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.

Functional and molecular biological evidence for a possible beta3-adrenoceptor in the human detrusor muscle. (1/193)

The possible existence of a beta3-adrenergic receptor (beta3-AR) in the human detrusor muscle was investigated by in vitro functional studies and analysis of mRNA expression. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of the human detrusor. The rank order for their relaxing potencies was isoprenaline (pD2 6.37+/-0.07) > or = noradrenaline (pD2 6.07+/-0.12) > or = adrenaline (pD2 5.88< or =0.11). Neither dobutamine (beta1- and beta2-AR agonist) nor procaterol (beta2-AR agonist) produced any significant relaxation at concentrations up to 10(-5) M. BRL37344A, CL316243 and CGP-12177A (beta3-AR agonists), relaxed the preparations significantly at concentrations higher than 10(-6) M. The pD2 values for BRL37344A, CL316243 and CGP-12177A were 6.42+/-0.25, 5.53+/-0.09 and 5.74+/-0.14, respectively. CGP-20712A (10(-7) - 10(-5) M), a beta1-AR antagonist, did not affect the isoprenaline-induced relaxation. On the other hand, ICI-118,551, a beta2-AR antagonist, produced a rightward parallel shift of the concentration-relaxation curve for isoprenaline only at the highest concentration used (10(-5) > M) and its pKB value was 5.71+/-0.19. Moreover, SR58894A (10(-7) - 10(-5) M), a beta3-AR antagonist, caused a rightward shift of the concentration-relaxation curve for isoprenaline in a concentration-dependent manner. The pA2 value and slope obtained from Schild plots were 6.24+/-0.20 and 0.68+/-0.31. The beta1-, beta2- and beta3-AR mRNAs were all positively expressed in detrusor smooth muscle preparations in a reverse transcription polymerase chain reaction assay. In conclusion, the present results provide the first evidence for the existence of the beta3-AR subtype in the human detrusor. They also suggest that the relaxation induced by adrenergic stimulation of the human detrusor is mediated mainly through beta3-AR activation.  (+info)

Inotropic and sympathetic responses to the intracoronary infusion of a beta2-receptor agonist: a human in vivo study. (2/193)

BACKGROUND: On the basis of the presence of beta2-receptors within the sympathetic nervous system, beta2-stimulation may increase cardiac sympathetic outflow. We addressed the hypothesis that sympathoexcitatory beta2-receptors are present in the human left ventricle. METHODS AND RESULTS: The beta2-agonist salbutamol was infused into the left coronary artery in 3 groups of patients: group 1 (n=9, no beta-blocker therapy), group 2 (n=7, beta1-selective blockade with atenolol), and group 3 (n=6, nonselective beta-blockade with nadolol). Left ventricular +dP/dt in response to increasing concentrations of salbutamol was measured in all groups, and cardiac norepinephrine spillover was measured in group 1. There were no systemic hemodynamic changes in any group. Salbutamol resulted in a 44+/-6% increase in +dP/dt in group 1, a 25+/-6% increase in group 2 (P<0.05 versus group 1), and no increase in group 3. Salbutamol also resulted in a 124+/-37% increase in cardiac norepinephrine spillover in group 1 (P<0.05). CONCLUSIONS: Evidence that salbutamol increased norepinephrine release from cardiac sympathetic nerves was provided by the observations that atenolol suppressed the salbutamol inotropic response, demonstrating that this response was mediated in part by beta1-receptors and that salbutamol also resulted in an increase in cardiac norepinephrine spillover. This result provides in vivo evidence, in humans, for the role of sympathoexcitatory cardiac beta2-receptors.  (+info)

Modulation of the pacemaker current If by beta-adrenoceptor subtypes in ventricular myocytes isolated from hypertensive and normotensive rats. (3/193)

OBJECTIVE: Both beta 1- and beta 2-adrenoceptors (beta 1-AR and beta 2-AR) are functionally present in human and rat ventricular myocytes. The two receptor subtypes are differently regulated during the development of myocardial hypertrophy and failure. I(f) is expressed in human and rat ventricular myocytes. In hypertrophied myocytes isolated from old spontaneously hypertensive rats (SHR) the density is much larger than in age-matched normotensive Wistar Kyoto (WKY). Due to the possible relevance of I(f) as an arrhythmogenic mechanism in the rat and human ventricle, we studied and compared the effects of beta 1-AR and beta 2-AR stimulation on I(f) in both hypertrophied and normal left ventricular myocytes of 18-month old SHR and WKY. METHODS: The whole-cell configuration of the patch-clamp technique was employed. Noradrenaline (NA, 1 microM) was used to stimulate beta 1-AR and isoprenaline (ISO, 1 microM) in the presence of the beta 1-AR antagonist CGP 20712A (0.1 microM) to stimulate beta 2-AR. RESULTS: In SHR, NA increased I(f) by causing a 10.8 +/- 0.9 mV (n = 10) positive shift in the voltage of maximal activation (V1/2); this effect was completely reversed by CGP 20712A. beta 2-AR stimulation was effective in seven out of 13 cells tested, where it caused a small positive shift in V1/2 (4.0 +/- 1.7 mV). Cyclopentyladenosine (CPA), a selective A1-receptor agonist, reversed the effect of NA; the antiadrenergic action of CPA was abolished in cells pre-incubated with pertussis toxin (PTX) to block inhibitory G proteins (Gi). In PTX-treated cells the shift in V1/2 caused by both beta 2-AR (9.6 +/- 1.7 mV, n = 6, p < 0.05) and beta 1-AR (17.6 +/- 1.9 mV, n =7, p < 0.05) was significantly greater than in control cells. Both beta-AR subtypes modulated I(f) activation also in WKY: beta 1-AR shifted V1/2 by 16.0 +/- 1.4 mV (n = 15) and beta 2-AR by 4.2 +/- 1.1 mV (n = 7). However, in PTX-treated WKY cells only the beta 2-AR effect was potentiated (shift in V1/2: 11.4 +/- 1.4 mV, n = 9, p < 0.01), while the beta 1-AR response was unchanged (18.9 +/- 4.2 mV, n = 5, n.s.). CONCLUSIONS: I(f) expressed in SHR hypertrophied ventricular myocytes is modulated by catecholamines mainly through the stimulation of the beta 1-AR subtype. The beta 1-AR response is, however, significantly lower than that observed in myocytes from normotensive rats, probably as a consequence of the presence of an increased inhibitory activity of Gi proteins. This post-receptorial control may be seen as a mechanism to limit the arrhythmogenicity of beta-AR stimulation in myocardial hypertrophy and failure.  (+info)

