinra therapy, respectively. The superior β-cell function of the ...
Objectives:. The aim of the Anti-Interleukin-1 in Diabetes Action trial (AIDA) study is to test the feasibility, safety/tolerability and potential efficacy of anti-IL-1 therapy in maintaining or enhancing beta-cell function in people with new onset Type 1 diabetes.. Trial Design:. A randomized, placebo controlled, double masked, parallel group, multicentre trial of IL-1 antagonism in subjects with newly-diagnosed Type 1 diabetes. Patients are instructed to inject 100 mg human recombinant interleukin-1 receptor antagonist (anakinra, Kineret®, Amgen, CA) or placebo s.c. once daily for 2 years. Endpoints will be evaluated every three months, with an interim analysis after 6 months.. Trial population:. The design will be a two-stage phase 2a study to address feasibility, safety/tolerability and potential efficacy. In the first phase 80 patients between 18 and 35 years of age with new on-set Type 1 diabetes will be randomized to anakinra or placebo, and endpoints ...
These data demonstrate icIL-1ra type I mRNA, sIL-1ra mRNA, and IL-1ra protein in human coronary arteries. IL-1ra protein colocalizes with IL-1β predominantly in the endothelium of these arteries, with less IL-1ra mRNA expression occurring in less-diseased DCM arteries. To our knowledge, this is the first documentation of IL-1ra expression by HCAECs. We also show only icIL-1ra type I mRNA expression in HUVECs and HCAECs stimulated in vitro with LPS/PMA or TGF-β. Previous reports have failed to detect IL-1ra mRNA in these cell types with the use of other stimuli and less sensitive detection methods, such as Northern blots,5 and there are no previous reports of immunohistochemistry for IL-1ra in human vessels. With the use of immunoprecipitation/Western blot techniques, our data also confirm that the expression of IL-1ra in HUVECs and HCAECs is intracellular. We have also demonstrated that the rare allele (IL-1RN *2/*2) of a VNTR polymorphism in the IL-1RN gene is associated with significantly ...
Kineret - Get up-to-date information on Kineret side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Kineret
Neonatal-onset multisystem inflammatory disease (NOMID) also known as chronic infantile neurological, cutaneous and articular syndrome (CINCA). Authoritative facts about the skin from DermNet New Zealand.
The IL-1 cytokine network in epidermal cells was studied in vitro, using the spontaneously transformed HaCAT human keratinocyte line. Intracellular (ic) IL-1 alpha and IL-1 receptor antagonist protein (IL-1Ra) following cell lysis were readily identified assayed using a capture ELISA; whereas in culture supernatants IL-1Ra was not detected, and IL-1 alpha was present at only very low levels. Confluent cultures of HaCAT cells were shown to provide optimal conditions for the study, since confluence increased the icIL-1Ra:IL-1 alpha ratio to a level as seen in vivo, which was independent of Ca2+ concentration in the culture medium. The IL-1Ra extracted from HaCAT cell lysates was functionally active, as demonstrated in the mouse thymocyte co-proliferation assay which could be blocked using a rabbit anti-IL-1Ra antibody. Transforming growth factor-beta (TGF-beta 1) stimulated a dose-dependent increase in HaCAT cell IL-1 alpha without changing ...
Gentaur molecular products has all kinds of products like :search , Alpha Dia \ Human Recombinant Purified Leptin Triple mutant Antagonist Protein \ LEP21-TM-20 for more molecular products just contact us
Actually, a clinical and laboratory remission, the eventual goal of the treatment, was achieved with anakinra. She was in remission, both under anakinra and canakinumab, according to disease activity score proposed by Kümmerle-Deschner et al.,(2,3) defined as a score less than 5 and normal serum CRP and SAA levels. In the absence of any clinical and laboratory sign of ongoing inflammation under anakinra, it is interesting for proteinuria to decrease further with canakinumab, although it was previously shown that anakinra-resistant cases may benefit from canakinumab and more patients achieved remission under canakinumab compared to anakinra.(3,4) Furthermore, to our knowledge, no case of canakinumab- resistant autoinflammatory disease, responsive to anakinra was reported to date. These observations are possibly due to the difference in half-lives and mechanisms of action between the two interleukin-1 blocking agents and may reflect an issue of efficacy. In case of amyloidosis secondary to MWS, ...
Chronic infantile neurologic cutaneous and articular (CINCA) syndrome, also known as neonatal onset multisystem inflammatory disease, or NOMID, is a congenital inflammatory disorder characterized by a triad of neonatal onset of cutaneous symptoms (skin rash), chronic meningitis, and joint pain with recurrent fever and inflammation. CINCA is the most severe form of the cryopyrin associated periodic syndromes (CAPS) caused by mutations in the CIAS1/NLRP3 gene. About 50% of affected individuals have mutations in this gene. This condition is inherited in an autosomal dominant fashion ...
IL-1R antagonist (IL-1Ra) exists as three well-characterized isoforms. The 17-kDa secretory IL-1Ra (sIL-1Ra) and 18-kDa intracellular IL-1Ra (icIL-1RaI) arise by alternative transcription of the same IL-1Ra gene. The recently described 16-kDa intracellular IL-1Ra (icIL-1RaII) is formed by alternative translation initiation of sIL-1Ra mRNA. Transcription and translation of IL-1Ra isoforms were examined in LPS-stimulated human neutrophils and PBMC using RT-PCR, ELISA, and Western blot analysis. LPS stimulation of neutrophils resulted in elevated sIL-1Ra mRNA levels by 1 h, whereas icIL-1RaI mRNA remained undetectable through 22 h of culture. Extracellular glycosylated sIL-1Ra protein and intracellular icIL-1RaII were observed in LPS-stimulated neutrophils by 3 h of culture; no icIL-1RaI protein was detected by immunoblot. LPS stimulation of PBMC resulted in elevated sIL-1Ra mRNA levels by 1 h and detectable icIL-1RaI mRNA at 8 h of culture. LPS-stimulated PBMC demonstrated extracellular glycosylated sIL
Kineret (anakinra) is a FDA-approved drug indicated for rheumatoid arthritis. Anakinra is a recombinant, nonglycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra). Anakinra blocks the biologic activity of IL -1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic effects including inflammatory and immunological responses.. This is a pilot, prospective, non-randomized, consecutive enrollment study that will enroll up to 12 subjects who meet the study defined inclusion and exclusion criteria.. Subjects will undergo standard of care chemotherapy treatment/regimens (i.e., modified FOLFIRINOX). Subjects will be dispensed a 2 weeks supply of anakinra the day they begin chemotherapy. They will be instructed to begin self-administering the ...
Human UC11 astrocytoma cells were used to investigate the role of protein kinase C (PKC) and other kinases in neurokinin (NK)1 receptor desensitization. The selective NK1 receptor agonist [Sar9,Met(O2)11]-substance P stimulated a biphasic accumulation of [3H]inositol phosphates ([3H]IPs) in the presence of 10 mM LiCl in cells that had been prelabeled with [3H]inositol. An initial rapid phase of [3H]IP accumulation during the first 1 min was followed by a slower sustained phase for up to 90 min. These results demonstrate that the human NK1 receptor desensitizes rapidly but only partially. The selective PKC inhibitor Ro31-8220 did not prevent rapid NK1 receptor desensitization but after a longer incubation significantly potentiated human NK1 receptor agonist-stimulated accumulation of [3H]IPs. These results suggest that, although PKC does not ...
The Autoinflammatory Alliance is a non-profit dedicated to increasing awareness, care and treatment for patients with Cryopyrin-Associated Periodic Syndromes, including: NOMID/CINCA, Muckle-Wells (MWS) Familial Cold Autoinflammatory Syndromes (FCAS), and other autoinflammatory diseases.
Looking for online definition of aprepitant in the Medical Dictionary? aprepitant explanation free. What is aprepitant? Meaning of aprepitant medical term. What does aprepitant mean?
In addition to, CB1-D2 receptor heteromers, not long ago Together with the aid of biochemical and biophysical research CB1-CB2 receptor heteromers is documented in nucleus accumbens and globus pallidus [175]. Typical attribute aspect observed with CB1-CB2 receptor heteromers is, CB1 receptor antagonists blocks the result of CB2 receptor agonists and, conversely, CB2 receptor antagonists blocks the result of CB1 receptor agonists As a result demonstrating a bidirectional phenomenon of cross-antagonism [175]. These heteromers may well describe preceding conflicting effects and could serve as therapeutic targets. Modern evidence implies that dopamine modulates the activity of SNpc neurons not just by regular dopamine ...
