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)

Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Endothelium receptor blockersEdit. Bosentan belongs to a new class of drug and works by blocking the receptors of the hormone ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ...

https://en.m.wikipedia.org/wiki/Antihypertensive_drug

Alpha-1 adrenergic receptor agonist Constrict the peripheral blood vessels aiding venous return. Midodrine[17][89][90][91] ... Antibodies against the Alpha 1 adrenergic receptor and muscarinic acetylcholine M4 receptor[4][5][6]. ... In these patients the selective Alpha-1 adrenergic receptor agonist midodrine may increase venous return, enhance stroke volume ... elevated levels of autoantibodies against the adrenergic alpha 1 receptor and against the muscarinic acetylcholine M4 receptor. ...

https://en.wikipedia.org/wiki/Postural_orthostatic_tachycardia_syndrome?fbclid=IwAR2m8ZJtGrPxMde9Kcig0hirlDDwZlopEkcXtoRcEKOdsmSvNO64truK5qc

... specifically at the 5-HT1A and 5-HT1B G-protein coupled receptors. Additionally, the effect of MDMA on alpha-2 receptors is ... Giovannitti JA, Thoms SM, Crawford JJ (2015-03-01). "Alpha-2 adrenergic receptor agonists: a review of current clinical ... Neurochemically, MDMA activates 5-hydroxytryptamine, or 5-HT serotonin receptors, ... After 2 hours, a supplemental 62.5mg dose of MDMA is administered orally. The therapist works with the patient for 6 hours, or ...

https://en.wikipedia.org/wiki/MDMA-assisted_psychotherapy

... converts alpha-methyldopamine into alpha-methylnorepinephrine, which is an agonist of the presynaptic α2-adrenergic receptor ... Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication. It works by stimulating the brain to decrease ... LAAD converts it into alpha-methyldopamine, a false prescursor to norepinephrine, which in turn reduces synthesis of ... with increased use of other safer and more tolerable agents such as alpha blockers, beta blockers, and calcium channel blockers ...

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

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 ... The 7 repeat variant of dopamine receptor D4 (DRD4-7R) causes increased inhibitory effects induced by dopamine and is ... Conversely, methylphenidate, …showed poor efficacy at the TAAR1 receptor. In this respect it is worth noting that the ...

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

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

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

Phenibut is a GABAB receptor agonist, as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels ( ... Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... The alpha1 antagonist prazosin could be effective for PTSD The Alpha-2 adrenergic receptor agonists clonidine and guanfacine ... Azapirones are a class of 5-HT1A receptor agonists. Currently approved azapirones include buspirone (Buspar) and tandospirone ( ...

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

... α2-adrenergic agonist, used to temporarily sedate animals yohimbine - used to reverse effects of xylazine, also called an " ... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists Albendazole ... dopamine receptor agonist used for the treatment of pituitary pars intermedia dysfunction in horses phenobarbital - anti- ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses carprofen - COX-2 ...

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

The drug Brindley injected into his penis was a non-specific vasodilator, an alpha-blocking agent, and the mechanism of action ... Causes of or contributors to ED include the following: Prescription drugs (e.g., SSRIs, beta blockers, alpha-2 adrenergic ... receptor agonists, thiazides, hormone modulators, and 5α-reductase inhibitors) Neurogenic disorders (e.g., diabetic neuropathy ... Brindley GS (October 1983). "Cavernosal alpha-blockade: a new technique for investigating and treating erectile impotence". Br ...

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

Beta-adrenergic blocking agents (beta blockers) also form part of the first line of treatment, adding to the improvement in ... Japp D, Shah A, Fisken S, Denvir M, Shenkin S, Japp A (January 2017). "Mineralocorticoid receptor antagonists in elderly ... Yohimbine can exacerbate heart failure by increasing blood pressure through alpha-2 adrenergic receptor antagonism. Heart ... dopamine agonists, TNF inhibitors, calcium channel blockers (especially verapamil and diltiazem), salbutamol, and tamsulosin. ...

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

... (pronounced GWAHN-a-benz, sold under the trade name Wytensin) is an alpha agonist of the alpha-2 adrenergic receptor ... 2: S543-6.[permanent dead link] v t e. ...

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

... responses of depressive symptoms to dopamine receptor agonists, decreased dopamine receptor D1 binding in the striatum, and ... Third, decreased size of the locus coeruleus, decreased activity of tyrosine hydroxylase, increased density of alpha-2 ... adrenergic receptor, and evidence from rat models suggest decreased adrenergic neurotransmission in depression. Furthermore, ... Secondly, the correlation between depression risk and polymorphisms in the 5-HTTLPR gene, which codes for serotonin receptors, ...

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

February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... and dopamine D3 receptors.[31][32] It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B ... and as a partial agonist at 5-HT1A.[31][33][34][35] Yohimbine interacts with serotonin and dopamine receptors in high ... "Regulation of pre-synaptic alpha adrenergic activity in the corpus cavernosum". Review. International Journal of Impotence ...

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

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 ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...

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

It is thought these effects are mediated via a partial agonist action at Alpha-2 adrenergic receptors, and TDIQ has been ... 72 (1-2): 379-87. doi:10.1016/S0091-3057(01)00768-7. PMID 11900809. S2CID 33311107. Young R (2007). "TDIQ (5,6,7,8-tetrahydro-1 ... 71 (1-2): 205-13. CiteSeerX 10.1.1.670.8659. doi:10.1016/S0091-3057(01)00666-9. PMID 11812524. S2CID 16553365. Glennon RA, ... TDIQ (also known as 6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinoline or MDTHIQ) is a drug used in scientific research, which ...

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

... σ receptor antagonists ... prevent the development of behavioral sensitization to METH [17, 18]. ... σ Receptor agonists have ... Methamphetamine is also an agonist of the alpha-2 adrenergic receptors and sigma receptors with a greater affinity for σ1 than ... An extremely large overdose may produce symptoms such as adrenergic storm, methamphetamine psychosis, substantially reduced or ... Methamphetamine has been identified as a potent full agonist of trace amine-associated receptor 1 (TAAR1), a G protein-coupled ...

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

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

... has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP- ... Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor ... Repinotan acts as a selective high-affinity full receptor agonist at the 5-HT1A receptor subtype. It increases the activity of ...

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

Agonists (−)-Dibromophakellin Antagonists Imiloxan Yohimbine Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000274286 - ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...

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

Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation". The Journal of Biological ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...

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

"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 veterinary anaesthesia where they affect sedation, ... 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

"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 ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... 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

... 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

... 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

... 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

Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Adrenergički receptor. Reference[уреди]. *^ Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait ...

https://sr.wikipedia.org/wiki/Alfa-2_adrenergički_receptor

... agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". ... Perry BD, U'Prichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2- ... adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. PMID 6276200. doi:10.1016/0014-2999(81)90123-0.. ... On takođe deluje kao parcijalni agonist 5-HT1A receptora i antagonist 5-HT2A i 5-HT2B receptora.[3][4][5] ...

https://sr.wikipedia.org/wiki/Rauvolscin

"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. Postoje tri ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...

https://sh.wikipedia.org/wiki/Alfa-2_adrenergički_receptor

... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ...