Isoeugenolol: a selective beta1-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties. (4/193)

Isoeugenolol (1.0, 3.0, 5.0 mg/kg, i.v.) produced a dose-dependent bradycardia and a decrease in blood pressure in anesthetized Wistar rats. Isoeugenolol inhibited the tachycardia effects induced by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by (-)phenylephrine. In isolated guinea pig tissues, isoeugenolol antagonized (-)isoproterenol-induced positive inotropic and chronotropic effects on the atria and tracheal relaxations in a concentration-dependent manner. The apparent pA2 values for isoeugenolol on right atria, left atria and trachea were 7.63+/-0.03, 7.89+/-0.12 and 6.12+/-0.05, respectively, indicating that isoeugenolol was a highly selective beta1-adrenoceptor blocker. On the other hand, isoeugenolol produced a mild direct cardiac depression at high concentration and was without intrinsic sympathomimetic activity (ISA). In isolated rat thoracic aorta, isoeugenolol relaxed more potently the contractions induced by (-)phenylephrine (10 microM) and 5-HT (10 microM) than those by high K+ (75 mM). In isolated guinea pig trachea, isoeugenolol attenuated the carbachol (1 microM)-con-tracted trachea more significantly than those contracted with high K+. Furthermore, the binding characteristics of isoeugenolol and various beta-adrenoceptor antagonists were evaluated in [3H]CGP-12177 binding to rat ventricle, lung and interscapular brown adipose tissue (IBAT) membranes. The -log IC50 values of isoeugenolol for predominate beta1-, beta2- and beta3-adrenergic receptor sites were 5.82+/-0.09, 4.74+/-0.05 and 4.73+/-0.12, respectively. In conclusion, isoeugenolol was found to be a highly selective beta1-adrenoceptor antagonist with tracheal and vascular smooth muscle relaxant activities, but was devoid of alpha-adrenoceptor-blocking action.  (+info)

Dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization. (5/193)

The use of dobutamine as selective beta(1)-adrenoceptor agonist in in vivo studies on human thermogenesis and lipid utilization was investigated in 20 men. At 2.5, 5, and 10 microg x kg(-1) x min(-1), dobutamine induced significant increases in energy expenditure, lipid oxidation, and lipolysis. The beta(1)-adrenoceptor antagonist atenolol (bolus: 42.5 microg/kg, infusion: 1.02 microg x kg(-1) x min(-1)) blocked all dobutamine-induced effects on thermogenesis and lipid utilization. All parameters remained at levels comparable to those during saline infusion. The dose of atenolol used did not inhibit beta(2)-adrenoceptor-specific changes in energy expenditure, lipid oxidation, and lipolysis during salbutamol infusion (85 ng x kg(-1) x min(-1)). This indicates that atenolol was specific for beta(1)-adrenoceptors and did not camouflage concomitant beta(2)-adrenoceptor stimulation during dobutamine infusion. Therefore, we conclude that dobutamine can be used as a selective beta(1)-adrenoceptor agonist at dosages +info)

Selective beta1-adrenoceptor blockade enhances the activity of the stimulatory G-protein in human atrial myocardium. (6/193)

1. Chronic selective beta1-adrenoceptor (beta1AR) blocker treatment enhances the sensitivity of beta2-adrenoceptor (beta2AR) in human heart (Hall et al., 1990; 1991). To clarify the mechanism of the cross-sensitization between beta1AR and beta2AR, we determined whether the stimulatory G-protein (G(s)alpha) function is increased in atria from beta1AR-blocker treated patients compared with non-beta-blocked patients, and investigated whether this change is caused by an alteration of post-translational modification of Gsalpha protein. 2. G(s)alpha function was determined by reconstitution of human atrial G(s)alpha into S49 cyc- cell membranes. In the reconstitution system, GTPgammaS stimulated cyclic AMP generation in a dose-dependent manner. Upon 10(-4) M GTPgammaS stimulation, G(s)alpha activity in the beta1AR-blocker, atenolol, treated group (78.2+/-10. 3 pmol cyclic AMP mg(-1) min(-1) 10(-3)) was 65% higher than that in non-beta-blocked patients (47.3+/-6.3 pmol cyclic AMP mg(-1) min(-1) 10(-3), n=15, P=0.02). 3. Isoelectric point (pI) valu G(s)alpha were measured by two dimensional gel electrophoresis (2D-E) and the amount of each isoform quantified by image analysis of a Western blot of the gel using specific antibody. Multiple isoforms of G(s)alpha were detected by 2D-E with different pI values. There were no significant differences between the groups of patients in either pI values or the proportions of the acidic isoforms of G(s)alpha to the main basic form (n=12, P>0.05). 4. The results suggest that chronic beta1AR-blockade enhances Gsalpha function in human atrium, and this may account in part for the hypersensitivity of beta2AR and other Gs-coupled receptors during beta1AR-blockade. The increased G(s)alpha function is unlikely to be caused directly by blockade of protein kinase A phosphorylation of G(s)alpha protein.  (+info)

