Adrenergic alpha 2 receptor agonists. Medical search

A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.

A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.

Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.

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.

Drugs that bind to and activate dopamine receptors.

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.

Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.

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

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

Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.

Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.

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

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.

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.

Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.

One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.

Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.

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.

Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.

Drugs that selectively bind to and activate alpha adrenergic receptors.

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.

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.

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.

Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.

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.

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)

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.

A selective D1 dopamine receptor agonist used primarily as a research tool.

Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.

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

Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.

A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.

Drugs that bind to and activate adrenergic receptors.

A dopamine D2/D3 receptor agonist.

A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

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).

Drugs that bind to and activate excitatory amino acid receptors.

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.

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

Compounds with BENZENE fused to AZEPINES.

A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.

A family of hexahydropyridines.

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.

An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.

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.

Drugs that selectively bind to and activate beta-adrenergic receptors.

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

A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.

A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.

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.

A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.

Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.

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.

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)

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.

One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.

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.

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.

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

A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.

An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.

Drugs that bind to and activate cholinergic receptors.

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/319)

The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors. (+info)

Role of potassium channels in the antinociception induced by agonists of alpha2-adrenoceptors. (2/319)

1. The effect of the administration of pertussis toxin (PTX) as well as modulators of different subtypes of K+ channels on the antinociception induced by clonidine and guanabenz was evaluated in the mouse hot plate test. 2. Pretreatment with pertussis toxin (0.25 microg per mouse i.c.v.) 7 days before the hot-plate test, prevented the antinociception induced by both clonidine (0.08-0.2 mg kg(-1), s.c.) and guanabenz (0.1-0.5 mg kg(-1), s.c.). 3. The administration of the K(ATP) channel openers minoxidil (10 microg per mouse, i.c.v.), pinacidil (25 microg per mouse, i.c.v.) and diazoxide (100 mg kg(-1), p.o.) potentiated the antinociception produced by clonidine and guanabenz whereas the K(ATP) channel blocker gliquidone (6 microg per mouse, i.c.v.) prevented the alpha2 adrenoceptor agonist-induced analgesia. 4. Pretreatment with an antisense oligonucleotide (aODN) to mKv1.1, a voltage-gated K+ channel, at the dose of 2.0 nmol per single i.c.v. injection, prevented the antinociception induced by both clonidine and guanabenz in comparison with degenerate oligonucleotide (dODN)-treated mice. 5. The administration of the Ca2+-gated K+ channel blocker apamin (0.5-2.0 ng per mouse, i.c.v.) never modified clonidine and guanabenz analgesia. 6. At the highest effective doses, none of the drugs used modified animals' gross behaviour nor impaired motor coordination, as revealed by the rota-rod test. 7. The present data demonstrate that both K(ATP) and mKv1.1 K+ channels represent an important step in the transduction mechanism underlying central antinociception induced by activation of alpha2 adrenoceptors. (+info)

Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/319)

The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory. (+info)

Cardiopulmonary effects of the alpha2-adrenoceptor agonists medetomidine and ST-91 in anesthetized sheep. (4/319)

To test the hypothesis that pulmonary alterations are more important than hemodynamic changes in alpha2-agonist-induced hypoxemia in ruminants, the cardiopulmonary effects of incremental doses of (4-[1-(2,3-dimethylphenyl)ethyl]-1H-imadazole) hydrochloride (medetomidine; 0.5, 1.0, 2.0, and 4 micrograms/kg) and 2-(2, 6-diethylphenylamino)-2-imidazol (ST-91; 1.5, 3.0, 6.0, and 12 micrograms/kg) were compared in five halothane-anesthetized, ventilated sheep using a placebo-controlled randomized crossover design. Pulmonary resistance (RL), dynamic compliance, and tidal volume changes in transpulmonary pressure (DeltaPpl) were determined by pneumotachography, whereas cardiac index (CI), mean pulmonary artery pressure (Ppa), and pulmonary artery wedge pressure (Ppaw) were determined using thermodilution and a Swan-Ganz catheter. The most important finding was the fall in partial pressure of oxygen in arterial blood (PaO2) after administration of medetomidine at a dose (0.5 micrograms/kg) 20 times less than the sedative dose. The PaO2 levels decreased to 214 mm Hg as compared with 510 mm Hg in the placebo-treated group. This decrease in PaO2 was associated with a decrease in dynamic compliance and an increase in RL, DeltaPpl, and the intrapulmonary shunt fraction without changes in heart rate, CI, mean arterial pressure, pulmonary vascular resistance, Ppa, or Ppaw. On the other hand, ST-91 only produced significant changes in PaO2 at the highest dose. After this dose of ST-91, the decrease in PaO2 was accompanied by a 50% decrease in CI and an increase in mean arterial pressure, Ppa, Ppaw, and the intrapulmonary shunt fraction without significant alterations of RL and DeltaPpl. The study suggests that the mechanism(s) by which medetomidine and ST-91 produce lower PaO2 are different and that drug-induced alterations in the pulmonary system are mainly responsible for the oxygen-lowering effect of medetomidine. (+info)

The alpha2A-adrenergic receptor discriminates between Gi heterotrimers of different betagamma subunit composition in Sf9 insect cell membranes. (5/319)

In view of the expanding roles of the betagamma subunits of the G proteins in signaling, the possibility was raised that the rich diversity of betagamma subunit combinations might contribute to the specificity of signaling at the level of the receptor. To test this possibility, Sf9 cell membranes expressing the recombinant alpha2A-adrenergic receptor were used to assess the contribution of the betagamma subunit composition. Reconstituted coupling between the receptor and heterotrimeric Gi protein was assayed by high affinity, guanine nucleotide-sensitive binding of the alpha2-adrenergic agonist, [3H]UK-14,304. Supporting this hypothesis, the present study showed clear differences in the abilities of the various betagamma dimers, including those containing the beta3 subtype and the newly described gamma4, gamma10, and gamma11 subtypes, to promote interaction of the same alphai subunit with the alpha2A-adrenergic receptor. (+info)

Effect of strenuous, acute exercise on alpha2-adrenergic agonist-potentiated platelet activation. (6/319)

Vigorous exercise transiently increases the risk of primary cardiac arrest. Strenuous, acute exercise can also increase the release of plasma epinephrine. Previous investigations have indicated that epinephrine can potentiate platelet activation by activating platelet alpha2-adrenoceptors. This study investigated how strenuous, acute exercise affects alpha2-adrenergic agonist-potentiated platelet activation by closely examining 15 sedentary men who exercised strenuously on a bicycle ergometer. Before and immediately after exercise, platelet adhesiveness on fibrinogen-coated surfaces, [Ca2+]i in platelets, the number and affinity of alpha2-adrenergic sites on the platelet surface, and plasma catecholamine levels were determined. The results of this study can be summarized as follows: (1) The affinity of alpha2-adrenergic receptors on platelets decreases while the maximal binding number significantly increases after strenuous exercise, thereby correlating with the rise in plasma catecholamine levels. (2) Basal, clonidine-treated, ADP-treated, and clonidine plus ADP-treated adhesiveness and [Ca2+]i in platelets increased after strenuous exercise. (3) Strenuous exercise is associated with higher percentages of ADP- and clonidine plus ADP-enhanced platelet adhesiveness and [Ca2+]i than at rest. (4) The synergistic effects of clonidine on ADP-enhanced platelet adhesiveness and [Ca2+]i after strenuous exercise are much greater than those at rest. Therefore, we conclude that strenuous, acute exercise enhances platelet activation, possibly by altering the performance of platelet alpha2-adrenergic receptors, facilitating the ability of ADP-activated fibrinogen receptors, and enhancing fibrinogen binding to platelet fibrinogen receptors. (+info)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (7/319)

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters. (+info)

Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. (8/319)

alpha2-Adrenergic receptor (AR)-selective compounds produce antihypertensive and antinociceptive effects. Moxonidine alleviates hypertension in multiple species, including humans. This study demonstrates that intrathecally administered moxonidine produces antinociception in mice. Antinociception was detected via the (52.5 degrees C) tail-flick and Substance P (SP) nociceptive tests. Moxonidine was intrathecally administered to ICR, mixed C57BL/6 x 129/Sv [wild type (WT)], or C57BL/6 x 129/Sv mice with dysfunctional alpha2aARs (D79N-alpha2a). The alpha2AR-selective antagonist SK&F 86466 and the mixed I1/alpha2AR-selective antagonist efaroxan were tested for inhibition of moxonidine-induced antinociception. Moxonidine prolonged tail-flick latencies in ICR (ED50 = 0.5 nmol; 0. 3-0.7), WT (0.17 nmol; 0.09-0.32), and D79N-alpha2a (0.32 nmol; 0. 074-1.6) mice. Moxonidine inhibited SP-elicited behavior in ICR (0. 04 nmol; 0.03-0.07), WT (0.4 nmol; 0.3-0.5), and D79N-alpha2a (1.1 nmol; 0.7-1.7) mice. Clonidine produced antinociception in WT but not D79N-alpha2a mice. SK&F 86466 and efaroxan both antagonized moxonidine-induced inhibition of SP-elicited behavior in all mouse lines. SK&F 86466 antagonism of moxonidine-induced antinociception implicates the participation of alpha2ARs. The comparable moxonidine potency between D79N-alpha2a and WT mice suggests that receptors other than alpha2a mediate moxonidine-induced antinociception. Conversely, absence of clonidine efficacy in D79N-alpha2a mice implies that alpha2aAR activation enables clonidine-induced antinociception. When clinically administered, moxonidine induces fewer side effects relative to clonidine; moxonidine-induced antinociception appears to involve a different alpha2AR subtype than clonidine-induced antinociception. Therefore, moxonidine may prove to be an effective treatment for pain with an improved side effect profile. (+info)

"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... Agonists (activators) of the α2-adrenergic receptor are frequently used in anaesthesia where they affect sedation, muscle ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ...

https://en.wikipedia.org/wiki/Alpha-2_adrenergic_receptor

... an α2A adrenergic receptor agonist. Medetomidine, an α2 adrenergic agonist. Nonspecific agonists act as agonists at both alpha- ... Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of ... but there was an increased incidence of hypotension and bradycardia Alpha blocker Adrenergic agonist Beta-adrenergic agonist ...

https://en.wikipedia.org/wiki/Alpha-adrenergic_agonist

... is an α2-adrenergic receptor agonist. Fox K, Dargie HJ, de Bono DP, Oliver MF, Wülfert E, Kharkevitch T (September ... Alpha-2 adrenergic receptor agonists, Imidazoles, Salicylamides, All stub articles, Organic compound stubs). ... agonist (mivazerol) on limiting myocardial ischaemia in stable angina". Heart. 82 (3): 383-5. doi:10.1136/hrt.82.3.383. PMC ...

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

This is because adrenergic stimulation by agonists results in normal calcium channel regulation. If these adrenergic receptors ... Adrenergic receptor Alpha blocker Antagonist Beta blocker List of adrenergic drugs Propanolol Sympathetic nervous system ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located ...

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

The DRD4 receptor is a G protein-coupled receptor that inhibits adenylyl cyclase. The DRD4-7R mutation results in a wide range ... Medications used include stimulants, atomoxetine, alpha-2 adrenergic receptor agonists, and sometimes antidepressants. In those ... 12 The majority of studies on nicotine and other nicotinic agonists as treatments for ADHD have shown favorable results; ... The 7 repeat variant of dopamine receptor D4 (DRD4-7R) causes increased inhibitory effects induced by dopamine and is ...

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

The Alpha-1 agonist prazosin could be effective for PTSD. The Alpha-2 agonists clonidine and guanfacine have demonstrated both ... Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... Buspirone (Buspar) is a 5-HT1A receptor agonist used to treated generalized anxiety disorder. If an individual has taken a ... Phenibut is a GABAB receptor agonist, as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels ( ...

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

"Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and ... Adrenergic receptor Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular ... alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1- ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...

https://en.wikipedia.org/wiki/Alpha-1_adrenergic_receptor

Alpha-1 adrenergic receptor agonists, Alpha-2 adrenergic receptor agonists, Antihypertensive agents, Beta-adrenergic agonists, ... converts alpha-methyldopamine into alpha-methylnorepinephrine, which is an agonist of the presynaptic α2-adrenergic receptor ... Methyldopa acts on alpha-2 adrenergic receptors, which are found on the pre synaptic nerve terminal. This inhibits the ... Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication. It works by stimulating the brain to decrease ...

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

The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... alpha-1 receptors. Under NE binding alpha-1 receptors cause vasoconstriction ( contraction of the vascular smooth muscle cells ... Agonists of alpha-2 receptors in the vascular smooth muscle lead to vasoconstriction. However, in clinical practice drugs ... Antagonists of alpha-1 receptors (doxazosin, prazosin) cause vasodilation (a decrease in vascular smooth muscle tone with ...

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

... is a sulfonamide α1-adrenergic receptor agonist. MacLean MR, Thomson M, Hiley CR (June 1989). "Pressor effects of the alpha 2- ... Alpha-1 adrenergic receptor agonists, Phenylethanolamines, Sulfonamides, All stub articles, Cardiovascular system drug stubs). ... adrenoceptor agonist B-HT 933 in anaesthetized and haemorrhagic rats: comparison with the haemodynamic effects of amidephrine ... 97 (2): 419-32. doi:10.1111/j.1476-5381.1989.tb11969.x. PMC 1854522. PMID 2569342. v t e (Articles with short description, ...

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

BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... SD, True TA, Rimele TJ, Saussy DL (January 1995). "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors ... 272 (2-3): R5-6. doi:10.1016/0014-2999(94)00751-R. PMID 7713154. v t e (Articles with short description, Short description ...

https://en.wikipedia.org/wiki/BMY-7378

Alpha-1 adrenergic receptor agonists, Alpha-2 adrenergic receptor agonists, Chloroethyl compounds, Imidazolines, Nitrogen ... Chloroethylclonidine is an irreversible agonist for adrenergic receptors, in particular alpha1B, D, C and alpha2A/D-subtypes. ... Docherty JR, O'Rourke M (February 1997). "The alpha-adrenoceptor-mediated actions of chloroethylclonidine". General ... 28 (2): 197-201. doi:10.1016/s0306-3623(96)00187-5. PMID 9013194. v t e (Drugs not assigned an ATC code, Articles with changed ...

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

... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... alpha-2A-, receptor". Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors ...

https://en.wikipedia.org/wiki/Alpha-2A_adrenergic_receptor

Zolpidem, a GABA-A receptor agonist and "Z-hypnotic" medication, has shown some efficacy in treating insomnia due to cannabis ... Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with ... Baclofen, a GABA-B receptor agonist and antispasmodic medication, has been found to reduce cravings but without a significant ... Buspirone, a serotonin 1A receptor (5-HT1A) agonist, has shown limited efficacy for treating anxiety in people with cannabis ...

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

... a Nonstimulant Selective Alpha(2A)-Adrenergic Receptor Agonist For Attention-Deficit/Hyperactivity Disorder". P & T. 35 (8): ... Guanfacine is a highly selective agonist of the α2A adrenergic receptor, with low affinity for other receptors. However it may ... MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors". The Journal of Pharmacology and ... Arnsten AF (October 2010), "The use of α2A adrenergic agonists for the treatment of attention-deficit/hyperactivity disorder", ...

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

... receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic ... like receptor and alpha(1)/alpha(2)-adrenoceptor". J Pharmacol Exp Ther. 303 (2): 805-14. doi:10.1124/jpet.102.039875. PMID ... Bromocriptine is a partial agonist of the dopamine D2 receptor. It also interacts with other dopamine receptors and with ... This is in contrast to other ergolines acting instead as 5-HT2B receptor agonists such as cabergoline and pergolide but is ...

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

... barbiturates and Alpha-adrenergic agonists, such as clonidine. Conversely, coadministration of NMDA-antagonists with alpha-2 ... In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are ... Karl Jansen, Ketamine: Dreams and Realities (2004) NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J ... The work of his team indicated that N-P receptors must be blocked for at least 2 hours to cause reversible changes, and at ...

https://en.wikipedia.org/wiki/Olney's_lesions

... is an agonist at the α-2A, 2B, and 2C adrenergic receptor subtypes, with the highest activity at the alpha-2A ... It is an α2A adrenergic receptor agonist. It was approved for use by the Food and Drug Administration in the United States in ... Lofexidine is structurally analogous to clonidine, another α2 adrenergic receptor agonist used for treatment of opioid ... atoms on the phenyl ring are necessary for lofexidine's agonism at the α2a adrenergic receptor subtype; removal of either ...

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

... (pronounced GWAHN-a-benz, sold under the trade name Wytensin) is an alpha agonist that is selective to the alpha-2 ... adrenergic receptor. Guanabenz is used as an antihypertensive drug, i.e. to treat high blood pressure (hypertension). The most ... Alpha-2 adrenergic receptor agonists, Chloroarenes, Guanidines, All stub articles, Antihypertensive agent stubs). ... 2 (3): S543-6. PMID 6599714.[permanent dead link] v t e (All articles with dead external links, Articles with dead external ...