Efficacy and safety were evaluated in 152 aprepitant and 150 control patients. The proportion of patients experiencing no emetic episodes was higher in the aprepitant regimen vs the control regimen during both acute (71.1% vs 53.3%) and delayed (55.3% vs 28.0%) phases. The median time to first vomiting (overall) was significantly longer for aprepitant vs control (94.5 vs 26.0 hours; P < 0.0001). The proportion of patients not requiring rescue medication use was higher for aprepitant vs control (66.4% vs 48.7%), and the time to first rescue medication use was longer for aprepitant vs control (P = 0.0024). Adverse events were similar between regimens and consistent with those in patients undergoing chemo. ...
Your faithful babysitter horse limps a little in the mornings, and he has a hard time getting up if hes been laying down. You dread it, but you know the reality is that arthritis might be setting in or getting worse.. Youve tried joint injections, and while that might have worked for a while, hes in pain again. So now what?. In AQHAs FREE Horse Arthritis Treatment ebook, youll learn about a new treatment option - IRAP - that is gaining results in horses with osteoarthritis.. Your first question might be, "What the heck is IRAP, anyway?" Youll get the answer to that question and others when you download this free report.. IRAP stands for Interleukin-1 receptor antagonist protein, and it might be able to help decrease inflammation and pain in joints affected by arthritis.. Your FREE Horse Arthritis Treatment ebook will show you:. ...
Aprepitant EP Impurity C ; Aprepitant para-Biphenyl Impurity ; 4-Defluoro-4-(p-fluorophenyl)aprepitant ; 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(Trifluoromethyl)phenyl]ethoxy]-3-(4′-fluoro biphenyl-4-yl) morpholin-4-yl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one and ...
Rolapitant is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR). By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long ...
Phase II study to evaluate the safety and efficacy of the oral neurokinin-1 receptor antagonist casopitant (GW679769) administered with ondansetron for the prevention of postoperative and postdischarge nausea and vomiting in high-risk patients.
The inflammatory effects of IL-1α/β are controlled by IL-1R antagonist (IL-1Ra). One IL-1Ra isoform is secreted, whereas three other isoforms (intracellular IL-1Ra [icIL-1Ra] 1, 2, and 3) are supposed to remain intracellular because of the absence of a signal peptide. In contrast to the well-characterized function of the secreted isoform, the biological role of the intracellular isoforms remains largely unclear. icIL-1Ra1 represents the major isoform in keratinocytes. We created icIL-1Ra1−/− mice and investigated the role of icIL-1Ra1 in Aldara (5% imiquimod)-induced psoriasis-like skin inflammation. Naive icIL-1Ra1−/− mice bred habitually and exhibited a normal phenotype. icIL-1Ra1 deficiency aggravated Aldara-induced skin inflammation, as demonstrated by increased ear thickness and increased mRNA levels of key proinflammatory cytokines. No intracellular effect of icIL-1Ra1 could be detected in isolated keratinocytes using RNA-sequencing analysis; however, Aldara treatment led to ...
Background. There are few data on anakinra use after failure of conventional medications for crystal-induced peripheral arthritis and/or crowned dens syndrome among complex hospitalized patients. Methods. We retrospectively analyzed the outcome of six patients affected with subacute crystal-induced arthritis who had received anakinra in second or third line therapy, including three patients with crowned dens syndrome and three others with gouty arthritis. Patients comorbidities, reasons for anakinra use and associated drugs, and outcomes were recorded. Results. All patients presented with elevated inflammatory syndrome, systemic symptoms with poly/oligoarthritis. Except for absolute contraindications, all patients were previously treated with full or decreased dose of NSAID, colchicine, and/or glucocorticoids, with unsatisfactory response. All three gouty patients exhibited complete responses in all acute involvements under anakinra within 3 to 5 days, including one of them who needed the
Aprepitant Oral capsule, Aprepitant Oral capsuleWhat is this medicine?APREPITANT (ap RE pi tant) is used with other medicines to prevent nausea and vomitin
The Autoinflammatory Alliance is a non-profit dedicated to increasing awareness, care and treatment for patients with Cryopyrin-Associated Periodic Syndromes, including: NOMID/CINCA, Muckle-Wells (MWS) Familial Cold Autoinflammatory Syndromes (FCAS), and other autoinflammatory diseases.
Dr. Sarah Altman is participating in a clinical trial to evaluate the efficacy of a novel neurokinin-3 receptor antagonist compared to a placebo in improving menstrual regularity, hirsutism, and other symptoms in women between 18-45 years of age with oligo-amenorrhea due to PCOS.. Please contact Dr. Sarah Altman if you are interested:. Aventiv Research 614-501-6164. 99 N Brice Rd Suite 260 Columbus, OH 43213. [email protected] ...
[140 Pages Report] Muckle-Wells Syndrome Market categorizes the global market By family of Cryopyrin (Associated periodic syndromes, mutation of CIAS1 gene) & By Geography
The "P" in substance "P" [SP] is mistakenly thought to signify Pain or Psychiatric substance. Substance P ("P" standing for "Preparation" or "Powder") is a neuropeptide - but only nominally so, as it is ubiquitous. Its receptor - the neurokinin type 1 - is distributed over cytoplasmic and nuclear membranes of many cell types (neurons, glia, endothelia of capillaries and lymphatics, fibroblasts, stem cells, white blood cells) in many tissues and organs. SP amplifies or excites most cellular processes.[15][16]. Substance P is a key first responder to most noxious/extreme stimuli (stressors), i.e., those with a potential to compromise biological integrity. SP is thus regarded as an immediate defense, stress, repair, survival system. The molecule, which is rapidly inactivated (or at times further activated by peptidases) is rapidly released - repetitively and chronically, as warranted, in the presence of a stressor. Unique among biological processes, SP release (and expression ...
This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in huma
We present data demonstrating the gene expression of substance P and its receptor in human peripheral blood-isolated monocytes and macrophages. Using the RT-PCR assay, preprotachykinin-A (substance P) mRNA is detected in human peripheral blood-isolated monocytes and macrophages. Among the alpha, beta, and gamma transcripts of the substance P gene, only the beta and gamma transcripts are detectable in these cells. By Southern blot assay these RT-PCR-amplified transcripts are recognized using a specific substance P probe. Sequence analysis of the RT-PCR products from both monocytes and macrophages also confirmed the structure of these transcripts, which are identical to those found in human neuronal cells. At the protein level, both human monocytes and macrophages produced endogenous substance P as determined by an enzyme immunoassay. Capsaicin, a vanillyl fatty acid amide (ingredient of hot pepper), released substance P from both human ...
A collection of disease information resources and questions answered by our Genetic and Rare Diseases Information Specialists for Muckle-Wells syndrome
The next medicine which is costliest in the world and is in our list is named as Arcalyst. This drug is manufactured by the pharmaceutical company named as Renege Pharmaceuticals. The other names of this drug are Rilonacept and IL-1 Trap. This medicine is used for the treatment of disease named as the Cryopyrin and its associated periodic syndromes. And also for the treatment of Muckle-Wells syndrome, familial cold autoinflammatory syndrome and neonatal onset multisystem inflammatory disease. If you are in need of this drug then you will have to pay 250,000 US dollars per year which is too much for a common man. This drug has been named as the Orphan Drug by the United States Food and Drug Administration. This drug was approved by the FDA on 8th May 2012.. 6. Myozyme. ...
Methods The eyes of IL-1Ra-deficient BALB/c mice were monitored histologically and by intravital videomicroscopy to determine if uveitis developed along with the expected spontaneous arthritis in ankles and knees. Expression levels of IL-1R and its negative regulators (IL-1Ra, IL-1RII, IL-1RAcP and single Ig IL-1R-related molecule) in eye and joint tissues were compared. Differences in uveitis induced by intraocular injection of lipopolysaccharide (LPS) in mice lacking IL-1R or IL-1Ra were assessed.. ...