Antisense inhibition of beta(1)-adrenergic receptor mRNA in a single dose produces a profound and prolonged reduction in high blood pressure in spontaneously hypertensive rats. (7/193)

BACKGROUND: beta-Blockers are the first line of therapy for hypertension. However, they are associated with side effects because of central nervous system (CNS) effects and beta(2)-adrenergic antagonism. To overcome these problems and provide a long-term beta(1)-blockade, antisense oligonucleotides against rat beta(1)-adrenergic receptor (beta(1)-AR) mRNA (beta(1)-AS-ODN) were designed and tested for the ability to inhibit cardiac beta(1)-ARs as well as lower blood pressure in spontaneously hypertensive rats (SHRs). METHODS AND RESULTS: Radioligand binding assay showed that a single intravenous injection of beta(1)-AS-ODN delivered in cationic liposomes significantly decreased cardiac beta(1)-AR density by 30% to 50% for 18 days (P<0.01), with no effect on beta(2)-ARs. This was accompanied by marked attenuation of beta(1)-AR-mediated positive inotropic response in isolated perfused hearts in vitro (P<0.02) and in conscious SHRs monitored by telemetry in vivo (P<0.02). Furthermore, the blood pressure of SHRs was reduced for 20 days, with a 38 mm Hg maximum drop. Heart rate was not significantly decreased. Quantitative autoradiography was performed to assess beta(1)-AS-ODN effects on the CNS, which demonstrated no changes in beta(1)-ARs in brain, in contrast to a significant reduction in heart and kidney (P<0.05). For comparison with beta-blockers, the effects of atenolol on cardiovascular hemodynamics were examined, which lowered blood pressure for only 10 hours and elicited appreciable bradycardia in SHRs. CONCLUSIONS: These results indicate that beta(1)-AS-ODN, a novel approach to specific beta(1)-blockade, has advantages over currently used beta-blockers in providing a profound and prolonged reduction in blood pressure without affecting heart rate, beta(2)-ARs, and the CNS. Diminished cardiac contractility resulting from less beta(1)-AR expression contributes to the antihypertensive effect.  (+info)

Negative inotropic effects of isoprenaline on isolated left atrial assays from aged transgenic mice with cardiac over-expression of human beta(2)-adrenoceptors. (8/193)

The action of isoprenaline has been evaluated in an isolated, left atrial assay, from aged transgenic mice with cardiac-specific over-expression of the beta(2)-adrenoceptor. In the assay, isoprenaline produced a negative inotropic concentration-response curve that was not altered by incubation with CGP-20712A (1 microM), a beta(1)-adrenoceptor antagonist. However, after incubation with ICI-118,551 (300 nM), a selective beta(2)-adrenoceptor antagonist, isoprenaline produced a positive inotropic concentration-effect curve that was located to the left of the negative inotropic curve. This suggests that the negative inotropic effect was mediated by a homogenous population of negatively-coupled beta(2)-adrenoceptors. In the presence of CGP-20712A (300 nM), the positive curve was shifted to the right, suggesting that the positive inotropic effect was mediated, at least in part, by beta(1)-adrenoceptors. These results differ substantially from those previously obtained in young transgenic mice. An outline of an explanatory model, based on a concept of over-expressed receptors 'stealing' G-proteins, is suggested.  (+info)