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

Beta2-adrenergic agonist Alpha-adrenergic agonist Asthma Beta blocker Beta-1 adrenergic receptor Beta-2 adrenergic receptor ... It also influences the specificity for the β-receptor subtypes. Direct-acting analog binds the β-adrenergic receptors directly ... β1 receptors make up to 75% of all beta receptors and are predominantly located in the heart. β2 receptors are found in ... β-receptors are membrane-bound receptors coupled to G-proteins. Three types of β-receptors have been identified by molecular ...

https://en.wikipedia.org/wiki/Discovery_and_development_of_beta2_agonists

Mu-opioid receptor agonists, Phenols, Semisynthetic opioids, World Health Organization essential medicines, Wikipedia medicine ... "Simultaneous treatment of hypertension and opiate withdrawal using an alpha 2 adrenergic agonist". J Natl Med Assoc. 75 (1): 89 ... Hydromorphone is believed to work by activating opioid receptors, mainly in the brain and spinal cord. Hydromorphone 2 mg IV is ... Hydromorphone is a semi-synthetic μ-opioid agonist. As a hydrogenated ketone of morphine, it shares the pharmacologic ...

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

1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors". Journal of Medicinal Chemistry. 37 (15): 2328-33. doi:10.1021/ ... 1992). "Resolution and adrenergic activities of the optical isomers of 4-[1-(1-naphthyl)ethyl]-1H-imidazole". Chirality. 4 (7 ... January 2004). "Medetomidine analogs as selective agonists for the human alpha2-adrenoceptors". Biochemical Pharmacology. 67 (1 ... Like other alpha-2 agonists, it produces sedative and muscle relaxant effects but without producing respiratory depression. It ...

https://en.wikipedia.org/wiki/4-NEMD

... a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice". The Journal of ... Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of ... Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). This receptor subtype is found in both the ... moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. In contrast, clonidine ...

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

... that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor ... It appears to be unique among cannabinoid compounds by also having high affinity and activity at alpha-2 adrenergic receptors ... Although general effects of its use as a dietary supplement remain undefined, the potent activity of cannabigerol at alpha-2 ... adrenergic receptors raises concerns about its safety for human consumption, possibly having unintended effects, such as ...

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

... alpha adrenergic receptor - alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - alpha-MSH - Ames test - amide - amine - amino - amino ... beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta-thromboglobulin - ...

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

Alpha-1 adrenergic receptor agonists, Alpha-2 adrenergic receptor agonists, Beta-adrenergic agonists, Cardiac stimulants, ... adrenaline and some phenylephrine derivatives on alpha-, beta- and beta- adrenergic receptors". South African Medical Journal ... suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much ... These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. Nusser E, Donath H, Russ W (August 1965 ...

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

... is an α2 adrenergic agonist. α2 agonists, through the activation of a G protein-coupled receptor, inhibit the ... Alpha-2 adrenergic receptor agonists, Imidazolines, Organobromides, Ophthalmology drugs, Quinoxalines, Wikipedia medicine ... Peripheral α2 agonist activity results in vasoconstriction of blood vessels (as opposed to central α2 agonist activity that ... The increased uveoscleral outflow from prolonged use may be explained by increased prostaglandin release due to α adrenergic ...

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

Alpha-1 adrenergic receptor agonists, Alpha-2 blockers, Cyclopropyl compounds, Imidazolines, Phenol ethers, All stub articles, ... Cirazoline is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, ... Ruffolo, R. R. Jr.; Waddell, J. E. (1982). "Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist ... Arnsten, A.F.T.; Jentsch, J.D. (September 1997). "The Alpha-1 Adrenergic Agonist, Cirazoline, Impairs Spatial Working Memory ...

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

Alpha-1 adrenergic receptor agonists, Alpha-2 adrenergic receptor agonists, Beta-adrenergic agonists, D1-receptor agonists, D2- ... It acts on D1 and α-adrenergic receptors as an agonist. Ibopamine was first prepared by Casagrande and co-workers. Instilled at ... After being hydrolysed to epinine, ibopamine is able to stimulate the alpha-adrenergic and D1 dopaminergic receptors, thereby ... The epinine, an analogue of dopamine, can stimulate dopamine receptors and to a lesser degree adrenergic receptors. Thus it is ...

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

... is a potent α2 adrenergic agonist. When xylazine and other α2 adrenergic receptor agonists are administered, they ... Alpha-2 adrenergic receptor agonists, Analgesics, Equine medications, Thiazines). ... It is an analog of clonidine and an agonist at the α2 class of adrenergic receptor. In veterinary anesthesia, xylazine is often ... Yohimbine, an α2 adrenergic receptor antagonist, has been used to decrease glucose levels to a healthy level. In clinical ...

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

Alpha2-adrenergic agonists, such as brimonidine and apraclonidine, work by a dual mechanism, decreasing aqueous humor ... Less-selective alpha agonists, such as epinephrine, decrease aqueous humor production through vasoconstriction of ciliary body ... Topical beta-adrenergic receptor antagonists, such as timolol, levobunolol, and betaxolol, decrease aqueous humor production by ... Prostaglandin agonists work by opening uveoscleral passageways. Beta-blockers, such as timolol, work by decreasing aqueous ...

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

... the dopamine D2 receptor, and the α1-adrenergic receptor. The weak antiserotonergic effects of hydroxyzine likely underlie its ... Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action ... Alpha-1 blockers, Antiemetics, Anxiolytics, Belgian inventions, D2 antagonists, Ethers, H1 receptor antagonists, ... identification of 4-methylhistamine as the first potent and selective H4 receptor agonist". The Journal of Pharmacology and ...

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

... while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of ... rabbits respond to alpha and beta MSH's (therefore not using the ACTH receptor), and guinea pigs responding to both ACTH and ... the receptor is glycosylated and expressed on the cell plasma membrane. MCR's have both endogenous agonists and antagonists. α- ... ACTH receptors are the shortest of the melanocortin receptor family and are the smallest known G-coupled receptors. Both human ...

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

In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is ... Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be ... Martin SW, Broadley KJ (May 1995). "Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade". Br ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ...

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

... has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... and dopamine D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and ... Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug ...

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

5-HT1A agonists, Adrenergic receptor modulators, Alpha-2 blockers, Aminotetralins, D1-receptor agonists, D2-receptor agonists, ... D5 receptor (Ki = 5.4 nM) α1A-adrenergic receptor (Ki = 176 nM) α1B-adrenergic receptor (Ki = 273 nM) α2A-adrenergic receptor ( ... α2B-adrenergic receptor (Ki = 27 nM) α2C-adrenergic receptor (Ki = 135 nM) 5-HT1A receptor (Ki = 30 nM) 5-HT7 receptor (Ki = 86 ... D3 receptor agonists, D4 receptor agonists, D5 receptor agonists, Phenols, Thiophenes). ...

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

Dual effects of yohimbine, rauwolscine and corynanthine as alpha-adrenoceptor antagonists and 5-HT-receptor agonists". Naunyn- ... Corynanthine acts as an α1-adrenergic and α2-adrenergic receptor antagonist with approximately 10-fold selectivity for the ... and rauwolscine which have around 30-fold higher affinity for the α2-adrenergic receptor over the α1-adrenergic receptor. As a ... Alpha-1 blockers, Alpha-2 blockers, Antihypertensive agents, Tryptamine alkaloids, Indoloquinolizines, Quinolizidine alkaloids) ...

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

... binds to α2-adrenergic receptor and imidazoline receptor binding sites, and blocks NMDA receptors and other cation ... Nicotinic, imidazoline I1 and I2, α2-adrenergic (no intrinsic activity-neither agonist nor antagonist), glutamate NMDAr, and ... Pineda, J.; Ruiz-Ortega, J. A.; Martín-Ruiz, R.; Ugedo, L. (1996-11-22). "Agmatine does not have activity at alpha 2- ... while agmatine binds to α2-adrenergic receptors, it exerts neither an agonistic nor antagonistic effect on these receptors, ...

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

Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ... Phenoxybenzamine also has irreversible antagonist/weak partial agonist properties at the serotonin 5-HT2A receptor. Due to its ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ...

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

In general, treatment often begins with an alpha-1 adrenergic receptor antagonist medication such as tamsulosin, which reduces ... GnRH receptor agonists, such as leuprorelin and goserelin, were subsequently developed and used to treat prostate cancer. ... This is often done through the use of GnRH analogues or agents that block the receptors that androgens act at, such as ... or male chronic pelvic pain syndrome is treated by a large variety of modalities including the medications alpha blockers, ...

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

It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been ... shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the ... January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences. 32 (4): 355-63. doi:10.1016 ... H1 receptor antagonists, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor antagonists, Tetracyclic ...