The interleukin-1 receptor antagonist (IL-1RA) is a protein that in humans is encoded by the IL1RN gene. IL-1RA was initially called the IL-1 inhibitor and was discovered separately in 1984 by two independent laboratories. IL-1RA is an agent that binds non-productively to the cell surface interleukin-1 receptor (IL-1R), the same receptor that binds interleukin 1 (IL-1), preventing IL-1 from sending a signal to that cell. IL-1RA is a member of the interleukin 1 cytokine family. IL1Ra is secreted by various types of cells including immune cells, epithelial cells, and adipocytes, and is a natural inhibitor of the pro-inflammatory effect of IL1β. This protein inhibits the activities of interleukin 1, alpha (IL1A) and interleukin 1, beta (IL1B), and modulates a variety of interleukin 1 related immune and inflammatory responses. This gene and five other closely related cytokine genes form a gene ...
Anakinra 100 mg daily by subcutaneous injection was started. Three hours after the first dose of anakinra, the rash resolved completely and her joint pain began to improve. Continuing with daily anakinra, the urticaria did not recur and the arthritis resolved. Two weeks after initiation of anakinra, the leukocytosis resolved; hemoglobin, CRP, and ferritin were normalized; and ESR was markedly improved. Her serum IgA level initially declined slightly, but reached a plateau and was not normalized (Figure 1). Continuation of daily anakinra sustained the clinical therapeutic effects and improvement of laboratory measures of systemic inflammation. She remained in remission at 8 months after initiation of anakinra. However, her finger-clubbing remained with no changes.. The clinical constellation of this case fits the spectrum of autoinflammatory diseases and closely resembles Schnitzlers syndrome. However, the major distinction of this case from Schnitzlers syndrome was the lack of monoclonal IgM ...
Background Anakinra pharmacokinetics and pharmacodynamics were investigated in children and adolescents treated for systemic-onset juvenile idiopathic arthritis (SJIA) and autoinflammatory syndromes.
Affinity Labels; Animals; Binding, Competitive; Cell Membrane; Electrophoresis, Polyacrylamide Gel; GTP-Binding Proteins; Guanosine 5-O-(3-Thiotriphosphate); Guanylyl Imidodiphosphate; Kinetics; Molecular Weight; Rats; Rats, Inbred Strains; Receptors, Neurokinin-1; Receptors, Neurotransmitter; purification; Submandibular Gland. ...
The majority of calls to poison control centers involve children younger than 5 years of age. Fortunately, children account for a minority of serious poisonings requiring emergency hospital treatment. Most common childhood ingestions involve nontoxic substances or nontoxic doses of potentially toxic drugs or products (See Nontoxic or Minimally Toxic Household Products). Table I-43 lists important causes of serious or fatal childhood poisoning, which include iron supplements (See Iron); tricyclic antidepressants (See Antidepressants, Tricyclic); cardiovascular medications such as digitalis (See Digoxin and Other Cardiac Glycosides), beta receptor antagonists (See Beta-Adrenergic Blockers), or calcium antagonists (See Calcium Channel Antagonists); methyl salicylate (See Salicylates); and hydrocarbons (See Hydrocarbons). ...
In treatment period 1, subjects will receive oral casopitant 150 mg on Day 1 and 50 mg on Days 2 and 3. In treatment period 2, they will be administered ketoconazole 400 mg once daily on Day 1 to Day 9 and oral casopitant 150 mg on Day 4 and 50 mg on Days 5 and 6. There will be a 14-day washout period between treatment periods 1 and 2 ...
BackgroundSystemic inflammation is accepted as one of the pathophysiological mechanisms of atrial fibrillation (AF). The role of inflammation has been shown previously. Interleukin (IL) system is the main modulator of the inflammatory responses and genetic polymorphisms of IL-1 cluster genes are associated with increased risk for inflammatory diseases. ObjectivesTo investigate the association between polymorphisms of IL-1 cluster genes and lone AF. Subjects and MethodsDNA samples were collected from 70 proven lone AF patients and 70 healthy subjects. Genomic DNA was typed for the variable number of the tandem repeat (VNTR) IL-1 receptor antagonist (RN) gene polymorphism, IL-1B -511 C , T(rs16944) promoter polymorphism, and +3953 C , T(rs1143634) polymorphism in exon 5 by polymerase chain reaction. ResultsIn lone AF group the frequency of IL-1RN2/2 and IL-1RN1/2 genotypes were higher than in the control group (7.2% vs 4.3% and 48.5% vs 22.8%, respectively; (2) = 14.1; P = ...
2016-02-23 Swedish Orphan Biovitrum AB (publ) (Sobi(TM)), today announced that it has decided to initiate two clinical programs with Kineret® (anakinra) in North America, with the aim of evaluating two new potential indications for Kineret where a significant need for alternative treatment options exists: acute gout and Stills disease. An increasing body of evidence suggests…. Read more » ...
Emend capsules contain the active ingredient aprepitant, which is a type of medicine called a neurokinin receptor antagonist. It is used to prevent nausea and vomiting that can be caused by chemotherapy treatment for cancer.
Most autoinflammatory diseases are known to be genetic conditions with a gene identified as involved in causing the symptoms. Although we do not know all the factors that may be involved in triggering flares, or how one came to have … Continue reading →. ...
On October 22, Amgen announced that it had submitted a supplemental Biologics License Application with the U.S. Food and Drug Administration for the use of Kineret to inhibit the progression of structural damage in adult RA patients.. Juvenile Rheumatoid Arthritis. A 16-week multi-center, blinded, placebo-controlled study of 76 pediatric JRA patients (aged 2 years -17 years) included a 12-week open-label "run-in" period in which all patients were treated with Kineret (1 mg/kg daily subcutaneous injections). The results after 12 weeks show that 64 percent of the patients who reached week 12 and were assessed for efficacy (n=56) exhibited at least a 30 percent improvement in their disease based on the JRA Core Set Criteria when compared to baseline, and were considered responders. The JRA Core Set Criteria include number of active joints, number of joints with limited motion, physicians global assessment, patients/parents global assessment, childrens Health Assessment Questionnaire, and a lab ...
Thank you for your interest in spreading the word about Biochemical Society Transactions.. NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.. ...
A study in mice revealed how diet-induced changes to intestinal bacteria can influence autoinflammatory disease. The results could guide new approaches to these diseases.
Background: Multiple Sclerosis (MS) is a neurodegenerative disease. It involves inflammation and demyelination. Since cytokines play an important role in the development of MS, genes encoding cytokines such as the Interleukin (IL)-1 family are candidate genes for MS susceptibility. Objective: To determine the relationship between IL-1 gene family and MS in the Turkish population. Methods: A total of 409 MS patients and 256 healthy controls were included in the study. IL-1A -889 (rs1800587), IL-1 RN variable number tandom repeat (VNTR), IL-1B -511 (rs 16944) and IL-1B +3953 (rs 1143634) polymorphisms were investigated from the genomic DNA, obtained via blood samples. Results: No association was found between IL-1A and IL-1RN polymorphisms and susceptibility to MS. However, we have found significantly decreased frequency of IL-1B -511 genotype (p = 0.004) in MS patients compared to controls. In addition, there was a significant association between IL-1B -511 (1/2) genotype and early onset MS ...
H2-receptor antagonists and Mirtazapine, H2-receptor antagonists and Macrolides, H2-receptor antagonists and Lidocaine, H2-receptor antagonists, H1N1 influenza virus vaccine (nasal), H1N1 influenza virus vaccine (injectable), Online Electronic Medical Diagnosis and Drugs, Medications, Articles, Glossary
Conclusions We herein show somatic NLRP3 mosaicism underlying MWS, probably representing a shared genetic mechanism in CAPS not restricted to CINCA syndrome. The data here described allowed definitive diagnoses of these patients, which had serious implications for gaining access to anti-interleukin 1 treatments under legal indication and for genetic counselling. The detection of somatic mosaicism is difficult when using conventional methods. Potential candidates should benefit from the use of modern genetic tools.. ...