Aims: The effects of a beta blocker, especially an ultra-short acting selective beta blocker, such as landiolol hydrochloride on the organ protection in sepsis are unclea..
Ultrasonic longitudinal displacements, delivered to the distal tips of small diameter wire waveguides, are known to be capable of disrupting complicated atherosclerotic plaques during vascular interventions. These ultrasonic displacements can disrupt plaques not only by direct contact ablation but also by pressure waves, associated cavitation, and acoustic streaming developed in the surrounding blood and tissue cavities. The pressure waves developed within the arterial lumen appear to play a major role but are complex to predict as they are determined by the distal tip output of the wire waveguide (both displacement and frequency), the geometric features of the waveguide tip, and the effects of biological fluid interactions. This work describes a numerical linear acoustic fluid-structure model of an ultrasonic wire waveguide and the blood surrounding the distal tip. The model predicts a standing wave structure in the wire waveguide, including stresses and displacements, and requires the ...
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Similar to the scenario in neonatal rat cardiomyocytes, β1-AR stimulation with isoproterenol induces a robust increase in cAMP accumulation that is associated with an increase in the amplitude and an acceleration of the kinetics of both the calcium transient and the twitch in adult rat ventricular myocytes. In contrast, only rather high concentrations of the β2-AR agonist zinterol (10-5 mol/L) modulate contractile function in adult rat ventricular myocytes (Figure 2⇑). Parenthetically, 2 laboratories have presented data to support the theoretical argument that 10-5 mol/L zinterol (in the absence of a β1-AR blocker) acts as a mixed β1-/β2-AR agonist; β2-AR selectivity is achieved only if a β1-AR blocker (such as CGP 20712A) is included in the assay.11 73 In contrast, Xiao and Lakatta74 maintain that the effects of high concentrations of zinterol (even without a β1-AR blocker) are attributable entirely to the minor population of β2-ARs in the preparation, and they present results to ...
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Sprawdź ile zapłacisz za lek Bisoprolol Actavis (Bidop) w aptece, znajdź tańsze zamienniki leku. Określ swoje uprawnienia i sprawdź jakie zniżki Ci przysługują.
Script error: No such module TemplatePar.Expression error: Unexpected , operator. Landiolol (INN) is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent. ...
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First, before I forget, extreme nausea can be a symptom that heart failure is worsening. Personally, though, Id expect it to become progressively worse, not to come rampaging out of nowhere the way it did - I still suspect Nebivolol was the culprit. I will, however, bear it in mind and keep a close eye…
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For both pied flycatchers and blackcaps, our data obtained under the stationary sky can best be explained by Hypothesis 3. Birds use the stars as a compass only, and this compass most likely is based on geometrical recognition of star patterns learned during ontogeny, and therefore seems independent of celestial rotation and time later in life.. The pied flycatchers clearly oriented in more or less the normal migratory direction all night, even though the stars were stationary. No clear change in direction towards the end of the night, as would be expected if they had been performing true star navigation, was observed (Hypothesis 1a-c). In other words, they did not seem to perceive any longitudinal displacement during the night. Also, there was no gradual change in orientation consistent with a time-compensated star compass (Hypothesis 2).. The data on the blackcaps are less clearcut, probably because of the relatively low sample size (N=7). The data appear to show a turn towards the west in the ...
Takotsubo syndrome (TTS), also known as broken heart syndrome, is a severe and acute heart failure syndrome that often resolves spontaneously but can also be associated with significant mortality. TTS predominantly affects post-menopausal women and is usually triggered by identifiable physical or emotional stress. Considerable evidence suggests the precipitating factor to be the catecholamine surge from excess sympathetic activity that occurs during these events because it can be mimicked by exogenous catecholamine administration (1). TTS was first described in 1990 in Japan (2), when the shape formed by an akinetic left ventricular apex with hyperkinetic basal segments was compared to a Japanese Octopus pot, or takotsubo.. The importance of catecholamines in the induction of TTS has since been robustly demonstrated in vivo in preclinical rodent models. A number of groups have used these models to investigate the pathophysiology of TTS, including how the direct catecholaminergic myocardial ...
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The pivotal stage of atherogenesis is antigen presentation by macrophages to T lymphocytes. This antigen could be a fragment of oxidized LDL"digested" by macrophage, heat shock protein 60, β2 glycoprotein I, or fragments of bacterial antigens. During interaction between these cells, an immunological response of type T helper 1 (cellular) or T helper 2 (humoral) arises. Th1 response and its mediators: (IFN-γ, TNF-α, interleukin 1, interleukin 12, and interleukin 18) increase atherogenesis, whereas Th2 response and its mediators: (interleukin 4, interleukin 5, and interleukin 10) decrease the development of atherosclerosis. The concept of atherosclerosis as an inflammatory disease is quite fresh; however, it is already considered an undisputable achievement of science, bringing particular therapeutic consequences ...
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Migliore farmacia Per ordinare Zebeta Bisoprolol senza ricetta. Zebeta Generico (Bisoprololo) è usato nel trattamento dell ipertensione. Bisoprololo è un beta-bloccante. Agisce su alcune componenti chimiche che causano la diminuzione del battito cardiaco e diminuiscono la capacità di pompare sangue da parte del cuore. ...