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

As of 2018, prazosin is the only alpha-1 blocker known to act as an inverse agonist at all alpha-1 adrenergic receptor subtypes ... Alpha-1 adrenergic receptors are present in vascular smooth muscle, the central nervous system, and other tissues. When alpha ... Alpha-1 blockers have no effect on renin release or cardio output. Alpha-1 blocker, blocks alpha receptors and it relaxes the ... Alpha-1 blockers (also called alpha-adrenergic blocking agents or alpha-1 antagonists) constitute a variety of drugs that block ...

https://en.wikipedia.org/wiki/Alpha-1_blocker

... adrenergic receptor on the response to regular use of albuterol in asthma" (PDF). American Journal of Respiratory and Critical ... caused by alpha-adrenoceptor downregulation and desensitization. The mechanism may specifically include receptor ... Inhalation of an agonist for the beta-2 adrenergic receptor, such as salbutamol (albuterol in the US), is the most common ... The control of the operation, in general, involves interaction of a stimulus molecule with a receptor/enzyme subsystem by, ...

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

They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ... Alpha-2 blockers, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor antagonists). ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ...

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

Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ... Iprindole also lacks significant alpha-blocking properties, and hence does not pose a risk of orthostatic hypotension. In ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ...

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

Dopamine binds to alpha-1 and beta-1 adrenergic receptors. Mediated through myocardial beta-1 adrenergic receptors, dopamine ... Dopamine agonists, Vasoconstrictors, Inotropic agents, World Health Organization essential medicines, Wikipedia medicine ... dopamine mainly triggers dopamine receptors and β1-adrenergic receptors while at high doses it works via α-adrenergic receptors ... Alpha-1 adrenergic receptor stimulation on vascular smooth muscle, leads to vasoconstriction and results in an increase in ...

https://en.wikipedia.org/wiki/Dopamine_(medication)

Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 20 (2): 375-385. doi:10.1093/schbul/20.2.375. PMID 8085139.{{cite journal}}: CS1 maint: multiple names: authors list (link) ...

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

... adrenergic agonists MeSH D27.505.519.625.050.100.100 - adrenergic alpha-agonists MeSH D27.505.519.625.050.100.200 - adrenergic ... estrogen receptor modulators MeSH D27.505.696.399.450.360.315 - estrogen antagonists MeSH D27.505.696.399.450.360.315.300 - ... adrenergic agonists MeSH D27.505.696.577.050.100.100 - adrenergic alpha-agonists MeSH D27.505.696.577.050.100.200 - adrenergic ... beta-agonists MeSH D27.505.519.625.050.200 - adrenergic antagonists MeSH D27.505.519.625.050.200.100 - adrenergic alpha- ...

https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D27)

5-Alpha-reductase inhibitor Angiotensin II receptor antagonist ACE inhibitor Alpha-adrenergic agonist Beta blocker Cholinergic ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs used to treat ... PPAR agonist) and mode of action (reducing blood triglycerides), and that are used to prevent and treat the same disease ( ...

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

... an adrenergic alpha-agonist, or an antihistamine nasal spray without risk of rhinitis medicamentosa. Nasal saline irrigation (a ... Kamekura R, Kojima T, Takano K, Go M, Sawada N, Himi T (2012). "The Role of IL-33 and Its Receptor ST2 in Human Nasal ... Th2 cells contribute to the body's inflammatory response to allergens, and specific ST2 receptors, also known as IL1RL1, on ... Another study focusing on Han Chinese children found that certain SNPs in the protein tyrosine phosphatase non-receptor 22 ( ...

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

Ephedrine Pseudoephedrine Adrenergic receptor Alpha adrenergic agonist List of adrenergic drugs Siegel, George J; et al. (2006 ... the adrenergic receptors). Directly acting adrenergic agonists act on adrenergic receptors. All adrenergic receptors are G- ... An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of ... Agonists of each class of receptor elicit these downstream responses. Indirectly acting adrenergic agonists affect the uptake ...

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

However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Recombinant activated protein C (drotrecogin alpha) was originally introduced for severe sepsis (as identified by a high APACHE ... There are four families of PRRs: the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I- ... This forced receptor interaction induces the production of pro-inflammatory chemical signals (cytokines) by T-cells. There are ...

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

2007). "Synergistic effect of PGD2 via prostanoid DP receptor on TNF-alpha-induced production of MCP-1 and IL-8 in human ... also known as β-Adrenergic receptor kinase 2 [BARK1]) and arrestin 2 (also known as Arrestin beta 1 [ARRB1]). These agents act ... "Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ...

https://en.wikipedia.org/wiki/Prostaglandin_DP1_receptor

Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. Implications of ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. Implications of ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. Implications of ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. Implications of ...

https://molpharm.aspetjournals.org/content/28/5/475/tab-article-info

Mark Walker, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Ophthalmology, American ... Beta-adrenergic blockers. Class Summary. These agents reduce elevated and normal intraocular pressure, with or without glaucoma ... Alpha 2-adrenergic agonists. Class Summary. These can decrease intraocular pressure by decreasing aqueous production. ... Selective alpha 2-receptor that reduces aqueous humor formation and increases uveoscleral outflow. ...

https://emedicine.medscape.com/article/1193218-medication

Human PIVs (HPIVs) are currently divided into 5 serotypes-HPIV-1, HPIV-2, HPIV-3, HPIV-4a, and HPIV-4b-in 2 different genera: ... Respirovirus (HPIV-1 and HPIV-3) and Rubulavirus (HPIV-2 and HPIV-4). ... Racemic epinephrine solution causes alpha-adrenergic receptor-mediated vasoconstriction of edematous tissues, thereby reversing ... Alpha/Beta Agonists. Class Summary. When delivered by air or oxygen-powered devices, epinephrine is directly delivered to ...

https://www.medscape.com/answers/224708-179733/which-medications-in-the-drug-class-corticosteroids-are-used-in-the-treatment-of-human-parainfluenza-viruses-hpiv-and-other-parainfluenza-viruses

... alpha(2)) and post-junctional (alpha(1)) adrenoceptor agonist prop … ... Receptors, Adrenergic, alpha / drug effects* Actions. * Search in PubMed * Search in MeSH ... Hypotensive and sedative effects of alpha-adrenoceptor agonists: relationship to alpha 1- and alpha 2-adrenoceptor potency D P ... Hypotensive and sedative effects of alpha-adrenoceptor agonists: relationship to alpha 1- and alpha 2-adrenoceptor potency D P ...

https://www.ncbi.nlm.nih.gov/pubmed/6113864

Receptors, Adrenergic, alpha-1/agonists. Adrenergic alpha-1 Receptor Agonists. Receptors, Adrenergic, alpha-1 /antagonists & ... Receptors, Adrenergic, beta-1/agonists. Adrenergic beta-1 Receptor Agonists. Receptors, Adrenergic, beta-1/antagonists & ... Receptors, Adrenergic, beta-3/agonists. Adrenergic beta-3 Receptor Agonists. Receptors, Adrenergic, beta-3/antagonists & ...

https://www.nlm.nih.gov/pubs/techbull/nd10/nd10_entry_combo_table.html

Alpha-1 & alpha-2 adrenergic receptor agonist; may reduce acqueous humor formation ... 2. This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.. ... Place one finger at the corner of your eye (near the nose) and apply gentle pressure for 1 to 2 minutes. This will prevent the ... Contraindicated (2)apraclonidine, linezolid. Mechanism: unknown. Contraindicated. Contraindicated in mfr. prescribing info.. ...

http://reference.medscape.com/drug/iopidine-apraclonidine-343591

Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRF R1, CRF R2; ... Molecular targets for which radioligands (agonist, antagonist, allosteric modulator) are needed include, but are not limited to ... neurokinin receptors: NK1, NK2, NK3; neuronal nicotinic receptor subunits: alpha 7 & alpha 4 beta 2; NMDA subunits; opioid ... This FOA is intended to stimulate the development of radioligands for molecular targets (e.g., receptors, cell adhesion ...

https://grants.nih.gov/grants/guide/pa-files/PAR-10-024.html

7.7 Alpha2-Adrenergic Agonists 8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy 8.2 Lactation 8.3 Females and Males of Reproductive ... Tizanidine hydrochloride is a central alpha2-adrenergic agonist. Tizanidine hydrochloride, USP is a white to slightly yellow ... 7.7 Alpha2-Adrenergic Agonists. Because hypotensive effects may be cumulative, it is not recommended that tizanidine be used ... Tizanidine hydrochloride is a central alpha-2-adrenergic agonist indicated for the management of spasticity. Because of the ...