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

腎上腺素受體激動藥 (α（英語：Alpha-adrenergic agonist） ... Glutamate receptor agonist（英語：Excitatory amino acid agonist） (AMPA（英語：Ampakine）) ... Acetylcholine receptor agonist（英語：Parasympathomimetic_drug） (Muscarinic（英語：Muscarinic agonist） ... Glutamate receptor antagonist（英語：Excitatory amino acid antagonist） (NMDA（英語：NMDA receptor

https://zh.wikipedia.org/zh-hk/肾上腺素

Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... although there is evidence that it may have some alpha-1 [7] and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ... is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.[1] Fenoldopam is used as ...

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

See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... Clortermine (Voranil) was developed by Ciba in the 1960s[1] and is an anorectic drug of the amphetamine class.[2] It is the 2- ... InChI=1S/C10H14ClN/c1-10(2,12)7-8-5-3-4-6-9(8)11/h3-6H,7,12H2,1-2H3 Y ...

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

σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... Sigma receptor modulators. σ1. *Agonists: 3-PPP. *4-PPBP. *5-MeO-DMT ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ...

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

... σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ...

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

Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH. gamolenic acid, gonadotropin release inhibitor ... antifungal, alkalinizing agents, quinolones, antibiotics, cholinergics, anticholinergics, antispasmodics, 5-alpha reductase ... inhaled and systemic corticosteroids, Beta2-adrenergic agonists, anticholinergics, Mast cell stabilizers. Leukotriene ...

https://en.m.wikipedia.org/wiki/Pharmaceutical

See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... N,alpha-Diethylphenylethylamine. *N-Ethylbuphedrone. *N-Ethylhexedrone. *N,N-Dimethylphenethylamine. *Naphthylamphetamine. * ... InChI=1S/C12H17N/c1-2-4-11(5-3-1)10-12-6-8-13-9-7-12/h1-5,12-13H,6-10H2 Y ...

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

Drugs such as bromocriptine act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... alpha-Ergocryptine. CH(CH3)2. CH2CH(CH3)2. Leucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references. ...

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

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

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

Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... Thyroid hormone receptor modulators. Receptor. (ligands). THR. *Agonists: Dextrothyroxine. *DIMIT. *DITPA. *Eprotirome (KB-2115 ... 978-81-89422-33-2. . Retrieved 6 May 2012.. *^ "Investigating leaks in Dams & Reservoirs" (PDF). IAEA.org. Retrieved 6 May 2012 ... 2 (4): 453-6. PMID 4290684.. *^ Woenckhaus, U.; Girlich, C. (2005). "Therapie und Prävention der Hyperthyreose" [Therapy and ...

https://en.wikipedia.org/wiki/Iodine-131

For nocturnal symptoms, intranasal corticosteroids can be combined with nightly oxymetazoline, an adrenergic alpha-agonist, or ... Nasal steroids, antihistamines such as diphenhydramine, cromolyn sodium, leukotriene receptor antagonists such as montelukast, ... Other measures that may be used second line include: decongestants, cromolyn, leukotriene receptor antagonists, and ... and leukotriene receptor antagonists such as montelukast.[5] Medications are, however, not sufficient or are associated with ...

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

In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ...

https://en.wikipedia.org/wiki/Serotonin-norepinephrine_reuptake_inhibitor

See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... 5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... History: 2,5-DMA was first synthesized in Tuckahoe, New York by Richard Baltzly and Johannes S. Buck in 1939.[3] ...

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

Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... on adrenergic receptors.[83] It is most usually marketed as the hydrochloride or sulfate salt. ... adrenergic receptors), producing sympathomimetic effects. Some drugs, such as MDMA and derivatives may decrease regulatory ...

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

5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... Prazosin - Sympatholytic, alpha blocker.. Comorbidity[edit]. GAD and depression[edit]. In the National Comorbidity Survey (2005 ... 19 (2): 107-116.. ,access-date=. requires ,url=. (help). *^ a b Scott, E. L. (2011, September 6). Anxiety Disorders With ... 88 (2): 73-7. PMC 1295099 . PMID 7769598.. *^ Morissette, Sandra Baker; Tull, Matthew T.; Gulliver, Suzy Bird; Kamholz, Barbara ...

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

See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... It is structurally similar to MDA, but without the methyl group at the alpha position. ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase ...

https://en.wikipedia.org/wiki/3,4-Methylenedioxyphenethylamine

See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... InChI=1S/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ... InChI=1/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ...

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

Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine is a nonselective agonist of all adrenergic ... Racemic adrenaline works by stimulation of the alpha adrenergic receptors in the airway, with resultant mucosal ... Epinephrine's binding to these receptors triggers a number of metabolic changes. Binding to α-adrenergic receptors inhibits ... Its actions vary by tissue type and tissue expression of adrenergic receptors. For example, high levels of epinephrine causes ...

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

α1（英语：Alpha-1 adrenergic receptor） (A, B, D) · α2（英语：Alpha-2 adrenergic receptor） (A, B, C) · β1 · β2 · β3 ... SL65.0155（英语：SL65.0155） - partial agonist. *CJ-033,466（英语：CJ-033,466） - partial agonist ... 腺苷酸（英语：Adenosine receptor） (A1, A2A, A2B, A3) · P2Y（英语：P2Y receptor） (1（英语：P2RY1）, 2（英语：P2RY2）, 4（英语：P2RY4）, 5（英语：LPAR6）, 6（英语： ... 乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺（英语：Dopamine receptor） (D1, D2, D3, D4, D5) · 组织胺（英语：Histamine receptor） (H1, H2, H3, H4) ·

https://zh.wikipedia.org/wiki/5-HT4受體

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 ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ... This forced receptor interaction induces the production of pro-inflammatory chemical signals (cytokines) by T-cells.[40] ...

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

Serotonin receptor agonists. *Serotonin-norepinephrine-dopamine releasing agents. *Substituted amphetamines. Hidden categories ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Adrenergic release blockers: Bethanidine. *Bretylium. * ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ...

https://en.wikipedia.org/wiki/3,4-methylenedioxy-N-ethylamphetamine

It is an alpha-2 adrenergic agonist that causes sedation and does have some analgesic properties. It has minimal effect on ... Midazolam[5] is a benzodiazepine that acts by stimulating inhibitory GABA receptors. Effects are seen within 2-5 minutes, and ... Propofol[5] is a non-barbiturate derivative that is thought to act by stimulating inhibitory GABA receptors and blocking ... It is phencyclidine that acts by partially blocking the NMDA receptors in the brain. Effects occur within 30 seconds, and last ...