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Metoprolol is a beta-blocker that affects the heart and circulation (blood flow through arteries and veins). Metoprolol is used to treat angina (chest
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Nebivolol is administered as a racemic mixture of equal proportions of "d" and "l" isomers. Nebivolol has 4 asymmetric centres, d-isomer refers to (S,R,R,R)-nebivolol and l-isomer to (R,S,S,S)-nebivolol. Antihypertensive effects of nebivolol appear to be greater with both isomers than with the d-isomer alone. Nebivolol exhibits greater degree of beta 1/beta 2-receptor selectivity compared with other commonly used beta-blockers.. The selectivity of Nebivolol on the beta 1-adrenergic receptor is 321-fold higher than for beta 2-adrenergic receptor. Conventional beta blockers are associated with unfavorable effects on metabolic parameters. Nebivolol has favorable metabolic profile, with no deleterious effect on insulin sensitivity which may result from its agonistic activity on the beta 3 adrenoreceptor. This beta blocker exhibits anti-proliferative and antioxidant properties [7].. The efficacy and tolerability of nebivolol have been evaluated in comparison with placebo and other beta-blockers ...
Higenamine is a tetrahydroisoquinoline present in several plants that has β-adrenergic receptor agonist activity. Study of the biosynthesis of higenamine has shown the participation of norcoclaurine synthase, which controls the stereochemistry to construct the (S)-isomer. However, when isolated from nature, higenamine is found as the racemate, or even the (R)-isomer. We recently reported the isolation of higenamine 4′-O-β-d-glucoside. Herein, its (R)- and (S)-isomers were synthesized and compared to precisely determine the stereochemistry of the isolate. Owing to their similar spectral properties, determination of the stereochemistry based on NMR data was considered inappropriate. Therefore, a high-performance liquid chromatography method was established to separate the isomers, and natural higenamine 4′-O-β-d-glucoside was determined to be a mixture of isomers.
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This study is an 18-week study to evaluate the tolerability of nebivolol compared to metoprolol ER in outpatients with mild to moderate hypertension taking HCTZ. It is a multi-center, randomized, double blind (DB), active-control, parallel-group study, starting with a 4-week HCTZ run-in phase, followed by a 12-week DB treatment phase. Patients meeting the entry criteria at the end of run-in are randomized to one of two treatment groups, nebivolol or metoprolol ER. Uptitration of dose of study drug will occur if needed during the first 4 weeks of the DB phase, after which there is an 8-week stable-dose period of treatment. A 2-week double-blind withdrawal phase follows, during which tapering off study drug occurs ...
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What is this medicine? BISOPROLOL (bis OH proe lol) is a beta-blocker. Beta-blockers reduce the workload on the heart and help it to beat more regularly.
... Zebeta is a beta-blocker which is used to treat high blood pressure (hypertension) by blocking the action of certain natural chemicals in your body such as epinephrine on the heart and blood vessels.
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.
Aug 27, 2012. Sandrone G, Mortara A, Torzillo D, La Rovere MT, Malliani A, Lombardi F. Effects of beta blockers atenolol or metoprolol on heart
Pro-Bisoprolol: Bisoprolol belongs to the class of medications called beta-blockers. Beta-blockers reduce the workload of the heart and help it to beat more regularly by blocking the effects of certain hormones. Bisoprolol is used alone and in combination with other medications to control mild to moderate high blood pressure but does not cure the condition.
Pro-Bisoprolol: Bisoprolol belongs to the class of medications called beta-blockers. Beta-blockers reduce the workload of the heart and help it to beat more regularly by blocking the effects of certain hormones. Bisoprolol is used alone and in combination with other medications to control mild to moderate high blood pressure but does not cure the condition.
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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 ...
... is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/jm00374a013. PMID ... 1-dimethylethylenediamine with urea, gives flestolol (5). Quon, CY; Stampfli, HF (1993). "Biochemical characterization of ... the ester 3. Reaction of that intermediate with amine 4, obtained by reaction of 1, ...
... is a beta-adrenergic selective antagonist tagged by radioisotopic iodine. Pindolol Ezrailson, E. G.; Garber, A. J ... A new beta adrenergic receptor probe". Journal of cyclic nucleotide research. 7 (1): 13-26. PMID 6265511. ...
... a family of G-protein-coupled receptors. Muscarinic toxins can be either receptor agonists or receptor antagonists, and in some ... 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". ... Novel Antagonists of Nicotinic Acetylcholine Receptors from Snake Venom". ACS Chemical Biology. 10 (12): 2805-2815. doi:10.1021 ...
"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 ...
Labetalol (koristi se za hipertenziju; it is a mixed alpha/beta adrenergic antagonist)[4] ... adrenergički receptor je G protein-spregnuti receptor koji vezuje Gq heterotrimerni G protein. Postoje tri visoko homologna ... Adrenergički receptor. Literatura[уреди]. *↑ Woodman OL, Vatner SF (1987). „Coronary vasoconstriction mediated by α1- and α2- ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
"Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes". ...
Beta blockers) β1-selective antagonists include: Acebutolol (in hypertension, angina pectoris and arrhythmias) Atenolol (in ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with ... "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by ... and beta 2-adrenergic receptors: structurally and functionally related receptors derived from distinct genes". Trends in ...