https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=99cc8f5f-b947-4ddc-99b6-1e4cef09b717

Adrenergic alpha-Agonists [D27.505.519.625.050.100.100] * Adrenergic alpha-1 Receptor Agonists [D27.505.519.625.050.100.100.100 ... Adrenergic alpha-Agonists [D27.505.696.577.050.100.100] * Adrenergic alpha-1 Receptor Agonists [D27.505.696.577.050.100.100.100 ... Adrenergic alpha2-Agonists Registry Number. 0. Previous Indexing. Adrenergic alpha-Agonists (1995-2010). Sympathomimetics (1966 ... Adrenergic Agents [D27.505.519.625.050] * Adrenergic Agonists [D27.505.519.625.050.100] * ...

https://meshb.nlm.nih.gov/record/ui?ui=D058647

... transient receptor potential vanilloid 1 receptor agonist); this reduced the heat hyperalgesia (and nonevoked pain) but not ... These include the NMDA receptor ketamine, the alpha-2-delta ligands pregabalin and gabapentin and the alpha-2-adrenergic ... The regulation of the surface delivery of this spinal AMPA receptor subunit is caused by stargazin (member of the AMPA receptor ... 127,192 Similar effects are observed by administration of tryptase-binding receptor antagonist (protease-activated receptor 2, ...

https://journals.lww.com/painrpts/Fulltext/2017/03000/Postoperative_pain_from_mechanisms_to_treatment.1.aspx

MeSH Terms: Adenosine Triphosphate/pharmacology*; Adrenergic alpha-Agonists/metabolism; Adrenergic alpha-Agonists/pharmacology ... The use of subtype-selective receptor agonists and antagonists confirmed the involvement of β2 receptors in mediating ... Receptors, Adrenergic, alpha-2/metabolism*; Receptors, Adrenergic, beta-2/metabolism*; Signal Transduction/drug effects; Signal ... Analysis of adrenergic receptor expression with quantitative PCR indicated that resting microglia primarily express β2 ...

https://tools.niehs.nih.gov/portfolio/index.cfm?do=portfolio.publicationDetail&id=2007516

The alpha-1 adrenergic agonist, cirazoline, impairs spatial working memory performance in aged monkeys. Pharmacol. Biochem. ... Intra-BLA infusions of GABAergic receptor antagonists enhance memory consolidation and GABAergic receptor agonists impair ... A glucocorticoid receptor agonist administered into the hippocampus shortly before retention testing also impairs memory ... Beta-adrenergic receptor antagonist antihypertensive medications impair arousal-induced modulation of working memory in elderly ...

http://scholarpedia.org/article/Modulation_of_memory

Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells.. Yu Y ... Alpha 2-Adrenergic Receptor Agonist Brimonidine Stimulates ERK1/2 and AKT Signaling via Transactivation of EGF Receptors in the ... 8. Receptor tyrosine kinase-dependent PI3K activation is an escape mechanism to vertical suppression of the EGFR/RAS/MAPK ... Concomitant inhibition of receptor tyrosine kinases and downstream AKT synergistically inhibited growth of KRAS/BRAF mutant ...

https://pubmedhh.nlm.nih.gov/biomarkers/search.php?id=27562229&mod=related&page=1&from=&outid=&proj=

Under physiological conditions, adrenergic stimulation has been shown to be a negative regulator of proinflammatory cytokine ... Enhanced adrenergic stimulation and catecholamine release are important components of the pathophysiology of sepsis. ... Data are also presented that demonstrate the involvement of protein kinase A activation with adrenergic agonist but not with IL ... Here we have investigated if adrenergic stimulation similarly inhibits TNF-alpha and IL-6 production by splenic macrophages ...

https://pubmed.ncbi.nlm.nih.gov/15151906/?dopt=Abstract

Adrenergic alpha-1 Receptor Agonists [D27.505.519.625.050.100.100.100] Adrenergic alpha-1 Receptor Agonists ... Adrenergic alpha2 Agonists Adrenergic alpha2-Agonists Agonists, Adrenergic alpha-2 alpha-2 Agonists, Adrenergic alpha2-Agonists ... Adrenergic alpha2 Agonists. Adrenergic alpha2-Agonists. Agonists, Adrenergic alpha-2. alpha-2 Agonists, Adrenergic. alpha2- ... Adrenergic alpha-2 Receptor Agonists - Preferred Concept UI. M0543921. Scope note. Compounds that bind to and activate ...

https://decs.bvsalud.org/en/ths/?filter=ths_termall&q=Agonistes+des+r%C3%A9cepteurs+alpha-2+adr%C3%A9nergiques

https://meshb-prev.nlm.nih.gov/record/ui?ui=D058647

... a partial nicotinic receptor agonist) and clonidine (an alpha-2 adrenergic agonist), were described in brief. ... a nicotinic receptor partial agonist). The antidepressant drug bupropion was not registered at the Jordan Food and Drug ... Stage 2 (June-July 2013): Conduct of a national situation analysis. A national situation analysis was conducted by KHCC and the ... King Hussein Cancer Centre (KHCC) and the Jordanian MoH were the 2 main parties spearheading the process. KHCC was founded in ...

https://www.emro.who.int/fr/emhj-volume-21-2015/volume-21-issue-11/jordan-tobacco-dependence-treatment-guidelines-rationale-and-development.html

... alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1 ... it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. ... binding assays at concentrations up to 100 microM and did not exhibit affinity for a number of other common receptor sites, ... or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not ...

https://www.prescriptiondrugs.com/gabapentin-tablets-usp-600-mg-and-800-mg-allied-pharma-inc/

This could be steadily increased act as a peripheral partial alpha-adrenergic receptor agonist, to 500 mg to 2 grams daily, up ... as an estrogen receptor agonist in therapy of infertility because of hyperprolacti some tissues and as an estrogen receptor ... Clomiphene is a se gestion, orthostasis, nausea/vomiting, and lective estrogen receptor modulator, meaning headache could occur ... Combined inhaled anticholinergics and quick-appearing beta2-agonists for preliminary therapy of acute bronchial asthma in kids ...

https://www.ehd.org/pregnancy-calendar/calendar.php?id=14354&week=3&comment_sort=&comment_p=3679

For this purpose, we generated mice that lack beta2-ARs or Gs-alpha selectively in SKM (SKM-ß2-AR-KO, SKM-Gs-KO mice). We also ... This study tested whether the in vivo treatment with clenbuterol (beta2-AR agonist) improves glucose metabolism by SKM beta2-AR ... Role of Skeletal Muscle in Beta2-adrenergic Receptor Mediated Improvements in Whole Body Glucose Homeostasis. Thursday, ... Previous work with cultured SKM cells indicates that activation of SKM beta2-adrenergic receptors (beta2-ARs) can promote ...

https://researchfestival.nih.gov/2017/posters/role-skeletal-muscle-beta2-adrenergic-receptor-mediated-improvements-whole

Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as ... The drug has minimal to no binding affinity for 5-HT3, dopamine, muscarinic, histamine (H1), opioid, or alpha-1 or alpha-2 ... Tegaserod is a selective partial agonist at the serotonin-4 (5-HT4) receptor and possesses gastrointestinal prokinetic activity ... Tegaserod is a 5-HT4 agonist that has demonstrated efficacy in the short-term treatment of women with IBS whose primary bowel ...

https://www.drugtopics.com/view/pt-portfolio-zelnorm

21556 Adenosine receptor antagonist 40787 Adrenaline agonist 23473 Adrenaline antagonist 90977 Adrenergic transmitter uptake ... 50524 Alpha adrenoreceptor agonist 21666 Alpha adrenoreceptor antagonist 26458 Alpha glucosidase inhibitor 125412 Alzheimers ... 81942 GABA A receptor agonist 77515 GABA A receptor antagonist 98060 GABA B receptor agonist 64771 GABA B receptor antagonist ... 12121 Opioid delta receptor agonist 12729 Opioid kappa receptor agonist 31484 Opioid mu receptor agonist 52696 Opioid partial ...

https://cactus.nci.nih.gov/ncidb2.2/PASS_Predictions.txt

In: DOURISH, C.T., COOPER, S.J., IVERSEN, S.D. and IVERSEN, L.L., eds., Multiple cholecystokinin receptors in the CNS Oxford ... Endogenous adrenergic control of reflexes evoked by mechanical stimulation of the heel in the decerebrated rabbit Neuroscience ... Alpha 2-adrenoceptors mediate inhibition of withdrawal reflexes after remote noxious stimuli in the anaesthetised rabbit ... 5-HT receptors involved in opioid-activated descending inhibition of spinal withdrawal reflexes in the decerebrated rabbit Pain ...