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

... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... Further support for the monoamine hypothesis came from monoamine depletion studies: Alpha-methyl-p-tyrosine (AMPT) is a ... Data from clinical studies have shown that DA agonists, such as bromocriptine, pramipexole and ropinirole, exhibit ... These include receptor desensitization, alterations in intracellular transduction cascades and gene expression, the induction ...

https://en.wikipedia.org/wiki/Serotonin–norepinephrine–dopamine_reuptake_inhibitor

... of the adrenergic receptor system by increasing the activity of norepinephrine at the postsynaptic α and β receptors.[26] The ... as alpha-agonists such as ephedrine constrict the internal urethral sphincter, mimicking the effects of sympathetic nervous ... Pharmacological Effects of Ephedrine Alkaloids on Human {alpha}1- and {alpha}2-Adrenergic Receptor Subtypes Archived 2011-03-05 ... on adrenergic receptors.[26][27] It is most usually marketed as the hydrochloride or sulfate salt. ...

https://en.m.wikipedia.org/wiki/Ephedrine

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

https://en.m.wikipedia.org/wiki/Cannabis_dependence

0/Adrenergic alpha-Agonists; 0/Iodine Radioisotopes; 0/Receptors, Adrenergic, alpha; 108294-53-7/4-iodoclonidine; 146-48-5/ ... Adrenergic alpha-Agonists / pharmacokinetics*. Blood Platelets / metabolism*. Cell Membrane / metabolism. Chromatography, Thin ... 8267204 - Methylprednisolone increases sensitivity to beta-adrenergic agonists within 48 hours in.... 6147954 - Adrenergic ... Thus, PIC behaves as a partial agonist in a human platelet aggregation assay. [125I]PIC binds to the alpha 2B-AR in NG-10815 ...

http://www.biomedsearch.com/nih/p-125Iiodoclonidine-partial-agonist-at/1974694.html

Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or Preventing An ...

https://www.lens.org/lens/patent/EP_2329849_A1/family

Adrenergic Receptor Pharmacology for Medicine faster and easier with Picmonics unforgettable videos, stories, and quizzes! ... Alpha-2 Agonists (Sympathoplegics). Quiz. Picmonics rapid review multiple-choice quiz allows you to assess your knowledge. ... Clonidine activates α receptors, which causes inhibition of norepinephrine release from synaptic vesicles. Clonidine is ... The primary mechanism of action of alpha-2 agonists is stimulation of presynaptic alpha-2 receptors in the central nervous ...

https://www.picmonic.com/pathways/medicine/courses/standard/pharmacology-160/adrenergic-receptor-pharmacology-36140/alpha-2-agonists-sympathoplegics_1145

Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Endothelium receptor blockers[edit]. Bosentan belongs to a new class of drug and works by blocking endothelin receptors. It is ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ...

http://www.let.rug.nl/~gosse/termpedia2/termpedia.php?language=dutch_general&density=7&link_color=000000&termpedia_system=perl_db&url=http%3A%2F%2Fen.wikipedia.org%2Fwiki%2FAntihypertensive

TAGS: adrenergic alpha-2 receptor agonistsanxiety disordersclonidineguanfacinehumansposttraumaticstress disorderssympathetic ... Keywords: Adrenergic alpha-2 receptor agonists, anxiety disorders, clonidine, guanfacine, humans, stress disorders, ... Alpha-2 receptor agonists for the treatment of posttraumatic stress disorder. Drugs in Context 2015; 4:212286. DOI: 10.7573/dic ... This article specifically reviews the literature on alpha-2 receptor agonist use for the treatment of PTSD and concludes that ...

https://www.drugsincontext.com/alpha-2-receptor-agonists-for-the-treatment-of-posttraumatic-stress-disorder/

Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic alpha-2 Receptor Agonists. Hypnotics and Sedatives. Central Nervous System Depressants. Physiological Effects of ... Alpha 2 Agonists for Sedation to Produce Better Outcomes From Critical Illness (A2B Trial) (A2B). The safety and scientific ... Alpha 2 Agonists for Sedation to Produce Better Outcomes From Critical Illness (A2B Trial): A Randomised, Parallel-group, ...

https://www.clinicaltrials.gov/ct2/show/NCT03653832

This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. The most potent ... imidazoles was synthesized and evaluated for activity at alpha 1- and alpha 2-adrenoceptors. ... This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. The most potent ... imidazoles was synthesized and evaluated for activity at alpha 1- and alpha 2-adrenoceptors. ...

https://pubmed.ncbi.nlm.nih.gov/9016324/

... on human lymphocytes alpha adrenergic receptor density, Journal of Allergy and Clinical Immunology, vol. 69, no. 1 II. ... on human lymphocytes alpha adrenergic receptor density. In: Journal of Allergy and Clinical Immunology. 1982 ; Vol. 69, No. 1 ... on human lymphocytes alpha adrenergic receptor density. Journal of Allergy and Clinical Immunology. 1982 Jan 1;69(1 II). ... on human lymphocytes alpha adrenergic receptor density. Journal of Allergy and Clinical Immunology, 69(1 II). ...

https://creighton.pure.elsevier.com/en/publications/effect-of-fenoterol-beta-2-agonist-on-human-lymphocytes-alpha-adr/

Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts. ...

https://jpet.aspetjournals.org/content/273/2/689

Beta Adrenergic Receptor Blockers (Class II Antiarrhythmics). Özkaya, Esen (et al.). Pages 111-121 ... Alpha-2 Adrenergic Receptor Agonists. Özkaya, Esen (et al.). Pages 93-97 ... Apart from the well-known angioedema/urticaria from ACE inhibitors, lichen planus / lichenoid reaction from beta adrenergic ...

https://www.springer.com/us/book/9781447165354?wt_mc=

... on human lymphocytes alpha adrenergic receptor density. Together they form a unique fingerprint. * Sort by ... Fingerprint Dive into the research topics of Effect of fenoterol (beta-2 agonist) ... Effect of fenoterol (beta-2 agonist) on human lymphocytes alpha adrenergic receptor density. ...

https://creighton.pure.elsevier.com/en/publications/effect-of-fenoterol-beta-2-agonist-on-human-lymphocytes-alpha-adr/fingerprints/?sortBy=alphabetically

Alpha-2 adrenergic agonists.. Kamibayashi T, Harasawa K, Maze M.. Can J Anaesth. 1997 May;44(5 Pt 2):R13-22. Review. English, ... Systemically administered alpha2-agonist-induced peripheral vasoconstriction in humans.. Talke P, Lobo E, Brown R. ...

https://www.ncbi.nlm.nih.gov/pubmed?linkname=pubmed_pubmed_reviews&from_uid=12826844

N-Methyl-D-Aspartate Receptor Antagonists. * Calcium Channel Blockers. * Adenosine. * Cholinergic Agonists. ... Alpha-2 Adrenergic Agonists. * ... Chapter 2. Acute and Chronic Pain in the Elderly (Pradeep ...

https://www.routledge.com/Clinical-Management-of-the-Elderly-Patient-in-Pain/McCleane-Smith/p/book/9780789026200

Chapman, I. M. ; Willoughby, John O. / Interactions between the effects of opioid, serotonin and alpha-2-adrenergic receptor ... Combinations of clonidine, 6 and 30 μg/kg, and the serotonin agonist quipazine 160 μg/kg had an additive effect on GH release. ... Combinations of clonidine, 6 and 30 μg/kg, and the serotonin agonist quipazine 160 μg/kg had an additive effect on GH release. ... Combinations of clonidine, 6 and 30 μg/kg, and the serotonin agonist quipazine 160 μg/kg had an additive effect on GH release. ...