... denotes selective antagonist to the receptor. Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... binds the beta 2-adrenergic receptor via the receptor cytoplasmic Arg-329 to Leu-413 domain and provides a mobile scaffold ...
... stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ... It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... a novel agonist at peripheral dopamine receptors and beta 2-adrenoceptors". British Journal of Pharmacology. 85 (3): 599-608. ...
... 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 ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ... β3-adrenergic receptors are located in fat cells.[6] Beta receptors are found on cells of the heart muscles, smooth muscles, ...
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... "Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
... carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular ... Wellstein A, Palm D, Belz GG (1986). "Affinity and selectivity of beta-adrenoceptor antagonists in vitro". J. Cardiovasc. ... and beta 2-adrenergic receptors" (PDF). Cardiovasc Drugs Ther. 13 (2): 123-6. doi:10.1023/A:1007784109255. PMID 10372227.. ... and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ventricular myocardium". ...
... beta _{2}} . The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert ... See also receptor antagonist) α 2 {\displaystyle \alpha _{2}} receptors. Agonists of α 2 {\displaystyle \alpha _{2}} receptors ... beta _{2}} receptors. Agonism of β 2 {\displaystyle \beta _{2}} receptors causes vasodilation and low blood pressure (i.e. the ... receptors in the vascular smooth muscle cells). Usage of β 2 {\displaystyle \beta _{2}} receptor agonists as hypotensive agents ...
Non-selective beta blockers are known to facilitate bronchospasm as well. Beta blockers bind into the β2 receptors and block ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... beta blockers (used to treat hypertension), a paradoxical result of using LABA drugs (to treat COPD) and other drugs. ...
... also known as β-Adrenergic receptor kinase 2 [BARK1]) and arrestin 2 (also known as Arrestin beta 1 [ARRB1]). These agents act ... Asapiprant (S-555739) and Laropiprant are selective receptor antagonists of DP1 whereas Vidupiprant is a receptor antagonist ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ... is primarily a receptor for prostaglandin D2 (PGD2). The receptor is a member of the Prostaglandin receptors belonging to the ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... Tsai BS, Yellin TO (1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic antidepressants ... Kanba S, Richelson E (1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain ... It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ...
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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 ...
... is a beta adrenergic receptor antagonist. Ban, T; Sada, S; Takahashi, Y; Sada, H; Fujita, T (1985). "Effects of para- ... substituted beta-adrenoceptor blocking agents and methyl-substituted phenoxypropanolamine derivatives on maximum upstroke ...
As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... The block on alpha-2 receptors further potentiates beta-effects, increasing cardiac output. Phenoxybenzamine has a long-lasting ... Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ...
... is a beta adrenergic receptor antagonist. Mahé, N; Do, B; Nicolaï, B; Rietveld, IB; Barrio, M; Tamarit, JL; Céolin, ...
... 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 ...
... 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 ...
Straube T, Frey JU (2003). "Involvement of beta-adrenergic receptors in protein synthesis-dependent late long-term potentiation ... an antagonist to the NMDA receptor, which prevented LTP in this pathway.[24] Conversely, LTP in the mossy fiber pathway is NMDA ... β-adrenergic receptor agonists such as norepinephrine may alter the protein synthesis-dependent late phase of LTP.[51] Nitric ... "Selective impairment of learning and blockade of long-term potentiation by an N-methyl-D-aspartate receptor antagonist, AP5". ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine then acting on lipolysis-inducing beta receptors.. Muscle mass[edit]. Males typically have more skeletal muscle ...
Receptor Antagonists BETA BLOCKING AGENTS CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Bevantolol is a beta- ... AGENTS CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Anti-Arrhythmia Agents A beta-adrenergic antagonist that ... BETA BLOCKING AGENTS CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Adrenergic beta-1 Receptor Antagonists A ... BETA BLOCKING AGENTS CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Adrenergic beta-1 Receptor Antagonists A ...
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Adrenergic Antagonists. Antihypertensive Agents. Vasodilator Agents. Adrenergic beta-1 Receptor Agonists. Adrenergic beta- ... Effects of the Novel Beta-adrenergic Antagonist Nebivolol (Bystolic) on Prehypertensive Subjects at Genetic Risk of ... Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. Physiological ... or allergy to any beta blocker therapy or may have contraindications to beta blocker therapy such as asthma, bradycardia, etc. ...
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This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)- ... Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. ... Agonist or antagonistBy similarity. 1. ,p>The ,a href="http://www.geneontology.org/">Gene Ontology (GO),/a> project provides a ... alpha-2A adrenergic receptor binding Source: MGI. *beta1-adrenergic receptor activity Source: MGI ,p>Inferred from Direct Assay ...
Comparison of Adrenergic Beta-receptor Antagonists in Angina Pectoris Br Med J 1973; 1 :138 ... Comparison of Adrenergic Beta-receptor Antagonists in Angina Pectoris. Br Med J 1973; 1 doi: https://doi.org/10.1136/bmj.1.5846 ... that metabolic breakdown products are probably of therapeutic importance only in so far as they antagonize beta-receptor ... Published 20 January 1973) Cite this as: Br Med J 1973;1:138 ... Comparison of Adrenergic Beta-receptor Antagonists in Angina ...