https://www.nottingham.ac.uk/research/groups/neuroscience/people/john.harris

... is an adrenergic receptor blocking agent that has both selective alpha1-adrenergic and nonselective beta-adrenergic receptor ... Drugs possessing beta-blocking properties can blunt the bronchodilator effect of beta-receptor agonist drugs in patients with ... Labetalol HCl combines both selective, competitive, alpha1-adrenergic blocking and nonselective, competitive, beta-adrenergic ... Due to the alpha1-receptor blocking activity of labetalol HCl, blood pressure is lowered more in the standing than in the ...

https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89d30255-8753-4cf2-8e93-e4d752eac87f

... adrenergic receptors. We create the concept of alpha1- and alpha2-ARs regulation of SWDs via modulation of thalamocortical ... Dexmedetomidine (Dex) was a highly selective alpha-2 agonist (0.003-0.049 mg/kg, i.p.). Injections of Dex did not elicit de ... Second, fabomotizole is a Sigma1R chaperone agonist, and exposure to Sigma1R antagonists blocks its anxiolytic effect. To prove ... Considering that pentylenetetrazole inhibits GABAA receptors, this result supports a role for this receptor in the activity ...

https://pesquisa.bvsalud.org/nicaragua/?lang=es&q=mh:Hipn%C3%B3ticos+y+Sedantes/farmacolog%C3%ADa

N0000194037 MED-RT alpha-Adrenergic Decongestant [EPC] N0000175957 MED-RT mu-Opioid Receptor Agonist [EPC] N0000191867 MED-RT ... N0000009932 MED-RT alpha-Adrenergic Agonist [EPC] N0000175552 MED-RT alpha-Hydroxy Acid [EPC] N0000175842 MED-RT alpha-Particle ... N0000010605 MED-RT alpha-1 Adrenergic Agonist [EPC] N0000186105 MED-RT beta-Adrenergic Agonist [EPC] N0000175555 MED-RT l- ... N0000175789 MED-RT Adrenergic alpha-Agonists [MoA] N0000000209 MED-RT Adrenergic alpha-Antagonists [MoA] N0000000099 MED-RT ...

https://evs.nci.nih.gov/ftp1/MED-RT/MEDRT.txt

Soluble Amyloid Precursor Protein alpha (sAPP alpha). beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) ... Repurposing beta-3 adrenergic receptor agonists for Alzheimers disease: beneficial effects in a mouse model BIBLIOGRAPHIC ... through β3 adrenergic receptor (β3AR) agonists or cold acclimation, counteracts metabolic deficits in rodents and humans. ... Methods: CL-316,243, a specific β3AR agonist, was administered to the triple transgenic mouse model of AD (3xTg-AD) and non- ...

http://alzped.nia.nih.gov/repurposing-beta-3-adrenergic

ß2-Adrenergic receptor agonists (ß2-agonists) activate PKA, and we hypothesized that ß2-agonists would beneficially impact HDE- ... TNF-alpha, CXCL1, and CXCL2 release in bronchoalveolar lavage fluid following a one-time exposure to HDE. Likewise, when mice ... Bronchial epithelial cells were cultured with the short-acting ß2-agonist salbutamol or the long-acting ß2-agonist salmeterol ... ß2-Agonist treatment significantly increased PKA activation and significantly decreased HDE-stimulated IL-6 and IL-8 production ...

http://www2a.cdc.gov/nioshtic-2/BuildQyr.asp?s1=agricultur%2A+or+farm%2A&f1=%2A&Adv=0&terms=1&PageNo=150&RecNo=1493&View=f&

The use of subtype-selective receptor agonists and antagonists confirmed the involvement of β2 receptors in mediating microglial process dynamics in resting cells and α2A receptors in activated cells. (nih.gov)
Co-application of NE with ATP to resting microglia blocked the ATP-induced process extension and migration in isolated microglia, and β2 receptor antagonists prolonged ATP effects in brain slice tissues, suggesting the presence of cross-talk between adrenergic and purinergic signaling in microglia. (nih.gov)
Pretreatment of macrophage cultures with beta(2)- (ICI-118551) but not beta(1)-adrenergic (atenolol) receptor antagonists reversed the epinephrine-mediated cytokine attenuation following LPS treatment. (nih.gov)
Adrenergic antagonists are a type of drug that blocks the action of adrenaline in the body . (osmosis.org)
Therefore, specific 5-HT 3 receptor antagonists, such as ondansetron and granisetron, are effective for treatment of vomiting that accompanies chemotherapy. (merckvetmanual.com)
Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. (lookformedical.com)
Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE . (lookformedical.com)

The tartrate salt form of brimonidine, an imidazole derivative and a selective alpha-2 adrenergic receptor agonist. (blogspot.com)

Beta-blockers are a type of adrenergic antagonist that blocks the sympathetic activation of Beta-adrenergic receptors. (osmosis.org)
These include the alpha-2 adrenergic agonists clonidine and guanfacine, the nonselective beta-adrenergic agent propranolol, and most promising prazosin, which is an alpha-1 adrenergic receptor antagonist that blocks the actions of NE on alpha-1 receptors(Petrakis, 2016). (professionalacademictutors.com)

Before and after treatments, plasma beta-endorphin levels were evaluated in response to three neuroendocrine tests: (a) clonidine, an alpha 2-presynaptic adrenergic agonist (1.25 mg i.v.) (b) naloxone, an opioid receptor antagonist (4 mg i.v.) and (c) fluoxetine, a serotonin selective reuptake inhibitor (30 mg p.o. (unifi.it)
Stimulation of the 5-HT 4 receptor increases the presynaptic release of acetylcholine and calcitonin gene-related peptide, thereby enhancing neurotransmission. (merckvetmanual.com)
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. (lookformedical.com)
While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS , the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release. (lookformedical.com)

Labetalol hydrochloride (HCl) is an adrenergic receptor blocking agent that has both selective alpha 1 -adrenergic and nonselective beta-adrenergic receptor blocking actions in a single substance. (nih.gov)
Labetalol HCl combines both selective, competitive, alpha 1 -adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. (nih.gov)
A nonselective alpha-adrenergic antagonist. (lookformedical.com)

Racemic epinephrine solution causes alpha-adrenergic receptor-mediated vasoconstriction of edematous tissues, thereby reversing upper airway edema. (medscape.com)
Glucocorticoids alter the sensitivity of epinephrine in influencing memory consolidation and, conversely, adrenergic activation induced by emotional arousal appears to be essential in enabling glucocorticoid modulation of memory consolidation. (scholarpedia.org)
Macrophage cultures from CLP animals incubated with either epinephrine or IL-10 for 2 h had significantly reduced TNF-alpha and IL-6 release in response to LPS. (nih.gov)
Alpha blockers and beta blockers are two types of postsynaptic anti-adrenergic medications that prevent their respective receptors from being stimulated by catecholamines, like norepinephrine and epinephrine . (osmosis.org)

Enhanced adrenergic stimulation and catecholamine release are important components of the pathophysiology of sepsis. (nih.gov)
Under physiological conditions, adrenergic stimulation has been shown to be a negative regulator of proinflammatory cytokine production through increasing IL-10 production. (nih.gov)
Here we have investigated if adrenergic stimulation similarly inhibits TNF-alpha and IL-6 production by splenic macrophages isolated from a polymicrobial sepsis model. (nih.gov)
Data are also presented that demonstrate the involvement of protein kinase A activation with adrenergic agonist but not with IL-10 stimulation. (nih.gov)
This study tested whether the in vivo treatment with clenbuterol (beta2-AR agonist) improves glucose metabolism by SKM beta2-AR stimulation. (nih.gov)
Bronchial epithelial cells were cultured with the short-acting ß2-agonist salbutamol or the long-acting ß2-agonist salmeterol prior to stimulation with HDE. (cdc.gov)
Brown adipose tissue (BAT) is the main thermogenic driver in mammals and its stimulation, through β3 adrenergic receptor (β3AR) agonists or cold acclimation, counteracts metabolic deficits in rodents and humans. (nih.gov)
Since metabolic disorders and AD share strong pathogenic links, we hypothesized that BAT stimulation through a β3AR agonist could exert benefits in AD as well. (nih.gov)
The present experiments were undertaken to investigate the electrophysiological responses of the canine saphenous vein evoked by perivascular nerve stimulation, norepinephrine or selective alpha adrenergic agonists before and after chronic sympathetic denervation. (elsevier.com)
Denervation augments selectively the electrical response to alpha-2 adrenergic stimulation. (elsevier.com)

Receptors of CLONIDINE and other IMIDAZOLINES. (lookformedical.com)