https://researchnow.flinders.edu.au/en/publications/interactions-between-the-effects-of-opioid-serotonin-and-alpha-2--2

https://en.wikipedia.org/wiki/Postural_orthostatic_tachycardia_syndrome?fbclid=IwAR2m8ZJtGrPxMde9Kcig0hirlDDwZlopEkcXtoRcEKOdsmSvNO64truK5qc

... derived receptors. α1, alpha-1 adrenergic receptor; α2C, alpha-2C adrenergic receptor; D2, dopamine receptor 2; DAT, dopamine ... receptor agonists. However, the first-generation 5-HT4 receptor agonists cisapride and tegaserod were withdrawn from the market ... 2004) The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol 143: ... Effects of 5-HT, 5-HT4 receptor agonists (prucalopride, tegaserod), 5-HT4 receptor antagonist SDZ 205-557, 5-HT2 receptor ...

http://jpet.aspetjournals.org/content/364/2/156

Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Subjects will be dosed orally once-daily in the AM at 1, 2, 3, 4, 5, 6, or 7 mg according to subjects weight and age ... This is an extension study that will allow participants access to Extended-release Guanfacine Hydrochloride (HCl) for up to 2 ... Final Assessment is the last valid assessment obtained after Baseline (Visit 2/Day 0) whilst on investigational product and ...

https://clinicaltrials.gov/show/NCT01500694

Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Dexmedetomidine, a highly selective arfa2-adrenergic agonist, is known to be a unique sedative agent which causes less acute ... A meta-analysis has shown that perioperative alfa2-adrenergic agonists, including dexmedetomidine infusion, decreased ... interleukin-6 and tumor necrosis factor alpha in endotoxemic rats. ...

https://www.clinicaltrials.gov/ct2/show/NCT01760967

Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Carbonic Anhydrase Inhibitors. ... Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... 1 drop of study medication taken approximately 12 hours apart, dosed 2 times a day for a total of two weeks ... 1 drop of study medication taken approximately 12 hours apart, dosed 2 times a day for a total of two weeks ...

https://clinicaltrials.gov/ct2/show/NCT00811850

Opioids possess agonist activity at the opioid receptors. The three current major classes of opioid receptors are mu, kappa, ... Suzanne White, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Clinical Toxicology, ... Numerous opioid agonists also exist; each has varying affinity for each receptor. Fentanyl and its derivatives (ie, sufentanil ... The primary action of benzodiazepines is agonist activity at the γ-aminobutyric acid (GABA)-associated benzodiazepine receptors ...

https://emedicine.medscape.com/article/834190-overview

Receptor, Serotonin, 5-HT2A / metabolism* * Receptors, Adrenergic, alpha-2 / metabolism * Receptors, Histamine H3 / metabolism ... receptor antagonists while a selective 5-HT(2B) receptor agonist and a selective 5-HT(2C) receptor agonist were without effect ... receptors because stress had no significant impact on other serotonin receptors, as well as histamine H(3) receptor and alpha(2 ... receptor agonist, to basolateral amygdala (BLA) slices dramatically enhanced frequency and amplitude of spontaneous inhibitory ...

https://pubmed.ncbi.nlm.nih.gov/18536707/

Combined alpha and beta-blockers. *Central agonists. *Peripheral adrenergic inhibitors. *Vasodilators. Diuretics. Diuretics ... Angiotensin needs a receptor- like a chemical "slot" to fit into or bind with- in order to constrict the blood vessel. ARBs ... Central agonists. Central agonists also help decrease the blood vessels ability to tense up or contract. The central agonists ... Some noted possible side effects of central agonists:. *Alpha methyldopa (Aldomet)* may produce a greater drop in blood ...

https://www.stroke.org/en/health-topics/high-blood-pressure/changes-you-can-make-to-manage-high-blood-pressure/types-of-blood-pressure-medications

... adrenergic receptor agonist, on human luteinized granulosa cells. In: Human Reproduction. 2005 ; Vol. 20, No. 11. pp. 3018-3025 ... adrenergic receptor agonist, on human luteinized granulosa cells, Human Reproduction, vol. 20, no. 11, pp. 3018-3025. ... adrenergic receptor agonist, on human luteinized granulosa cells. / Young, Fiona; Menadue, Margaret; Lavranos, Tina. ... adrenergic receptor agonist, on human luteinized granulosa cells",. author = "Fiona Young and Margaret Menadue and Tina ...

https://researchnow.flinders.edu.au/en/publications/effects-of-the-insecticide-amitraz-an-alpha2-adrenergic-receptor-

Prostaglandin F2-alpha analog. Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral ... A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. Has minimal ... Prostaglandin F2-alpha analog. Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral ... Selectively blocks beta 1-adrenergic receptors with little or no effect on beta 2-receptors. Reduces IOP by reducing production ...

https://emedicine.medscape.com/article/1207362-medication

Alpha-adrenergic agonist. 4-NEMD • Clonidine • Dexmedetomidine • Lofexidine • Medetomidine • Romifidine • Tizanidine • Xylazine ... GABAB receptor / GHB receptor. GHB Type. Aceburic acid • GABOB • GHB (Sodium Oxybate, Xyrem®) • GBL • 1,4-Butanediol. ... Histamine receptor &. Acetylcholine receptor. Antihistamines &. Anticholinergics. Doxylamine • Hydroxyzine • Diphenhydramine • ... Other receptors/. ungrouped. Aldehydes. Acetylglycinamide chloral hydrate • Chloral hydrate • Chloralodol • Dichloralphenazone ...

https://www.newworldencyclopedia.org/entry/Chloral_hydrate

Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...

http://www.biomedsearch.com/nih/Role-adrenergic-alpha-2-receptors/19233186.html

Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. These results suggest that [3H]rauwolscine ... 3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes. ...

https://www.ncbi.nlm.nih.gov/pubmed/6276200

Phenylephrine: Alpha1-adrenergic receptor agonist; it causes dilation of the pupil by contracting the radial muscle of the iris ... Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1- ... Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. ... Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. While linezolid is expected to interact ...

https://www.drugs.com/ppa/phenylephrine-and-ketorolac.html

... a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital-anesthetized rats ... Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to ... Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital- ... Pretreatment with the alpha 2-adrenoceptor antagonist rauwolscine (0.5 mg/kg, i.v.) blocked the bradycardia induced by ...

http://www.curehunter.com/public/pubmed9241327.do

Alpha1-adrenergic receptor agonists (phenylephrine). Case Outcome. The child was showing systemic effects from the mydriatic ... Alpha-2 receptor agonists (brimonidine). * ... and peripherally muscarinic receptor sites results in a ... However, recall that the sweat glands, while sympathetically innervated, utilize muscarinic receptors to signal for increased ... Medical Toxicology and Adverse Drug Experience, Volume 2 (4), 287-293. Lexi-Comp OnlineTM , Pediatric & Neonatal Lexi-Drugs ...

https://epmonthly.com/article/the-ocular-anticholinergic-crisis-a-startling-episode-with-an-inconsolable-hallucinating-two-year-old-highlights-a-rare-ocular-emergency/