antagonist. Details. DB00335. Atenolol. approved. yes. antagonist. Details. DB00373. Timolol. approved. yes. antagonist. ... Beta-1 adrenergic receptor. P08588. Details. Drug Relations. Drug Relations. DrugBank ID. Name. Drug group. Pharmacological ... Beta-1 adrenergic receptor. Details. Name. Beta-1 adrenergic receptor. Kind. protein. Organism. Human. Polypeptides. Name. ...
0 (Adrenergic beta-3 Receptor Agonists); 0 (Adrenergic beta-3 Receptor Antagonists); 0 (Enzyme Inhibitors); 0 (RNA, Messenger ... 0 (Adrenergic beta-Antagonists); 0 (Propanolamines); 67P356D8GH (Acebutolol); 820484N8I3 (Histamine); DRB57K47QC (Celiprolol); ... Dopamine receptor agonists.iii. Dopamine receptor antagonists.iv. Dopamine-depletor drugs.v. Drugs that increase the production ... 0 (Receptors, Adrenergic, beta-3); 0 (Vasodilator Agents); 31C4KY9ESH (Nitric Oxide); DRB57K47QC (Celiprolol); EC 1.14.13.39 ( ...
Info Adrenergic Antagonists. * Info Adrenergic beta-3 Receptor Antagonists. * Info Adrenergic beta-Antagonists ... 3-(2-Ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate View Synonyms. View Structure. ... 1 result for Category equals ADRENERGIC BETA-3 RECEPTOR ANTAGONISTS. Property. Value. ...
10 results for Category equals ADRENERGIC BETA-1 RECEPTOR ANTAGONISTS Info. Please enable JavaScript in your browser. Row ...
For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E, ... used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor ... Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been ... Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000 ...
"Potent and selective human beta(3)-adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes". ...
Labetalol (koristi se za hipertenziju; it is a mixed alpha/beta adrenergic antagonist)[4] ... adrenergički receptor je G protein-spregnuti receptor koji vezuje Gq heterotrimerni G protein. Postoje tri visoko homologna ... Adrenergički receptor. Literatura[уреди]. *↑ Woodman OL, Vatner SF (1987). „Coronary vasoconstriction mediated by α1- and α2- ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Adrenergic Antagonists); 0 (Propanolamines); 0 (Receptors, Adrenergic, beta); 0NM31M53PW (Butoxamine); 42200-33-9 (Nadolol); ... 0 (Adrenergic Antagonists); 0 (Antidepressive Agents); 0 (Benzazepines); 0 (Dopamine Antagonists); 0 (Receptors, Adrenergic); 0 ... 0 (Adrenergic Antagonists); 0 (Catecholamines); 0 (Receptors, Adrenergic); 0 (TRPV Cation Channels); 0 (Trpv1 protein, rat); ... 0 (Adrenergic Antagonists); 0 (Carbazoles); 0 (Piperazines); 0 (Receptors, Adrenergic, alpha-1); 0P2197HHHN (carbazole). ...
2015 Oct 1;121(19):3444-51. doi: 10.1002/cncr.29392. Epub 2015 Aug 24. Multicenter Study; Research Support, N.I.H., Extramural ... Adrenergic beta-Antagonists. Grant support. *CA109298/CA/NCI NIH HHS/United States ... The median OS based on beta-blocker receptor selectivity was 94.9 months for those receiving nonselective beta-blockers versus ... and the remaining patients were receiving nonselective beta antagonists. The primary indication for beta-blocker use was ...
Helping you find trustworthy answers on Alpha Adrenergic Antagonist , Latest evidence made easy ... Find all the evidence you need on Alpha Adrenergic Antagonist via the Trip Database. ... A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to ... adrenergic fibers, Beta Adrenergic Receptors are one of two major classes of adrenergic receptors (alpha and beta) based on ...
Beta-adrenergic antagonist:. 1. Beta adrenergic receptor blockade improves?. 2. Mechanisms for doing this? ... 3. Beta agonist: stimulates the heart, can be used short term. 4. Amrinone potentiates dobutamine --, additional stimulation ... Beta blockers improve overall prognosis and ventricular function. 2. They do this (above) by reducing potential for sudden ... 1. decrease in stroke volume. 2. Increased stroke volume; Bc the curve is flattened there is a decrease in LVEDP with only a ...
Antagonist for aldosterone receptor 17 Which family of drugs contain ephedrine Increased release and direct adrenergic receptor ... What type of receptor is used to transmit interleukin 2-10,15 ... Alpha and Beta agonists 64 What type of receptor is used to ... Heart block (increased AV node conduction) (M2 antagonist). Cholinergic poisoning (organophosphates and AChE inhibators) (M1 ...
A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and ... 07/01/1982 - "Acebutolol, a relatively cardioselective beta-adrenergic blocking drug, was administered to 20 men with coronary ... 07/01/1984 - "The hemodynamic dose-response effects of intravenous acebutolol, a cardioselective beta-adrenoceptor antagonist ... A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and ...
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 ...
Beta-2 adrenergic receptor, inactive state, dimer. 2rh1. Homo sapiens. Eukaryo. plasma. 2. 14. 31.8 ± 0.9. 0 ± 1. -143.2. ... Adenosine receptor A2a, complex with antagonist. 3uza. Homo sapiens. Eukaryo. plasma. 1. 7. 31.6 ± 0.6. 8 ± 1. -72.5. ... Beta-2 adrenergic receptor, active state, complex with antibody. 3p0g. Homo sapiens. Eukaryo. plasma. 1. 7. 30.1 ± 1.4. 9 ± 1. ... Beta-2 adrenergic receptor, active state, complex with G-protein. 3sn6. Homo sapiens. Eukaryo. plasma. 1. 7. 31.0 ± 1.6. 8 ± 1 ...
A critical role for beta cell M3 muscarinic acetylcholine receptors in regulating insulin release and blood glucose homeostasis ... adrenergic receptor stimulation. J Cell Biol. 2010;189(3):573-587.. View this article via: PubMed CrossRef Google Scholar ... Isoform-specific antagonists of exchange proteins directly activated by cAMP. Proc Natl Acad Sci U S A. 2012;109(45):18613- ... Loss of Lkb1 in adult beta cells increases beta cell mass and enhances glucose tolerance in mice. Cell Metab. 2009;10(4):285- ...
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- ... Receptors, Adrenergic, alpha-2 / agonists, antagonists & inhibitors, physiology*. Yohimbine / pharmacology. beta-Endorphin / ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ...