METHODS AND RESULTS: We measured serum RA concentrations in 1499 patients with angiographically confirmed coronary artery disease (mean age, 61 years; male, 67%) recruited from October 2008 and December 2011 in the Guangdong Coronary Artery Disease Cohort. During a median (interquartile range) period of 4.4 (3.6 to 6.1) years of follow-up, there were 295 all-cause mortality, among which 208 had cardiovascular mortality. Serum RA level was significantly lower in participants with mortality (median 21 [11-47] nmol/L) than in those without mortality (median 39 [19-86] nmol/L). In multivariate analyses, the hazard ratios for total mortality among those in the lowest (referent) to highest quartiles of serum RA measured at study entry were 1.0, 0.83, 0.74, and 0.56, respectively (P-trend,0.001). For cardiovascular mortality, the comparable hazard ratios were 1.0, 0.76, 0.69, and 0.60 (P-trend,0.001). Furthermore, high RA levels (defined as ,median) were associated with lower risk of total mortality ...
Thank you for your interest in spreading the word about The Journal of Immunology.. NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.. ...
Objective: Interleukin (IL)-1 impairs insulin secretion and induces beta-cell apoptosis. Pancreatic beta-cell IL-1 expression is increased and interleukin-1-receptor antagonist (IL-1Ra) expression reduced in patients with type 2 diabetes mellitus. Treatment with recombinant IL-1Ra improves glycemia and beta-cell function and reduces inflammatory markers in patients with type 2 diabetes mellitus. Here we investigated the durability of these responses.. Research Design and Methods: Among 70 ambulatory patients with type 2 diabetes and A1C and body mass index higher than 7.5% and 27, respectively, randomly assigned to receive 13 weeks of anakinra, a recombinant human IL-1Ra, or placebo, 67 completed treatment and were included in this double-blinded 39 week follow-up study. Primary outcome was change in betacell function following anakinra withdrawal. Analysis was done by intention-to-treat.. Results: ...
Hepatitis C virus (HCV) causes hepatitis, liver cirrhosis and hepatocellular carcinoma, and may also induce type II mixed cryoglobulinemia syndrome (MC), a disease characterized by clonal B-cell lymphoproliferations that can evolve into non-Hodgkins lymphoma (NHL). Interleukin-1 (IL-1) is a cytokine that plays an important role in initiating the cascade of events of immunoinflammatory responses through costimulation of T lymphocytes, B-cell proliferation, induction of adhesion molecules and stimulation of the production of other inflammatory cytokines. The role of IL-1 in immunoinflammatory responses is highlighted by the presence of endogenous regulators (IL-1 receptor antagonist, soluble receptors type 1 and II, human IL-1 accessory protein) that, when secreted into the blood stream may serve as endogenous regulators of IL-1 action. The aim of this study was to evaluate whether abnormalities in the blood levels of IL-1β IL-1 ...
stopcaidnow.org Our mission is simple-Educate, Provide Awareness, and Fund Researchers who are committed to finding a cure. StopCAIDnow(501c3) is focused on providing tools to better educate Doctors and the community on AutoInflammatory diseases. There is a need for an understanding of these diseases so proper diagnosis can be made, and treatment can be started. This will help alleviate the inflammation process, 7 the pain that comes with it. Proper diagnosis is urgent for the prognosis of these diseases. If left untreated damage to the tissues, organs & vision(for some) will not only be irreversible but devastating. ...
Unknown author (‎2003)‎. Aprepitant for nausea and vomiting during chemotherapy. WHO drug information 2003 ; 17(‎2)‎ : 107 https://apps.who.int/iris/handle/10665/72139 ...
Do not take this medicine if you already have nausea and vomiting. Ask your health care provider what to do if you already have nausea.. Birth control pills and other methods of hormonal contraception (for example, IUD or patch) may not work properly while you are taking this medicine. Use an extra method of birth control during treatment and for 1 month after your last dose of aprepitant.. This medicine should not be used continuously for a long time.. Visit your doctor or health care professional for regular check-ups. This medicine may change your liver function blood test results.. ...
If you are a society or association member and require assistance with obtaining online access instructions please contact our Journal Customer Services team ...
1812661DNAHomo sapiens 1cggcacgagg gcccagagga ataagttaac cttggtgcct gcgtccgtga gaattcagca 60tggaatgtct ctactatttc ctgggatttc tgctcctggc tgcaagattg ccacttgatg 120ccgccaaacg atttcatgat gtgctgggca atgaaagacc ttctgcttac atgagggagc 180acaatcaatt aaatggctgg tcttctgatg aaaatgactg gaatgaaaaa ctctacccag 240tgtggaagcg gggagacatg aggtggaaaa actcctggaa gggaggccgt gtgcaggcgg 300tcctgaccag tgactcacca gccctcgtgg gctcaaatat aacatttgcg gtgaacctga 360tattccctag atgccaaaag gaagatgcca atggcaacat agtctatgag aagaactgca 420gaaatgaggc tggtttatct gctgatccat atgtttacaa ctggacagca tggtcagagg 480acagtgacgg ggaaaatggc accggccaaa gccatcataa cgtcttccct gatgggaaac 540cttttcctca ccaccccgga tggagaagat ggaatttcat ctacgtcttc cacacacttg 600gtcagtattt ccagaaattg ggacgatgtt cagtgagagt ttctgtgaac acagccaatg 660tgacacttgg gcctcaactc atggaagtga ctgtctacag aagacatgga cgggcatatg 720ttcccatcgc acaagtgaaa gatgtgtacg tggtaacaga tcagattcct gtgtttgtga 780ctatgttcca gaagaacgat cgaaattcat ccgacgaaac cttcccaaag atctccccat 840tatgtttgat gtcctgattc ...
Why are people interested in IL-1? Because IL-1 cytokines family are usually over-expressed at tumor sites or inflammatory, these cytokines could be used as bio-markers to help diagnose in advance. Also, since IL-1α, IL-1β and IL-1ra all have the ability to bind to the type 1 IL-1 receptor(IL-1R), and the binding of IL-1α or IL-1β to IL-1R is an early step in IL-1 signal transduction, blocking this interaction may therefore be a useful target for the development of new drugs[5]. For example, in this paper[7], the author therapeutically designed a superior cytokine antagonist(EBI-005, optimized receptor antagonist chimerized with IL-1β and IL-1Ra) for topical ophthalmic use. ...
Background and purpose: The inflammatory cytokine interleukin-1 (IL-1) has profound actions in the brain causing neuronal cell death and exacerbating mind damage. barrier model was generated by co-culture of porcine mind microvascular endothelial cells with astrocytes. The mechanisms of transcellular transport of IL-1β and IL-1 receptor antagonist were characterized with this model using endocytosis inhibitors and IL-1 receptor-blocking antibodies. Important results: Transcellular IL-1β and IL-1 receptor DMH-1 antagonist transport was temperature-dependent and IL-1β was transferred with higher affinity than IL-1 receptor antagonist. IL-1β inhibited IL-1 receptor antagonist transport more potently than IL-1 receptor antagonist inhibited IL-1β transport. Transport of IL-1β and IL-1 ...
Swedish Orphan Biovitrum AB (publ) operates in the Pharmaceutical Preparations sector. Swedish Orphan Biovitrum publ AB is a Sweden-based pharmaceutical company. The Company develops, manufactures and sells medications within hemophilia, autoimmune diseases, metabolic diseases and cancer supportive care. The Companys product portfolio is divided into three business segments: the Core Products segment offers pharmaceuticals within Inflammation area, and Genetics and metabolic therapeutic area; the Partner Products segment offers about 40 pharmaceuticals within hematology, oncology and emergency medicines, and the ReFacto Manufacturing segment. The Company has subsidiaries in Sweden, Denmark, Finland, Norway, United Kingdom and France, among others. On September 9, 2013, the Company acquired the full rights to develop and commercialize Kineret (anakinra) from Amgen, the biotechnology company based in the United States.
Naproxen 100 mg - 1 month diagnosed with adult onset stills disease and on kineret (anakinra) 100 mg naproxen 500 mg prednisone 20mg. What diet and natural remedies will help? None. Watch your carbohydrate and calorie intake to lessen weight gain related to prednisone. Other than that diet and home remedies are worthless.
Associates with OSMR to form the interleukin-31 receptor which activates STAT3 and to a lower extent STAT1 and STAT5. May function in skin immunity (PubMed:15184896). Mediates IL31-induced itch, probably in a manner dependent on cation channels TRPA1 and TRPV1 (PubMed:24373353). Positively regulates numbers and cycling status of immature subsets of myeloid progenitor cells in bone marrow in vivo and enhances myeloid progenitor cell survival in vitro (PubMed:17379091).