125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] bromoxidine (UK14,304), which represented approximately 40% of the sites bound by the antagonist [3H]yohimbine. (biomedsearch.com)
Agonist-antagonist studies were performed in an attempt to further define these interactions. (edu.au)
The CC2 antagonist idazoxan (2 mg/kg i.v.) prevented release due to intravenous clonidine, morphine and quipazine, but not GH-releasing factor (GRF) 25 μg/kg. (edu.au)
The results of these agonist-antagonist studies do not provide a consistent explanation for the observed interactions. (edu.au)
This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (biomedsearch.com)
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. (nih.gov)
3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in bovine cerebral cortex. (nih.gov)
Pretreatment with the alpha 2-adrenoceptor antagonist rauwolscine (0.5 mg/kg, i.v.) blocked the bradycardia induced by mivazerol as well as the inhibitory effect of mivazerol on surgical stress-induced elevations in HR and BP. (curehunter.com)
Selected examples are: Clonidine (mixed alpha2-adrenergic and imidazoline-I1 receptor agonist) Dexmedetomidine Fadolmidine Guanfacine, (preference for alpha2A-subtype of adrenoceptor) Guanabenz (most selective agonist for alpha2-adrenergic as opposed to imidazoline-I1) Guanoxabenz (metabolite of guanabenz) Guanethidine (peripheral alpha2-receptor agonist) Xylazine, Tizanidine Medetomidine Methyldopa Methylnorepinephrine Norepinephrine (R)-3-nitrobiphenyline is an α2C selective agonist as well as being a weak antagonist at the α2A and α2B subtypes. (wikipedia.org)
Agonists 4-NEMD 7-Me-marsanidine (also I1 agonist) Agmatine (also I agonist, NMDA, 5-HT3, nicotinic antagonist and NOS inhibitor) Apraclonidine Brimonidine Cannabigerol (also acts as a moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist). (wikipedia.org)
What effect would an antagonist alone have on receptor activation? (brainscape.com)
A vasopressin antagonist that binds to the V2-receptor of LLC-PK, renal epithelial cells is highly laterally mobile but does not effect ligand-induced receptor immobilization. (springer.com)
PE responses were completely blocked by the alpha 1-antagonist prazosin (200 nM, n = 4 slices), but not by the alpha 2- antagonist yohimbine (n = 3 slices). (jneurosci.org)
Tolazoline is a non-selective competitive α-adrenergic receptor antagonist. (selleckchem.com)
Characterization with agonist and antagonist radioligands and relationship to adenylate cyclase. (aspetjournals.org)
The concentration-effect curve for UK and NE was shifted to the right by the alpha 2-antagonist yohimbine (10(-6) M), with new EC50 of 49.7 +/- 12.2 (p less than 0.001) nM and 10.3 +/- 22 nM. (jimmunol.org)
The presence of a MO alpha-adrenergic receptor was established by demonstrating binding of the alpha 2-adrenergic antagonist 3H-yohimbine to membranes prepared from MO. (jimmunol.org)

Among the most important and most widely used medications are thiazide diuretics , calcium channel blockers , ACE inhibitors , angiotensin II receptor antagonists (ARBs), and beta blockers . (rug.nl)
In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACE inhibitors , or angiotensin II receptor antagonists . (rug.nl)
The 8th Joint National Committee (JNC-8) recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with thiazide -type diuretics, ACE inhibitors , or angiotensin II receptor antagonists for all patients regardless of age or race. (rug.nl)
However, ACE inhibitors (and angiotensin II receptor antagonists) should not be a first-line treatment for black hypertensives without chronic kidney disease . (rug.nl)
These results indicate that in whole animal studies (I) additive or synergistic drug combinations cannot generally be predicted, (2) less than additive interactions of agonists regularly occur and (3) antagonists are unhelpful in dissecting the nature of the negative interactions. (edu.au)
This effect was blocked by selective 5-HT(2A) receptor antagonists while a selective 5-HT(2B) receptor agonist and a selective 5-HT(2C) receptor agonist were without effect on sIPSCs. (nih.gov)
Side effects of alpha 1 receptor antagonists? (brainscape.com)
The authors note the limited utility of NMDA receptor antagonists and alpha-2 adrenergic agonists. (lww.com)
Abandoning the old opioid-centric model, physicians are focusing more on nonsteroidal anti-inflammatories, acetaminophen, gabapentinoids, NMDA antagonists, alpha-2-agonists, and sodium and calcium channel blocking agents. (apsf.org)
The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. (patents.com)
Carprolactams as Potent CGRP Receptor Antagonists for the Treament of Migraine", Bioorg Med. (patents.com)
Carlos G. Musso and Jose Alfie, "Resistant Hypertension in the Elderly-Second Line Treatments: Aldosterone Antagonists, Central Alpha-Agonist Agents, Alpha-Adrenergic Receptor Blockers, Direct Vasodilators, and Exogenous Nitric Oxide Donors", Cardiovascular & Hematological Agents in Medicinal Chemistry (2014) 12: 170. (eurekaselect.com)

Hearts preconditioned with increasing concentrations of phenylephrine (an alpha-1 adrenergic receptor agonist) produced a reduction in the incidence of reperfusion-induced ventricular fibrillation (VF) and ventricular tachycardia (VT). (aspetjournals.org)
Following irrigation with diluted phenylephrine/ketorolac solution, plasma concentrations of phenylephrine were 1.2 to 1.4 ng/mL within 2 hours and plasma concentrations of ketorolac were 1 to 4.2 ng/mL within 8 hours. (drugs.com)
5. A method according to claim 1, wherein said alpha adrenergic receptor agonist is selected from the group consisting of epinephrine, norepinephrine, methoxamine, and phenylephrine. (freepatentsonline.com)
Although complete selectivity between receptor agonism is rarely achieved, phenylephrine is an α 1 agonist, while clonidine and methyldopa are α 2 partial agonists [1] . (wikidoc.org)
The alpha 1- agonist phenylephrine (PE) (10-100 microM) evoked complex [Ca2+]i signals (22 of 26 slices, 90 of 90 cells in responding slices) composed of both a prolonged component (5.1 +/- 1.8 min), synchronized in neighboring cells, and multiple, mainly asynchronous [Ca2+]i spikes (25.0 +/- 11.6 sec). (jneurosci.org)

Apart from the well-known angioedema/urticaria from ACE inhibitors, lichen planus / lichenoid reaction from beta adrenergic blockers and photosensitivity from thiazid diuretics, ACDR from CV drugs might be seen in a wide spectrum extending to rare but life-threatening conditions such as erythroderma, Stevens-Johnson syndrome, toxic epidermal necrolysis or drug hypersensitivity syndrome. (springer.com)
Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or oral), and alpha 2-agonists. (medscape.com)
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. (drugs.com)
Alpha-adrenergic agonists have the opposite function of alpha blockers. (wikipedia.org)
Brimonidine reduces intraocular pressure through a dual mechanism of action: reduction of aqueous humor production and increased uveoscleral outflow.2 Unlike beta-blockers, brimonidine is not contraindicated in patients with cardiopulmonary disorders. (swan.ac.uk)
Alpha blockers reduce resistance in the arteries and relax the muscle tone of the vascular walls. (nationaljewish.org)
Angiotensin II receptor blockers block angiotensin, a chemical in the body that narrows arteries, to keep the blood vessels open and reduce blood pressure. (nationaljewish.org)
An appropriate therapy for RH can be achieved by the addition of second line antihypertensive drugs: antialdosteronic diuretics, central agents, alpha blockers, direct vasodilating agents, and exogenous nitric oxide donors. (eurekaselect.com)