Key words: Adrenergic beta-antagonists; Vasodilator agents; Arterial pressure; Pulse wave analysis; Hypertension ... adrenergic receptor antagonist that relaxes vascular smooth muscle by nitric oxide-and cyclic GMP-dependent mechanisms. Nitric ... Nebivolol: a third-generation beta-adrenergic blocker. Ann Pharmacother. 2006;40(7-8):1353-60. [ Links ] ... Effect of beta blockers on central aortic pressure in African-Americans. J Am Soc Hypertens. 2011;5(2):94-101. [ Links ] ...
  • Clinical pharmacology studies have demonstrated beta-blocking activity by showing (1) reduction in heart rate and cardiac output at rest and on exercise, (2) reduction of systolic and diastolic blood pressure at rest and on exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. (neurolex.org)
  • title=Molecular pharmacology and modeling of vasopressin receptors. (enacademic.com)
  • The beta-adrenergic antagonist ligand (+/-)-[125I] iodocyanopindolol binds to 2 X 10(5) receptors per purified adult rat cardiomyocyte, with a dissociation constant of 70 pM. (ahajournals.org)
  • Isoprenaline has higher affinity for β 1 than adrenaline , which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. (worldheritage.org)
  • Isoprenaline has higher affinity for β 1 than noradrenaline , which, in turn, binds with higher affinity than adrenaline . (enacademic.com)
  • Amelio AL, McAnany PK, Bloom DC (2006) A chromatin insulator-like element in the herpes simplex virus type 1 latency-associated transcript region binds CCCTC-binding factor and displays enhancer-blocking and silencing activities. (springer.com)
  • ICI binds to the β 2 subtype with at least 100 times greater affinity than β 1 or β 3 , the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
  • In biochemistry , a receptor is a protein on the cell membrane or within the cytoplasm or cell nucleus that binds to a specific molecule (a ligand ), such as a neurotransmitter , hormone , or other substance, and initiates the cellular response to the ligand. (chemeurope.com)
  • Not every ligand that binds to a receptor also activates the receptor. (chemeurope.com)
  • This study examined the characteristics and distribution of sarcolemmal and light vesicular beta-adrenergic receptors (BAR) in left ventricular myocardium from 15 adults (aged 17 to 58 years) without left ventricular dysfunction or coronary artery disease and 29 patients (aged 14 to 53 years) with end-stage congestive heart failure (CHF). (semanticscholar.org)
  • Other studies found an interaction between ACE inhibitors and the ACE insertion/deletion (I/D) polymorphism, which resulted in differences in AT(1) receptor mRNA expression, left ventricular hypertrophy and arterial stiffness between different genetic variants. (uu.nl)
  • CONCLUSIONS: Enalaprilat attenuates beta-adrenergic contractility and enhances left ventricular distensibility in patients with DCM, but not in subjects with normal left ventricular function. (elsevier.com)
  • The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it. (wikipedia.org)
  • Ehlers-Danlos Syndrome, Vascular Type, also known as eds iv , is related to ehlers-danlos syndrome and aortic aneurysm , and has symptoms including hemoptysis An important gene associated with Ehlers-Danlos Syndrome, Vascular Type is COL3A1 (Collagen Type III Alpha 1 Chain), and among its related pathways/superpathways are Integrin Pathway and Phospholipase-C Pathway . (malacards.org)
  • Quantitative analyses indicated that ICP0 expression was blocked using HSV-1/TRβ1 for infection during T 3 washout, suggesting that overexpression of TRβ1 is likely to delay its inhibitory effect on viral gene expression. (springer.com)
  • Bedadala GR, Pinnoji RC, Hsia SC (2007) Early growth response gene 1 (Egr-1) regulates HSV-1 ICP4 and ICP22 gene expression. (springer.com)
  • Bedadala GR et al (2010) Thyroid hormone controls the gene expression of HSV-1 LAT and ICP0 in neuronal cells. (springer.com)
  • 2014) A novel thyroid hormone mediated regulation of HSV-1 gene expression and replication is specific to neuronal cells and associated with disruption of chromatin condensation. (springer.com)
  • With regard to blood pressure response, interactions were found between genetic polymorphisms for endothelial nitric oxide synthase and diuretics, the alpha-adducin gene and diuretics, the alpha-subunit of G protein and beta-adrenoceptor antagonists, and the ACE gene and angiotensin II type 1 (AT(1)) receptor antagonists. (uu.nl)
  • Also, drug-gene interactions between calcium channel antagonists and ACE I/D polymorphism regarding arterial stiffness have been reported. (uu.nl)
  • and (ii) at least one nitric oxide enhancing compound, wherein the patient has at least one polymolphism in a beta 1 adrenergic receptor gene. (patentsencyclopedia.com)
  • 2. The method of claim 1, wherein the at least one polymorphism in the beta 1 adrenergic receptor gene is an Arg389Arg polymorphism and/or a Gly389Gly polymorphism in the beta 1 adrenergic receptor gene. (patentsencyclopedia.com)
  • 3. The method of claim 1, wherein the patient has at least one polymorphism in the endothelial nitric oxide synthase (NOS3) gene and/or at least one polymorphism in an aldosterone synthase promoter gene. (patentsencyclopedia.com)
  • These receptors often can enter the cell nucleus and modulate gene expression in response to the activation by the ligand. (chemeurope.com)
  • Bisoprolol je kardioprotektivni lijek jer selektivno i kompetitivno blokira kateholaminsku (adrenalinsku) stimulaciju β 1 adrenergičkih receptora (adrenoreceptora), koji se uglavnom nalaze u ćelijama srčanog mišića i provodnom tkivu srca (kardiospecifičan), ali također i u jukstaglomerularnim ćelijama bubrega . (wikipedia.org)
  • Recently, a +9/-9 exon 1 polymorphism of the B2BKR was shown to be strongly associated with LV growth response among normotensive males undergoing physical training. (diva-portal.org)
  • Accumulating evidence suggests that stress-induced sympathetic nervous system (SNS) activation of β-adrenergic receptor signaling may play a role in the regulation of various cancer types including pancreatic cancer ( 4-7 ). (aacrjournals.org)
  • Regional differences in the beta receptor densities were found for the atria and ventricles and for the areas within the left ventricle in cats with no coronary occlusion and dilevalol or saline. (biomedsearch.com)