The proinflamatory cytokine interleukin-1b (IL-1b) and the interleukin-1 receptor antagonist (IL-1Ra), which is a specific inhibitor of IL-1 activity, have been shown to be induced in vitro byMycobacterium tuberculosis. Moreover patients with tuberculosis present an elevated serum concentration of IL-1Ra and IL-1Ra was identified as a marker of disease activity in tuberculosis (Juffermans et al., 1998). Within the IL-1b gene, two biallelic polymorphisms have been identified at positions −511 and +3953, respectively. An 86-base pair variable number of tandem repeats polymorphism with five different alleles is found in theIL-1Ra gene. Genetic analysis detected that theIL-1Ra VNTR allele A2 was associated with a higher production of IL-1Ra in response to M. tuberculosisinfection. Indeed, individuals with the IL-1Ra A2+ allele produced 1.9-fold more IL-1Ra than patients with IL-1Ra A2- alleles (Wilkinson et al., 1999). The two polymorphisms in IL-1bwere not clearly associated ...
The Autoinflammatory Alliance is very pleased to have our new 2015 Holiday Ornament in stock! We will be sending these customizable "Rare Wonder" snowflake photo ornaments to all our donors that have contributed generously this year, volunteered their time, or … Continue reading →. ...
Tolerance of monocytes/macrophages to endotoxin (lipopolysaccharide [LPS]) can be induced both in vivo and in vitro by LPS itself. Exposure to LPS, even at a very low dose, induces a downregulation of cytokine response to a second high dose LPS challenge. To learn more about the unknown mechanisms of this phenomenon, we studied the role of antiinflammatory cytokines in this process. Preculture of human peripheral blood monocytes for 24 hours with low concentrations of LPS induced hyporesponsiveness to high-dose LPS rechallenge with respect to tumor necrosis factor (TNF) alpha and interleukin (IL) 10 but not IL-1RA production. These results suggest that LPS tolerance reflects a functional switch of monocytes rather than a general LPS hyporesponsiveness. IL-10 and transforming growth factor (TGF) beta 1 showed additive effects in replacing LPS for induction of LPS hyporesponsiveness in vitro. Additionally, neutralizing anti-IL-10 and anti-TGF-beta monoclonal antibodies ...
The cytokine mda-7/interleukin (IL)-24 has been suggested to function as a tumor suppressor in a number of solid tumor types and to promote cancer-specific cell death in a context-dependent manner. Li and colleagues reveal that mammary tumorigenesis in rats was suppressed by single administration of an adenovirus-expressing mda-7/IL-24. Mechanistically, mda-7/IL-24 induced the expression of growth arrest-specific gene 3 (GAS3/PMP22) to inhibit the attachment and proliferation of tumor cells in part by blocking the interaction of β1-integrin with fibronectin. Using primary human breast cancer specimens, they found a positive correlation between the expression of the IL-24 receptor (IL20RA) and GAS3. Moreover, IL20RA expression was correlated with metastasis-free survival in HER2+ patient samples. Thus, a novel GAS3-integrin/fibronectin inhibitory pathway has been identified downstream of mda-7/IL-24 that can be targeted for therapy.. ...
SUMMARYAs Q fever is associated with an inflammatory syndrome, we determined circulating levels of inflammatory cytokines, cytokine antagonists, and activation markers of leucocytes in patients with acute Q fever and Q fever endocarditis. Tumour necrosis factor (TNF) and IL-6, but not IL-1β, were ma
039 and p=0.006, Erlotinib respectively). At week 12, the TB IRIS group trended toward greater HLADR+ CD38+ CD8+ T cell counts than the Other IRIS group (p=0.072), and exhibited significantly greater counts than the No IRIS group (p=0.007) (Figure 3C). In contrast, CD8+ T cells expressing only HLADR were increased by HAART in both their relative frequency (Figure 3A) and absolute counts (Figure 3D). Figure 3 Frequencies and absolute counts of activated CD8 T cell subsets. A) Frequencies of activated CD8 T cell subsets according to CD38 and HLADR expression during follow up. The numbers in each quadrant correspond to the mean of all patients�� percentage … Figure 4 Expansion of activated naive CD8 T cells during TB IRIS.. Zebra plots of CD8+ T cell maturation subpopulations according to CCR7 and CD45RA expression (see Methods) in a week 8 sample from a TB IRIS patient (A), and of week 8 sample from an Other IRIS … No differences between groups in the absolute counts of CD38+ HLADR- or ...
Abstract:. Previous works from our laboratory demonstrated that the monoclonal antibody (MAb) called R7B4 is directed to an epitope shared by various receptors corresponding to the type I cytokine receptor family, containing the common motif WSXWS or the homologous F(Y)GEFS. Later a consensus peptide significantly recognized by the MAb was identified and synthesized (sequence HGYWSEWSPE). In the present work, an homologous of the consensus sequence (HHGYWSEWSPE) was conjugated to PADRE adjuvant to produce Ab that could simulate the MAb activity, that is, acting as hormone and/or cytokine antagonists. The covalently conjugated peptide-PADRE was a better immunogen than the consensus peptide alone according to the reactivity of sera from C57BL/6 immunized mice and, besides, no Ab to PADRE were detected. Furthermore, Ab to consensus peptide elicited after peptide-PADRE inoculation into mice behaved as immunomodulatory agents, ...
Interleukin 1 receptor antagonist (IL-1Ra) is an acute-phase protein.: Interleukin 1 receptor antagonist (IL-1Ra) levels are elevated in the blood of patients w
View our 3 Oxytocin Receptor Antagonists products for your research including Oxytocin Receptor Antagonists Small Molecules and Oxytocin Receptor Antagonists Peptides.
Buy BAN ORL 24 (CAS 1401463-54-4), a water soluble potent, selective ORL1 non-peptide antagonist. Join researchers using high quality BAN ORL 24 from Abcam and…
Most people think all arthritis is the same, which causes major misunderstanding for patients living with the second most popular type of arthritis - the kind caused by autoimmune and autoinflammatory diseases.
TESARO Inc has announced that rolapitant (Varubi), a neurokinin-1 (NK-1) receptor antagonist, is now available in the United States.
Preferential exclusion of sucrose from recombinant interleukin-1 receptor antagonist: Role in restricted conformational mobility and compaction of native state Journal Article ...
Wolters Kluwer Health may email you for journal alerts and information, but is committed to maintaining your privacy and will not share your personal information without your express consent. For more information, please refer to our Privacy Policy ...
Patient and physician information for this medication, which is used to relieve pain and swelling caused by rheumatoid arthritis. ...
An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSORs product, whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the SPONSORs product, was also an AE. Changes resulting from normal growth and development which did not vary significantly in frequency or severity from expected levels were not to be considered adverse events. Vomiting and retching were not defined as AEs during the period of data collection (24 hours following the end of surgery) unless they met the definition of an SAE. The percentage of participants discontinuing study due to an AE was reported by dose group ...
The pseudotetrapeptide compound MEN 11558 is a potent antagonist at the human tachykinin NK2 receptor. It was being developed by Menarini in Italy, and is an
Expression of IL20RA (IL-20R1, ZCYTOR7) in cancer tissue. The cancer tissue page shows antibody staining of the protein in 20 different cancers.
Recombinant Human IL-10 (mammalian expressed, carrier-free) - IL-10 was first described as a cytokine that is produced by T helper 2 (Th2) cell clones.
Buy CellAura fluorescent D3 antagonist [BP897-red] - an affordable, high quality D3 receptor antagonist from Hello Bio, a trusted supplier for life science researchers worldwide
GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
The mGluR4 (type III) receptor antagonist MPPG specifically prevented the change in paired pulse facilitation (PPF) upon inhibition of glutamate uptake.A shows
This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Description - Human interleukin 1 receptor antagonist (IL1RN, IL1F3, IL1RA, IRAP; Gene ID: 3557) is a protein that is produced in at least two forms, one that stays inside the cell and one that is secreted. This assay is for the secreted version. IL-1RA is secreted by various cell types including epithelial cells, monocytes, and adipocytes. It binds to the IL-1 receptor thus preventing signaling by both IL-1α and IL 1β cytokines ...
The present invention relates to the use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( 		               ...Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ( ...

... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E, ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 ...
more infohttp://www.bio-medicine.org/biology-technology/Screening-for-potential-beta-2-adrenergic-receptor-antagonists-using-CypHer5E-and-IN-Cell-Analyzer-1000-1255-1/

Current Computer - Aided Drug Design: Ingenta Connect Table Of ContentsCurrent Computer - Aided Drug Design: Ingenta Connect Table Of Contents

Analysis of Drug Design for a Selection of G Protein-Coupled Neuro- Receptors Using Neural Network Techniques pp. 202-211(10) ... Ligand and Structure Based Models for the Identification of Beta 2 Adrenergic Receptor Antagonists pp. 222-236(15) Authors: ... Interaction studies of Withania somniferas key metabolite Withaferin A with different receptors associated with cardiovascular ...
more infohttps://www.ingentaconnect.com/content/ben/cad/2015/00000011/00000003

Cell lines expressing recombinant aequorin and a G-protein coupled receptor for functional screening (         INTRODUCTION    ...Cell lines expressing recombinant aequorin and a G-protein coupled receptor for functional screening ( INTRODUCTION ...

... receptor,for,functional,screening,biological,advanced biology technology,biology laboratory technology,biology device ... INTRODUCTION ...Many G-protein coupled receptors (GPCRs) trigger upon binding of an a...One of the methods of choice (reviewed ... TSH-Receptor. This system can be used to detect either agonists or antagonists. Surmountable antagonists as well as non- ... Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000. 11. The use of CypHer5 ...
more infohttp://www.bio-medicine.org/biology-technology/Cell-lines-expressing-recombinant-aequorin-and-a-G-protein-coupled-receptor-for-functional-screening-1376-1/

Code System ConceptCode System Concept

Product containing beta adrenergic receptor antagonist (product) {33252009 , SNOMED-CT } Other Relationships No other ... Product containing beta-2 adrenergic receptor antagonist (product). Code System Preferred Concept Name. Product containing beta ...
more infohttps://phinvads.cdc.gov/vads/ViewCodeSystemConcept.action?oid=2.16.840.1.113883.6.96&code=770388003

Stachel-independent modulation of GPR56/ADGRG1 signaling by synthetic ligands directed to its extracellular region | PNASStachel-independent modulation of GPR56/ADGRG1 signaling by synthetic ligands directed to its extracellular region | PNAS

1994) Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor. Mol Pharmacol 45:390-394. ... 1982) Adrenergic receptors in the heart. Annu Rev Physiol 44:475-484. ... 2016) Dihydromunduletone is a small-molecule selective adhesion G protein-coupled receptor antagonist. Mol Pharmacol 90:214-224 ... 2011) Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature 477:549-555. ...
more infohttp://www.pnas.org/content/114/38/10095

Code System ConceptCode System Concept

Substance with beta adrenergic receptor antagonist mechanism of action (substance) {373254001 , SNOMED-CT } ... Beta-2 adrenergic receptor antagonist Current Synonym true false 3780864010 Beta-2 adrenergic receptor blocker Current Synonym ... Substance with beta-2 adrenergic receptor antagonist mechanism of action Current Synonym true false ... Substance with beta-2 adrenergic receptor antagonist mechanism of action (substance). Code System Preferred Concept Name. ...
more infohttps://phinvads.cdc.gov/vads/ViewCodeSystemConcept.action?oid=2.16.840.1.113883.6.96&code=37751002

Ultibro Breezhaler | European Medicines AgencyUltibro Breezhaler | European Medicines Agency