The stress-induced effect appeared to be specific to 5-HT(2A) receptors because stress had no significant impact on other serotonin receptors, as well as histamine H(3) receptor and alpha(2) adrenoceptor signaling in the BLA. (nih.gov)
Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to prevent adverse cardiac outcome in perioperative patients with, or at risk coronary artery disease . (curehunter.com)
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. (wikipedia.org)
α-2-ADRENOCEPTORS are known to mediate analgesia, and α-2-adrenoceptor agonists (such as clonidine) have proven effective in the treatment of pain, such as intractable cancer pain, 1,2 postsurgical pain, 3,4 and sympathetically maintained pain. (asahq.org)
Alfa-2 ( α 2 ) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje G i heterotrimerni G protein . (wikipedia.org)
ADRA2B (Adrenoceptor Alpha 2B) is a Protein Coding gene. (genecards.org)
These results support a primary role of NE release and alpha 1-adrenoceptor stimulation in neuron-astrocyte communication in the mature CNS. (jneurosci.org)
However, it may be effective in counteracting alpha-adrenoceptor-mediated vasospasm in human radial arteries. (selleckchem.com)

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. (drugs.com)
The chapter on other drugs used in acute pain highlights the utility of non-opioid adjuncts, emphasizes a practical approach, and introduces the concept of COX-2 inhibitors for acute pain management. (lww.com)
Peripheral adrenergic inhibitors block neurotransmitters in the brain from sending a message to the heart muscle telling it to constrict (have a heart attack). (nationaljewish.org)
Receptor Tyrosine Kinase Inhibitors," Current Opinion in Investigational Drugs, 2 (2):280-286 (2001). (patentgenius.com)

We investigated the α-adrenergic pharmacology of analgesia using models of tactile hypersensitivity induced with chemical stimuli that sensitize pain pathways at spinal or peripheral sites. (asahq.org)
Current Opinion in Pharmacology, 2:374-381 (2002). (patentgenius.com)

The primary mechanism of action of alpha-2 agonists is stimulation of presynaptic alpha-2 receptors in the central nervous system. (picmonic.com)
Our results show that alpha-1 adrenergic stimulation (preconditioning) can prevent postischemic abnormalities in intracellular ions, reperfusion arrhythmias, and contractile function without the inhibition of O2 delivery. (aspetjournals.org)
10 The primary mechanism of antinociception is the direct stimulation of the alpha-2-adrenoreceptors in the central nervous system and spinal cord. (apsf.org)
11 Direct stimulation of alpha-2-receptors also inhibits nociceptive neuronal firing, thereby reducing the release of substance P, a key excitatory neuropeptide responsible for painful responses. (apsf.org)
Stimulation-evoked release of 3H-norepinephrine was inhibited by the cholinergic agonists methacholine, oxotremorine, muscarine, carbamylcholine and acetylcholine (plus eserine), but was unmodified by pilocarpine or nicotine. (arvojournals.org)
Alpha1-adrenergic stimulation of phosphatidylinositol-phosphatidic acid turnover in rat parotid cells. (aspetjournals.org)
Stimulation of alpha-adrenergic receptor augments the production of macrophage-derived tumor necrosis factor. (jimmunol.org)

Dexmedetomidine, a highly selective arfa2-adrenergic agonist, is known to be a unique sedative agent which causes less acute tolerance, drug addiction and withdrawal compared with gamma-aminobutyrate (GABA) agonists. (clinicaltrials.gov)
Taniguchi and colleagues demonstrated that dexmedetomidine reduced high mortality rates and the plasma cytokine concentrations, interleukin-6 and tumor necrosis factor alpha in endotoxemic rats. (clinicaltrials.gov)
A meta-analysis has shown that perioperative alfa2-adrenergic agonists, including dexmedetomidine infusion, decreased cardiovascular events on patients undergoing cardiac surgery. (clinicaltrials.gov)
Medications such as clonidine and dexmedetomidine target pre-synaptic auto receptors, therefore leading to an overall decrease in norepinephrine which clinically can cause effects such as sedation, analgesia, lowering of blood pressure and bradycardia. (wikipedia.org)
Clonidine and other α-2 agonists used clinically (tizanidine, brimonidine and dexmedetomidine) activate to varying degrees three structurally distinct subtypes of the α-2 receptor: α-2A, α-2B, and α-2C. (asahq.org)
The two common alpha-2-agonists used in clinical practice today are clonidine and dexmedetomidine. (apsf.org)
11 Dexmedetomidine has a much higher affinity (approximately 8:1) than clonidine at the alpha-2 receptor site. (apsf.org)
In the Group RecDex, the administration of dexmedetomidine induced mild-moderate losses of mucosal architecture in the colon and rectum, 2 h after rectal inoculation. (scielo.br)
1 , 2 , 3 , 4 , 5 and 6 In addition to benzodiazepines such as midazolam, which are commonly used for this purpose, the use of alpha 2 agonists such as clonidine and dexmedetomidine is becoming popular. (scielo.br)
Dexmedetomidine is an alpha adrenergic agonist with high levels of specificity and selectivity to alpha 2 receptors. (scielo.br)
Specific Aim 2: Investigate the efficacy of dexmedetomidine for inducing sleep in a Phase II randomized double-blind placebo-controlled study. (bioportfolio.com)
Dexmedetomidine is an alpha-2 adrenergic agonist that is typically administered as an anesthetic adjunct. (bioportfolio.com)
Dexmedetomidine is thought to alter arousal primarily through its actions on pre-synaptic alpha-2A adrenergic receptors on neurons projecting from the LC. (bioportfolio.com)

Clonidine activates α receptors, which causes inhibition of norepinephrine release from synaptic vesicles. (picmonic.com)
Thus, serotonin primarily acts via 5-HT(2A) receptors to facilitate BLA GABAergic inhibition. (nih.gov)
This severe impairment of 5-HT(2A) receptor-mediated facilitation of BLA GABAergic inhibition might result in an amygdala circuitry with hyperexcitability, and a lower threshold of activation, and thus be an important mechanism underlying the emergence of stress-associated psychiatric symptoms. (nih.gov)
Inhibition of acetylcholine neurotransmission at its centrally nicotinic and muscarinic, and peripherally muscarinic receptor sites results in a constellation of symptoms that define the anticholinergic toxidrome. (epmonthly.com)
Folklore says that inhibition of a2 adrenergic receptors with Yohimbine treats what? (brainscape.com)
It is concluded that clonidine produces (or potentiates) analgesic effects of various drugs and that the analgesic effect of nitrous oxide is attributed to the effect on the central noradrenergic system, possibly by an activation of the descending inhibitory system and/or inhibition of the primary sensory afferent neuron via alpha-2 adrenergic receptors. (nii.ac.jp)
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (abcam.com)
Cholinergic inhibition of adrenergic neurosecretion in the rabbit iris-ciliary body. (arvojournals.org)
Agonist-induced inhibition was antagonized selectively by atropine, indicating a muscarinic response. (arvojournals.org)