Brimonidine Tartrate Ophthalmic Solution is an alpha adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (nih.gov)
Brimonidine tartrate ophthalmic solution is contraindicated in neonates and infants (under the age of 2 years). (nih.gov)
Brimonidine Tartrate ophthalmic solution 0.2% is an alpha adrenergic receptor agonist. (com.bd)

16. Regorafenib suppresses epidermal growth factor receptor signaling-modulated progression of colorectal cancer. (nih.gov)
17. Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells. (nih.gov)
An orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. (blogspot.com)

Open-channel blockade is less effective on GluN3B than GluN3A subunit-containing NMDA receptors European Journal of Pharmacology. (nottingham.ac.uk)

For this purpose, we generated mice that lack beta2-ARs or Gs-alpha selectively in SKM (SKM-ß2-AR-KO, SKM-Gs-KO mice). (nih.gov)

Taken together, these findings suggest that adrenergic mechanisms may influence peripheral tissue macrophage inflammatory cytokine response following trauma and sepsis, independent of the effects of IL-10. (nih.gov)
Here, we show that β3AR agonist administration decreased body weight and improved peripheral glucose metabolism and BAT thermogenesis in both non-transgenic and 3xTg-AD mice. (nih.gov)
Metoclopramide is a central dopaminergic receptor antagonist and peripheral 5-HT 3 receptor antagonist and 5-HT 4 receptor agonist with GI and CNS effects. (merckvetmanual.com)

The slow depolarization was inhibited by rauwolescine or phentolamine, but not by prazosin, whereas excitatory junction potentials were not inhibited by alpha adrenergic blockers. (elsevier.com)
Several randomized controlled trials have found that the alpha-1 blocker prazosin is effective in reducing symptoms of posttraumatic stress disorder (PTSD) among active-duty soldiers(Roundup, 2017). (professionalacademictutors.com)

12. Concomitant inhibition of receptor tyrosine kinases and downstream AKT synergistically inhibited growth of KRAS/BRAF mutant colorectal cancer cells. (nih.gov)

The drug has minimal to no binding affinity for 5-HT 3 , dopamine, muscarinic, histamine (H 1 ), opioid, or alpha-1 or alpha-2 adrenergic receptors. (drugtopics.com)

The alpha(1)-adrenoceptor potencies were quite similar for the five drugs and varied between 3.2 mug/kg for ICI 110802 and 8.7 mu/kg for ICI 106720. (nih.gov)
Potency as alpha(2)-adrenoceptor agonists was also assessed in the mouse vas deferens. (nih.gov)
Methyldopa is an alpha2-adrenoceptor selective agonist CAS:5. (guidechem.com)
A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity. (lookformedical.com)

Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists . (lookformedical.com)

19. Alpha 2-Adrenergic Receptor Agonist Brimonidine Stimulates ERK1/2 and AKT Signaling via Transactivation of EGF Receptors in the Human MIO-M1 Müller Cell Line. (nih.gov)
Alcon Brimonidine is contraindicated in children aged less than 2 years because of serious systemic safety risk. (pillintrip.com)
Safety concerns related to the systemic absorption of brimonidine have also been identified for the age group 2 to 12 years. (pillintrip.com)
Alcon Brimonidine should not be used in children or adolescents aged 2 to 18 years. (pillintrip.com)
Brimonidine is an α-2 adrenoreceptor agonist that is more selective for the α-2 adrenoreceptor than α-1. (com.bd)

Guanfacine is a selective alpha-2A adrenergic receptor agonist in that it has 15-20 times higher affinity for this receptor subtype than for the alpha-2B or alpha-2C subtypes. (allsales.in)
Preclinical research suggests guanfacine modulates signalling in the prefrontal cortex and basal ganglia through direct modification of synaptic noradrenalin transmission at the alpha 2- adrenergic receptors. (allsales.in)

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS . (nih.gov)
ß2-Adrenergic receptor agonists (ß2-agonists) activate PKA, and we hypothesized that ß2-agonists would beneficially impact HDE-induced adverse airway inflammatory consequences. (cdc.gov)
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. (lookformedical.com)

The memory-modulating effects of glucocorticoids appear to involve the selective activation of the low-affinity glucocorticoid receptor. (scholarpedia.org)
Results of the in silico studies demonstrated that QUR has better binding interaction with GABAA α3, ß1, and Î³2 subunits when compared with DZP, whereas LIN showed moderate affinity with the GABAA receptor. (bvsalud.org)
The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. (lookformedical.com)

We unclosed some alpha2-adrenergic mechanisms of sedation and provocation of SWDs in rats with spontaneous spike-wave epilepsy (WAG/Rij and Wistar) and in control non-epileptic rats (NEW) of both sexes. (bvsalud.org)

Specific 5-HT 4 receptor agonists, such as cisapride, enhance neurotransmission and depend on natural stimuli to evoke peristaltic and secretory reflexes. (merckvetmanual.com)

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABA A or GABA B radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. (prescriptiondrugs.com)

The effect of serotonin on intestinal activity is coordinated by 5-HT receptor subtypes. (merckvetmanual.com)
However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. (lookformedical.com)

Microglia respond to tissue damage through activation of ATP/ADP receptors followed by directional process extension to the damaged area. (nih.gov)
8. Receptor tyrosine kinase-dependent PI3K activation is an escape mechanism to vertical suppression of the EGFR/RAS/MAPK pathway in KRAS-mutated human colorectal cancer cell lines. (nih.gov)
9. KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer. (nih.gov)
Previous work with cultured SKM cells indicates that activation of SKM beta2-adrenergic receptors (beta2-ARs) can promote glucose uptake. (nih.gov)
Activation of 5-HT 4 receptors in the GI tract by tegaserod stimulates the peristaltic reflex and intestinal secretion, in addition to inhibiting visceral sensitivity. (drugtopics.com)
Subjects with long-lasting SWDs at baseline were at high risk of absence status after activation of alpha2- adrenergic receptors. (bvsalud.org)
ß2-Agonist treatment significantly increased PKA activation and significantly decreased HDE-stimulated IL-6 and IL-8 production in a concentration- and time-dependent manner. (cdc.gov)
Transiently activated during lymphocyte activation, CD30 (tumor necrosis factor receptor superfamily, member 8;TNFRSF8) may be constitutively expressed in hematologic malignancies including Hodgkin lymphoma and some T-cell non-Hodgkin lymphomas. (blogspot.com)
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS. (lookformedical.com)

Inactive Sendai virus grown in LLC-MK(2) cells, which possessed an uncleaved precursor glycoprotein, F, and was noninfectious to tissue culture cells, neither grew nor caused pathological changes in the lung of mice. (nih.gov)

Agonist and antagonist binding to alpha 2-adrenergic receptors in purified membranes from human platelets. (aspetjournals.org)

Norepinephrine modulates the motility of resting and activated microglia via different adrenergic receptors. (nih.gov)
However, glucocorticoids may also act more rapidly by interacting with membrane receptors and/or potentiating the efficacy of the norepinephrine-signal cascade via an interaction with G-protein-mediated actions. (scholarpedia.org)
These results indicate that in the canine saphenous vein norepinephrine, whether added exogenously or released from sympathetic nerves, causes predominant depolarization by activating alpha-2 adrenergic receptors. (elsevier.com)

Tegaserod, by acting as an agonist at neuronal 5-HT 4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. (drugtopics.com)

An adrenergic alpha-2 agonist used as a sedative, analgesic and centrally acting muscle relaxant in VETERINARY MEDICINE. (lookformedical.com)

Glucocorticoids act through intracellular and intranuclear receptors and can affect gene transcription by direct binding of receptor homodimers to DNA . (scholarpedia.org)

One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. (lookformedical.com)

The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction . (lookformedical.com)

Tegaserod is a 5-HT 4 agonist that has demonstrated efficacy in the short-term treatment of women with IBS whose primary bowel symptom is constipation. (drugtopics.com)
We evaluated the efficacy and safety of dupilumab (SAR231893/REGN668), a fully human monoclonal antibody to the alpha subunit of the interleukin-4 receptor, in patients with persistent, moderate-to-severe asthma and elevated eosinophil levels. (nih.gov)
To date, a number of adrenergic agents have been tested for their efficacy in treating PTSD. (professionalacademictutors.com)

The goal of this work was to investigate whether different fractions of somatic cells in cow milk do produce prostaglandins, leukotrienes and the cytokine tumor necrosis factor alpha (TNFalpha). (gene-quantification.de)

An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS . (lookformedical.com)