Muscarinic receptor antagonists and long-acting beta-2-adrenergic agonists are commonly combined in the management of COPD. ... Glycopyrronium is a muscarinic-receptor antagonist. It works by blocking some receptors called muscarinic receptors, which ... Indacaterol is a long-acting beta-2 agonist. It works by attaching to beta-2-adrenergic receptors found in the muscles of many ... When inhaled, indacaterol reaches the receptors in the airways and activates them. This causes the muscles of the airways to ...
more infohttps://www.ema.europa.eu/en/medicines/human/EPAR/ultibro-breezhaler

Homology Modeling of Cannabinoid Receptors: Discovery of Cannabinoid Analogues for Therapeutic Use | SpringerLinkHomology Modeling of Cannabinoid Receptors: Discovery of Cannabinoid Analogues for Therapeutic Use | SpringerLink

Structure of a beta(1)-adrenergic G-protein-coupled receptor.Google Scholar ... Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography.Google Scholar ... The 2.6 Angstrom Crystal Structure of a Human A(2A) Adenosine Receptor Bound to an Antagonist. Science 322:1211-1217.PubMed ... These compounds primarily target the cannabinoid receptors 1 (CB1) and Cannabinoid receptors 2 (CB2). This chapter focuses on ...
more infohttps://link.springer.com/protocol/10.1007%2F978-1-61779-465-0_35

Er Dilaterol effektive til fedtforbrænding & Bygning magert muskelvæv?Er Dilaterol effektive til fedtforbrænding & Bygning magert muskelvæv?

It is a beta-2 adrenergic receptor antagonist. Clenbuterol also works to relax the smooth muscles of the body such as those ... It only affects the beta-2 receptor. It mimics adrenaline in that has the ability to raise the core temperature of the person ... The breaks in the cycle allow the beta-2 receptors to clear out the substance and return to their normal state. Without the ...
more infohttps://steroidly.com/da/dilaterol/

ANORO ELLIPTA 55 micrograms/22 micrograms inhalation powder, pre-dispensed - Summary of Product Characteristics (SmPC) - (eMC)ANORO ELLIPTA 55 micrograms/22 micrograms inhalation powder, pre-dispensed - Summary of Product Characteristics (SmPC) - (eMC)

Umeclidinium/vilanterol is a combination inhaled long-acting muscarinic receptor antagonist/long-acting beta2-adrenergic ... Beta-adrenergic blockers Medicinal products containing beta-adrenergic blockers may weaken or antagonise the effect of beta2- ... findings were those typically associated with the primary pharmacology of either muscarinic receptor antagonists or beta2- ... adrenergic agonists, such as vilanterol. Concurrent use of either non-selective or selective beta-adrenergic blockers should be ...
more infohttps://www.medicines.org.uk/emc/medicine/28949/SPC/Anoro+Ellipta+55+micrograms+22+micrograms+inhalation+powder+c+pre-dispensed/

Falintolol - WikipediaFalintolol - Wikipedia

Falintolol is a beta-adrenergic receptor antagonist. Conti, P; Dallanoce, C; De Amici, M; De Micheli, C; Klotz, KN (1998). " ... "Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor ... antagonists". Bioorganic & Medicinal Chemistry. 6 (4): 401-8. doi:10.1016/s0968-0896(97)10051-7. PMID 9597184. ...
more infohttps://en.wikipedia.org/wiki/Falintolol

Application # 2018/0071285. SYSTEMS PHARMACOLOGY FOR TREATING OCULAR DISORDERS - Patents.comApplication # 2018/0071285. SYSTEMS PHARMACOLOGY FOR TREATING OCULAR DISORDERS - Patents.com

... antagonists, Dopamine receptor D1 antagonists, Dopamine receptor D5 antagonists, .beta.1 adrenergic receptor antagonists, .beta ... antagonists, Dopamine receptor D1 antagonists, Dopamine receptor D5 antagonists, .beta.1 adrenergic receptor antagonists, .beta ... antagonists, Dopamine receptor D1 antagonists, Dopamine receptor D5 antagonists, .beta.1 adrenergic receptor antagonists, .beta ... antagonists, Dopamine receptor D1 antagonists, Dopamine receptor D5 antagonists, .beta.1 adrenergic receptor antagonists, .beta ...
more infohttp://patents.com/us-20180071285.html

Allergy and Asthma Proceedings: Ingenta Connect Table Of ContentsAllergy and Asthma Proceedings: Ingenta Connect Table Of Contents

Comparable effect of a leukotriene receptor antagonist and long-acting beta2-adrenergic agonist in cough variant asthma pp. e78 ... Beta2-adrenergic receptor haplotype/polymorphisms and asthma susceptibility and clinical phenotype in a Chinese Han population ...
more infohttps://www.ingentaconnect.com/content/ocean/aap/2010/00000031/00000005%3Bjsessionid=8p9u9agirk7rp.x-ic-live-02

Pharmacogenomic Evaluation of Antihypertensive Responses 2 - Full Text View - ClinicalTrials.govPharmacogenomic Evaluation of Antihypertensive Responses 2 - Full Text View - ClinicalTrials.gov

Adrenergic beta-1 Receptor Antagonists. Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... This study is aimed at determining the genetic factors that may influence a persons response to either a beta-blocker or a ... a beta-blocker (metoprolol) and a thiazide diuretic (chlorthalidone) in a sequential monotherapy design in 400 hypertensive ... Pharmacogenomic Evaluation of Antihypertensive Responses 2 (PEAR2). The safety and scientific validity of this study is the ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01203852?recr=Open&intr=%22Antihypertensive+Agents%22&rank=11

Childhood Asthma Research and Education (CARE) Network Trial - Montelukast or Azithromycin for Reduction of Inhaled...Childhood Asthma Research and Education (CARE) Network Trial - Montelukast or Azithromycin for Reduction of Inhaled...

Hormones, Hormone Substitutes, and Hormone Antagonists. Adrenergic beta-2 Receptor Agonists. Adrenergic beta-Agonists. ... or a leukotriene receptor antagonist (montelukast) will provide a steroid-sparing effect when compared to placebo as the dose ... Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. Leukotriene Antagonists. Hormone ... will be enrolled as uncontrolled and observed closely for symptoms or low peak flows for 2 weeks. The rationale for enrolling ...
more infohttps://clinicaltrials.gov/ct2/show/NCT00471809

Flestolol - WikipediaFlestolol - Wikipedia

Flestolol is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... 1. Novel .beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/ ...
more infohttps://en.wikipedia.org/wiki/Flestolol

The in Vitro Pharmacology of the Beta-Adrenergic Receptor Pet Ligand (S)-Fluorocarazolol Reveals High Affinity for Cloned Beta...The in Vitro Pharmacology of the Beta-Adrenergic Receptor Pet Ligand (S)-Fluorocarazolol Reveals High Affinity for Cloned Beta...

... since 5-HT1A receptors are expressed at very low levels outside the central nervous system. Indeed, computer simulations ... FCZ for the h5-HT1A receptor is not likely to interfere with studies of peripheral beta-adrenergic receptors, ... Interaction of the Beta Adrenergic Receptor Antagonist Bucindolol With Serotonergic Receptors SW Watts et al. J Cardiovasc ... Bucindolol is a nonselective beta-adrenergic receptor antagonist that has additional vasodilating properties. Because some beta ...
more infohttps://pubmed.ncbi.nlm.nih.gov/11512051/

Free Pharmacology Flashcards about Anxiety DisordersFree Pharmacology Flashcards about Anxiety Disorders

5-HT2 receptors hypersensitive. `. Treatment SAD 1st line SSRI or CBT. Pharmacotherapy x 10-12 weeks at max dose before ... Dec Cortisol d/t adrenal exhaustion, HPA Axis - down regulation of beta and alpha-2 adrenergic receptors, increased reactivity ... decreased receptor binding, low levels of metabolites, high incidence in Parkinsons, Emergence of SAD during antipsychotic tx. ... Reductions in central BZD receptor density FDA Approved for PD. Fluoxetine, Sertraline, Paroxetine (all SSRI effective except ...
more infohttps://www.studystack.com/flashcard-2278524

Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks.Role of adrenergic alpha-2-receptors on feeding behavior in layer-type chicks.

Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... beta-Endorphin / pharmacology. Chemical. Reg. No./Substance: 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/ ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...
more infohttp://www.biomedsearch.com/nih/Role-adrenergic-alpha-2-receptors/19233186.html

Beta blocker - WikipediaBeta blocker - Wikipedia

... beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor antagonists, beta adrenergic receptor antagonists. ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ...
more infohttps://en.wikipedia.org/wiki/Beta_blocker

Nebivolol in Patients With Systolic Stage 2 HypertensionNebivolol in Patients With Systolic Stage 2 Hypertension

A cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial ... More From BioPortfolio on "Nebivolol in Patients With Systolic Stage 2 Hypertension". *Related Companies*Related Events*Related ... Home » Topics » Adempas (riociguat) » Research » Nebivolol in Patients With Systolic Stage 2 Hypertension ... Nebivolol in Patients With Systolic Stage 2 Hypertension. 2014-08-27 03:16:21 , BioPortfolio ...
more infohttps://www.bioportfolio.com/resources/trial/68521/Nebivolol-in-Patients-With-Systolic-Stage-2-Hypertension.html

Primary polydipsia - WikipediaPrimary polydipsia - Wikipedia

... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ... 157 (2): 569-593. doi:10.1111/j.1749-6632.1969.tb12908.x. ISSN 1749-6632. Siegler EL, Tamres D, Berlin JA, Allen-Taylor L, ...
more infohttps://en.wikipedia.org/wiki/Primary_polydipsia

Pathway and mechanism of drug binding to G-protein-coupled receptors | PNASPathway and mechanism of drug binding to G-protein-coupled receptors | PNAS

1979) Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. ... 1982) Adrenergic ligand liposolubility in membranes: Direct assessment in a beta-adrenergic binding system. Mol Pharmacol 22:5- ... The three beta blockers and the beta agonist we studied all bound to the receptors along a predominant pathway involving entry ... 1975) Identification of cardiac β-adrenergic receptors by (−) [3H]alprenolol binding. Proc Natl Acad Sci USA 72:1564-1568. ...
more infohttps://www.pnas.org/content/108/32/13118

Publikationen › Department Chemie und PharmaziePublikationen › Department Chemie und Pharmazie

Development of covalent antagonists for beta 1-and beta 2-adrenergic receptors. In: Bioorganic & Medicinal Chemistry 27 (2019 ... Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias. In: Journal of Medicinal Chemistry 62 (2019), S ... Hamilton Receptor‐Mediated Self‐Assembly of Orthogonally Functionalized Au and TiO2 Nanoparticles. In: Helvetica Chimica Acta ... Conformational Complexity and Dynamics in a Muscarinic Receptor Revealed by NMR Spectroscopy. In: Molecular Cell 75 (2019), S. ...
more infohttps://www.chemie.nat.fau.de/forschung/publikationen/

Human Ultracell VHuman Ultracell V

Antianginal: Calcium antagonists - Nifedipine. *Competitive antagonist of beta 1 and beta 2 adrenergic receptors: Propranolol ... cell tissues is facilitated by the empathy developed by Biocell Laboratories between these components and the receptor proteins ... Beta-lactams, aminoglycosides, cephalosporins, macrolides. Intestinal motility regulators. Cisapride, metoclopramide, ... Beta-blockers: Atenolol, Metoprolol, Carvedilol, Bisoprolol. *Thiazide diuretics: Hydrochlorothiazide, chlorthalidone, ...
more infohttp://www.biocellmedical.com/en/human-ultracell-V/
  • G protein-coupled receptors enable cells to sense extracellular signals and translate them into physiological responses. (pnas.org)
  • In addition to a transmembrane domain that transduces signals into the cytoplasm, adhesion G protein-coupled receptors (aGPCRs) have large extracellular regions (ECRs) that interact with proteins in the extracellular space. (pnas.org)
  • In contrast, receptors from the adhesion, secretin, and frizzled/taste2 families and even some from the rhodopsin family have one or more extracellular domains ( 4 ). (pnas.org)
  • These ligands all lie buried within a deep binding pocket-the canonical "orthosteric" site that is cradled within a characteristic bundle of seven transmembrane helices-that is typically accessed from the extracellular side of the receptor. (pnas.org)
  • Adhesion G protein-coupled receptors (aGPCRs) play critical roles in diverse biological processes, including neurodevelopment and cancer progression. (pnas.org)
  • Although ECRs regulate receptor function, it is not clear whether ECRs play a direct regulatory role in G-protein signaling or simply serve as a protective cap for the activating " Stachel " sequence. (pnas.org)
  • The most sensitive receptors that regulate ventilation are. (cram.com)
  • When inhaled, indacaterol reaches the receptors in the airways and activates them. (europa.eu)
  • A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation. (patents.com)
  • Thus, (S)-FCZ may not be a suitable PET ligand for studies of central nervous system beta-adrenergic receptors unless the contribution by 5-HT1A sites can be shown to be negligible. (nih.gov)
  • 2004. Cannabinoid CB1 receptor protein expression in the rat choroid plexus: a possible involvement of cannabinoids in the regulation of cerebrospinal fluid. (springer.com)
  • The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer-type chicks. (biomedsearch.com)
  • Alpha-2 adrenergic transmission and human baroreflex regulation. (biomedsearch.com)
  • To test the effects in humans, we assessed autonomic vasomotor tone and baroreflex regulation in 9 normal young adults on 2 occasions, once with and once without clonidine. (biomedsearch.com)
  • 2006. Cannabinoid receptors as therapeutic targets for obesity and metabolic diseases. (springer.com)
  • G-protein-coupled receptors (GCPRs) represent the largest class of drug targets, and one-third of all drugs act by binding to GCPRs. (pnas.org)
  • 2. Seed cells at a density of 8000 cells/well in 100 µl of culture medium. (bio-medicine.org)
  • 2007. Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: Safety, tolerability, and therapeutic potential. (springer.com)
  • For live-cell receptor internalization studies, an enhanced version of this dye, CypHer5E, has been developed (3). (bio-medicine.org)
  • We captured this pharmaceutically critical process in atomic detail using the first unbiased molecular dynamics simulations in which drug molecules spontaneously associate with G-protein-coupled receptors to achieve final poses matching those determined crystallographically. (pnas.org)
  • Surprisingly, association with this vestibule, at a distance of 15 Å from the binding pocket, often presents the largest energetic barrier to binding, despite the fact that subsequent entry into the binding pocket requires the receptor to deform and the drug to squeeze through a narrow passage. (pnas.org)
  • Our atomic-level description of the binding process suggests opportunities for allosteric modulation and provides a structural foundation for future optimization of drug-receptor binding and unbinding rates. (pnas.org)
  • The young people at highest risk of long-term social disability present with emerging signs of social decline, buying cialis in usa in association with low level psychotic symptoms, emotional and behavioural disorder, and often accompanied by substance misuse problems and risk of harm to self and others [ 1, 2]. (jewelrymaison.com)