Lucemyra (lofexidine) is a central alpha-2 adrenergic agonist. (centerwatch.com)
Zanaflex belongs to a class of drugs called Central Alpha-2-Adrenergic Agonist . (rxlist.com)
Zanaflex is a central alpha-2-adrenergic agonist indicated for the management of spasticity . (rxlist.com)
Lucemyra belongs to a group of drugs called central alpha-2 adrenergic agonists. (rxwiki.com)

PIC had minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, but it potentiated platelet aggregation induced by ADP with an EC50 of 1.5 microM. (biomedsearch.com)
The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
Jans DA, Peters R, Fahrenholz F. Lateral mobility of the phospholipase-C-activating vasopressin V,-type receptor in A7r5 smooth muscle cells: a comparison with the adenylate cyclase-coupled V2-receptor. (springer.com)
Vasopressin V2-receptor mobile fraction and ligand-dependent adenylate cyclase-activity are directly correlated in LLC-PK, renal epithelial cells. (springer.com)
Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (springer.com)
Tolkovsky AM, Levitzki A. Coupling of a single adenylate cyclase to two receptors: adenosine and catecholamine. (springer.com)
Tolkovsky A, Braun S, Levitzki A. Kinetics of interaction between 3-receptors, GTP-proteins and the catalytic subunit of turkey erythrocyte adenylate cyclase. (springer.com)
Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)

ergotamine etilefrine indanidine mephentermine metaraminol methoxamine mivazerol naphazoline norfenefrine octopamine phenylpropanolamine propylhexedrine rilmenidine romifidine synephrine talipexole Alpha-adrenergic agonists, more specifically the auto receptors of alpha 2 neurons, are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary bodies of the eye and also by increasing uveoscleral outflow. (wikipedia.org)
10 At the cellular level, alpha-2-agonists inhibit cyclic adenosine monophosphate, which reduces potassium efflux and calcium influx causing a hyperpolarized state of the adrenergic neurons. (apsf.org)
This protein is a member of a subfamily of G protein-coupled receptors that regulate neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (nih.gov)

Clonidine and guanfacine are alpha-2 receptor agonists that decrease sympathetic outflow from the central nervous system. (drugsincontext.com)
This is an extension study that will allow participants access to Extended-release Guanfacine Hydrochloride (HCl) for up to 2 years. (clinicaltrials.gov)
Furthermore, we addressed whether guanfacine, an α 2 -adrenergic agonist that reduces stress-triggered maladaptive behavioral responses to drugs of abuse, could relief from SDPS-induced anhedonia. (frontiersin.org)

Drugs of this class are used to treat hypertension, as they reduce peripheral resistance by stimulating postsynaptic α 2 adrenoreceptors in the central nervous system. (picmonic.com)
Systemically administered alpha2-agonist-induced peripheral vasoconstriction in humans. (nih.gov)
Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central and peripheral nervous systems. (wikipedia.org)

Tolazoline has moderate alpha-adrenergic blocking activity and has histamine agonist activity. (selleckchem.com)
Pharmacological characterization of histamine receptors mediating the elevation of cyclic AMP. (aspetjournals.org)

Stimulates alpha-adrenergic receptors in CNS, decreasing sympathetic outflow, inhibiting vasoconstriction, and ultimately reducing blood pressure. (thefreedictionary.com)
It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. (hmdb.ca)
Xylometazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion. (hmdb.ca)

Selective alpha 2-receptor that reduces aqueous humor formation and increases uveoscleral outflow. (medscape.com)
Lucemyra is an oral, selective alpha 2-adrenergic receptor agonist that reduces the release of norepinephrine. (fda.gov)

however, the α-2A subtype has also been associated with dose-dependent sedation and decreased blood pressure, thus narrowing the therapeutic window of α-2 agonists when used clinically for analgesic activity. (asahq.org)

α 2 agonists are a class of medication which act on α 2 adrenergic receptors to yield a decreased sympathetic outflow centrally. (picmonic.com)
Drugs of this class are centrally acting and decrease sympathetic outflow, as they activate medullary presynaptic α 2 adrenoceptors. (picmonic.com)
Remember that α 2 activation decreases sympathetic outflow. (picmonic.com)
The α2-adrenergic receptor binds both norepinephrine released by sympathetic postganglionic fibers and epinephrine (adrenaline) released by the adrenal medulla, binding norepinephrine with slightly higher affinity. (wikipedia.org)
The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. (hmdb.ca)

What Brimonidine Tartrate/Timolol Eye Drops, Solution is and what it is used for 2. (drugs.com)
Brimonidine Tartrate/Timolol should not be used in children less than 2 years old and should not usually be used in children aged 2 to 17. (drugs.com)
4. The implant of claim 1, wherein the alpha-2 adrenergic receptor agonist is brimonidine tartrate. (freepatentsonline.com)
Chemically, brimonidine tartrate is 5-Bromo-6-(2-imidazolidinylideneamino) quinoxaline L-tartrate. (swan.ac.uk)

Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous humor production and possibly increases outflow of aqueous humor. (medscape.com)
Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral outflow. (medscape.com)
Early treatment and management of glaucoma, which predominantly involves the lowering of intraocular pressure, is critical since glaucoma is considered to be a common cause of blindness worldwide.2,6, Ophthalmically, brimonidine is used to lower intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow. (swan.ac.uk)

Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. (wikipedia.org)
Brimonidine is more selective for the α-2 adrenoreceptor. (swan.ac.uk)
There are very few studies using an alpha-2 adrenoreceptor agonist clonidine in ophthalmic blocks, and these have shown contradictory results. (ispub.com)

Further research to define the role of various alpha receptor subtypes is needed to identify strategies for separating the analgesic and sedative effects of α-2 agonists. (asahq.org)
Adrenergic alpha2 receptors are divided into three subtypes in humans: alpha2A, alpha2B and alpha2C. (genecards.org)
Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. (aspetjournals.org)

Xylometazoline Oxymetazoline Apraclonidine[citation needed] Cirazoline Epinephrine The following agents are also listed as agonists by MeSH. (wikipedia.org)