While these medicine have an uncontested Use of inhaled beta-2 agonists for therapy of bronchial asthma painkilling impact, the excessive prevalence of appreciable side was reported signicantly more typically in feminine than in male effects, significantly with extensive and long-term use, is nicely senior and youth soccer gamers. (ehd.org)
When trypsin treatment was made which cleaved F into F(1) and F(2) subunits, the virus became activated so that it could initiate replication in the bronchial epithelium of the lung. (nih.gov)
A protease mutant, TR-2, which was able to be activated only by chymotrypsin but not by trypsin, could also initiate replication in the bronchial epithelium, when activated by chymotrypsin before inoculation into mice. (nih.gov)

Glucocorticoids are highly lipophilic and, thus, readily enter the brain and bind directly to mineralocorticoid receptors and glucocorticoid receptors. (scholarpedia.org)
We enrolled patients with persistent, moderate-to-severe asthma and a blood eosinophil count of at least 300 cells per microliter or a sputum eosinophil level of at least 3% who used medium-dose to high-dose inhaled glucocorticoids plus long-acting beta-agonists (LABAs). (nih.gov)

Methyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.Target: alpha-adrenergic agonistMethyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. (guidechem.com)

Implications of receptor-inhibitory nucleotide-binding protein stoichiometry. (aspetjournals.org)

then the participant will take the study drugs at home for about 4 weeks, followed by another 2-day stay in the clinic. (nih.gov)
The 5-HT 1P receptor initiates peristaltic and secretory reflexes, but so far no drugs have been developed to target this specific receptor. (merckvetmanual.com)

In the present report, we evaluated adrenergic mechanisms of generalized spike-wave epileptic discharges (SWDs), which are the encephalographic hallmarks of idiopathic generalized epilepsies. (bvsalud.org)
Type 2 diabetes mellitus (T2DM) and metabolic syndrome (MetS) are common comorbidities in chronic obstructive pulmonary disease (COPD), but the underlying pathogenic mechanisms are poorly understood. (dovepress.com)

Tegaserod is a selective partial agonist at the serotonin-4 (5-HT 4 ) receptor and possesses gastrointestinal prokinetic activity. (drugtopics.com)

Beta 2 -receptor blockade was demonstrated by inhibition of the isoproterenol-induced fall in diastolic blood pressure. (nih.gov)

For this, we observed the ability of test and standard medications to interact with various gamma-aminobutyric acid A receptor (GABAA) subunits. (bvsalud.org)

Labetalol HCl produces dose-related falls in blood pressure without reflex tachycardia and without significant reduction in heart rate, presumably through a mixture of its alpha- and beta-blocking effects. (nih.gov)
The peak effects of single oral doses of labetalol HCl occur within 2 to 4 hours. (nih.gov)
Effects on various type 2 helper T-cell (Th2)-associated biomarkers and safety and tolerability were also evaluated. (nih.gov)

Metabolic syndrome (MetS) is a cluster of consumption of saturated fats to unsaturated fats, metabolic risk factors for cardiovascular disease and increase the intake of fruits, vegetables, legumes type 2 diabetes. (bvsalud.org)

An antibody-drug conjugate (ADC) directed against the tumor necrosis factor (TNF) receptor CD30 with potential antineoplastic activity. (blogspot.com)

Skeletal muscle (SKM) insulin resistance is a hallmark of type 2 diabetes (T2D), one of the largest health problems worldwide. (nih.gov)

Ribavirin (1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide) is a synthetic nucleoside analogue that resembles guanosine and inosine. (medscape.com)
In man, the ratios of alpha- to beta-blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. (nih.gov)
Beta 2 -agonist activity has been demonstrated in animals with minimal beta 1 -agonist (ISA) activity detected. (nih.gov)
In animals, at doses greater than those required for alpha-or beta-adrenergic blockade, a membrane stabilizing effect has been demonstrated. (nih.gov)
Labetalol HCl's beta 1 -receptor blockade in man was demonstrated by a small decrease in the resting heart rate, attenuation of tachycardia produced by isoproterenol or exercise, and by attenuation of the reflex tachycardia to the hypotension produced by amyl nitrite. (nih.gov)
Both the alpha-and beta-blocking actions of orally administered labetalol HCl contribute to a decrease in blood pressure in hypertensive patients. (nih.gov)
Stuckey et al19 evaluated whether an 8-week and central alpha 2-1 and beta-adrenergic receptors. (bvsalud.org)
8. History of hypertension or subjects on antihypertensive therapy since the combination therapy on other beta receptors is unknown. (nih.gov)
this scheme does not respect the alpha-beta distinction. (lookformedical.com)

Heart attack, Stroke and Type 2 diabetes. (bvsalud.org)

Using an established intranasal inhalation exposure model, we found that salbutamol pretreatment reduced airway neutrophil influx and IL-6, TNF-alpha, CXCL1, and CXCL2 release in bronchoalveolar lavage fluid following a one-time exposure to HDE. (cdc.gov)
Together, these results support the need for future clinical investigations to evaluate the utility of ß2-agonist therapies in the treatment of airway inflammation associated with CAFO dust exposure. (cdc.gov)

Anatomy1

Organisms3

Chemicals and Drugs61

Analytical, Diagnostic and Therapeutic Techniques and Equipment1

Phenomena and Processes2

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/319)

Role of potassium channels in the antinociception induced by agonists of alpha2-adrenoceptors. (2/319)

Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/319)

Cardiopulmonary effects of the alpha2-adrenoceptor agonists medetomidine and ST-91 in anesthetized sheep. (4/319)

The alpha2A-adrenergic receptor discriminates between Gi heterotrimers of different betagamma subunit composition in Sf9 insect cell membranes. (5/319)

Effect of strenuous, acute exercise on alpha2-adrenergic agonist-potentiated platelet activation. (6/319)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (7/319)

Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. (8/319)

Wakefulness-Promoting Agents

Receptors, Adrenergic, alpha-2

Purinergic P1 Receptor Agonists

Serotonin Receptor Agonists

Dopamine Agonists

Serotonin 5-HT1 Receptor Agonists

Serotonin 5-HT2 Receptor Agonists

Adenosine A1 Receptor Agonists

Dose-Response Relationship, Drug

GABA Agonists

GABA-A Receptor Agonists

Adenosine A2 Receptor Agonists

GABA-B Receptor Agonists

Adrenergic alpha-2 Receptor Agonists

Cannabinoid Receptor Agonists

Serotonin 5-HT4 Receptor Agonists

Rats, Sprague-Dawley

Purinergic P2 Receptor Agonists

Receptors, Adrenergic, alpha

alpha 1-Antitrypsin

Receptors, Opioid, kappa

Adenosine A3 Receptor Agonists

Adrenergic alpha-Agonists

Histamine Agonists

Adenosine

Muscarinic Agonists

Nicotinic Agonists

Receptors, Opioid, mu

Serotonin Antagonists

Phenethylamines

Receptors, Dopamine D2

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine

Adrenergic beta-3 Receptor Agonists

Rats, Wistar

Hypoxia-Inducible Factor 1, alpha Subunit

Receptors, Opioid, delta

Adrenergic Agonists

Quinpirole

Baclofen

Receptors, Purinergic P1

Excitatory Amino Acid Agonists

Receptors, Dopamine D1

Radioligand Assay

Benzazepines

8-Hydroxy-2-(di-n-propylamino)tetralin

Piperidines

Signal Transduction

Enkephalin, Ala(2)-MePhe(4)-Gly(5)-

Receptor, Adenosine A2A

Adrenergic beta-Agonists

Cannabinoids

alpha7 Nicotinic Acetylcholine Receptor

Receptors, Adrenergic, alpha-1

Receptors, Opioid

Muscimol

Adrenergic alpha-1 Receptor Agonists

Cells, Cultured

Ligands

Pyrrolidines

Receptors, Serotonin

Receptors, Nicotinic

Naphthalenes

Mice, Inbred C57BL

Calcium

Cyclic AMP

Adenosine-5'-(N-ethylcarboxamide)

Clonidine

Cholinergic Agonists

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/319)

Role of potassium channels in the antinociception induced by agonists of alpha2-adrenoceptors. (2/319)

Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/319)

Cardiopulmonary effects of the alpha2-adrenoceptor agonists medetomidine and ST-91 in anesthetized sheep. (4/319)

The alpha2A-adrenergic receptor discriminates between Gi heterotrimers of different betagamma subunit composition in Sf9 insect cell membranes. (5/319)

Effect of strenuous, acute exercise on alpha2-adrenergic agonist-potentiated platelet activation. (6/319)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (7/319)

Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. (8/319)

Alpha-2 adrenergic receptor

Alpha-adrenergic agonist

Mivazerol

Adrenergic antagonist