There are two other drugs used less often called 'alpha-2 agonists' that have both sedative and pain-killing actions, which may make it easier for patients to be more awake and comfortable on the ventilator. (clinicaltrials.gov)
The investigators want to know whether starting an alpha2-agonist drug early in ICU, and using this instead of propofol as much as possible, can help keep patients more lightly sedated but still comfortable, and whether patients spend less time on the ventilator with these drugs. (clinicaltrials.gov)
However, the first-generation 5-HT 4 receptor agonists cisapride and tegaserod were withdrawn from the market owing to rare cardiovascular adverse events that were not 5-HT 4 -receptor-related but due to the lack of selectivity of these drugs. (aspetjournals.org)
Alpha 2 -adrenergic agonists are the first line of pharmacologic therapy, but dopamine-receptor-blocking drugs are required for multiple, complex tics. (aafp.org)
Dopamine-receptor-blocking drugs are associated with potential side effects including sedation, weight gain, acute dystonic reactions, and tardive dyskinesia. (aafp.org)
Alpha 2 -adrenergic agonists are useful in treating patients with Tourette's syndrome, although they improve tics to a lesser degree than dopamine-receptor-blocking drugs. (aafp.org)
Dopamine-receptor-blocking drugs are the most effective treatment for tics. (aafp.org)
Since G protein coupled receptors (GPCRs) are target of forty percent of clinically used drugs, here we discuss the newly identified cardioprotective agents that bind GPCRs of adrenalin, adenosine, melatonin, ghrelin, galanin, apelin, prokineticin and cannabidiol. (frontiersin.org)
However, most of the anticancer drugs display a wide array of cardiovascular toxicities, leading to interruption of cancer therapies and maladaptive remodeling in hearts, affecting the short- and long-term quality of life ( 2 - 4 ). (frontiersin.org)
Second line drugs are also used when there is allergy or intolerance to the first line ones [2, 3]. (eurekaselect.com)
Causes contributing to harmful drug?drug interactions include narrow therapeutic dosage ranges associated with certain drugs and a patient?s disease state (Tables 1 and 2). (pharmacytimes.com)

The investigators want to know whether starting an alpha2-agonist drug early in ICU can help keep patients more lightly sedated but still comfortable, and whether patients spend less time on the ventilator. (clinicaltrials.gov)

Xylazine is a potent α2 (Alpha 2) adrenergic agonist, and is classified as a sedative and analgesic. (wikihow.com)

[1] [2] Its sedative properties were first published in 1869 and subsequently, because of its easy synthesis, it was widely used. (newworldencyclopedia.org)

Thus, PIC behaves as a partial agonist in a human platelet aggregation assay. (biomedsearch.com)
Apparent "down-regulation" of human platelet alpha 2-adrenergic receptors is due to retained agonist. (aspetjournals.org)

125I]PIC binds to the alpha 2B-AR in NG-10815 cell membranes with a Kd of 0.5 +/- 0.1 nM. (biomedsearch.com)
These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes. (nih.gov)
This product is an aliquot of membranes from Sf9 cells transfected with the human recombinant alpha 2a Adrenergic Receptor. (abcam.com)

Lucemyra binds to specific receptors in the brain and decreases norepinephrine release. (rxwiki.com)

p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor. (biomedsearch.com)
Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. (wikipedia.org)

Beta-adrenergic blocker that has little or no intrinsic sympathomimetic effects and membrane-stabilizing activity. (medscape.com)
Blocks beta 1- and beta 2-receptors and has mild intrinsic sympathomimetic effects. (medscape.com)
Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. (wikipedia.org)
Xylometazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. (hmdb.ca)

[2] There are many classes of antihypertensives, which lower blood pressure by different means. (rug.nl)

Agonists (activators) of the α2-adrenergic receptor are frequently used in veterinary anaesthesia where they affect sedation, muscle relaxation and analgesia through effects on the central nervous system (CNS). (wikipedia.org)
5 However, the systemic use of α-2 agonists for long-term analgesia has been limited by a narrow therapeutic window due to the potential for sedation and cardiovascular depression. (asahq.org)

Here we report the nonclinical cardiovascular profile of the selective 5-HT 4 receptor agonist prucalopride. (aspetjournals.org)
To assess its non-5-HT 4 receptor-mediated effects on cardiovascular electrophysiological parameters, in vitro studies were performed in human ether-à-go-go-related gene-transfected cells, guinea pig ventricular myocytes and papillary muscle preparations, rabbit and dog Purkinje fibers, and the Langendorff rabbit heart. (aspetjournals.org)
Prucalopride may thus provide therapeutic benefit without the cardiovascular risks reported for other 5-HT 4 receptor agonists. (aspetjournals.org)
Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital-anesthetized rats. (curehunter.com)

a dopamine receptor agonist sodium oxybate (Jazz), and a neuromuscular blocking agent botulinum toxin A (Allergan). (massagemag.com)

However, recall that the sweat glands, while sympathetically innervated, utilize muscarinic receptors to signal for increased perspiration. (epmonthly.com)
Muscarinic cholinergic receptors on cultured thyroid cells. (aspetjournals.org)

2 Given the concern that abuse sometimes starts with opioids prescribed in the course of medical care, health care systems throughout the world have adopted a multimodal approach to acute and chronic pain management to reduce opioid prescriptions. (apsf.org)
Study 1 was a 2-part efficacy, safety, and dose-response study conducted in the United States in patients meeting DSM-IV criteria for opioid dependence who were physically dependent on short-acting opioids (e.g., heroin, hydrocodone, oxycodone). (centerwatch.com)

It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (biomedsearch.com)

Selectively blocks beta 1-adrenergic receptors with little or no effect on beta 2-receptors. (medscape.com)
An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors . (wikidoc.org)

Atropine alone markedly enhanced norepinephrine release, revealing considerable tonic activation of prejunctional cholinergic receptors in this system. (arvojournals.org)

α1 agonist: stimulates phospholipase C activity. (wikipedia.org)

Discontinue Lucemyra with a gradual dose reduction over a 2- to 4-day period to mitigate Lucemyra withdrawal symptoms. (centerwatch.com)
Lucemyra may reduce the effectiveness of oral naltrexone if used within 2 hours of each other. (rxwiki.com)

Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. (drugs.com)
2. The implant of claim 1, wherein the alpha-2 adrenergic receptor agonist is selected from the group consisting of quinoxalines, (2-imidozolin-2-ylamino) quinoxalines, 5-bromo-6-(2-imidozolin-2-ylamino) quinoxalines, derivatives thereof and mixtures thereof. (freepatentsonline.com)

Cholinergic and alpha 2-adrenergic effects on neurosecretion were non-additive, suggesting that the underlying receptors coexist at neurotransmitter release sites. (arvojournals.org)

Blockade of a2 receptors increases what? (brainscape.com)
NE (2-100 microM) evoked [Ca2+]i increases (7 of 8 slices, 24 of 24 cells in responding slices) characterized by an initial rise, 20-50 sec to peak, followed by a slower return to baseline (over approximately 8 min). (jneurosci.org)
The metabotropic agonist t-ACPD (30 or 50 microM) did not increase astrocytic [Ca2+]i in hippocampal slices (0 of 5), while kainate (200 microM or 1 mM) induced brief (1-2 min) [Ca2+]i increases only rarely (2 of 8 applications in 6 slices). (jneurosci.org)
Incorporation of G alpha z-Specific Sequence at the Carboxyl Terminus Increases the Promiscuity of Galpha16 toward Gi-coupled Receptors. (patentgenius.com)
Dosage can be gradually increased by 2 mg to 4 mg at each dose, with 1 to 4 days between dosage increases, until a satisfactory reduction of muscle tone is achieved. (rxlist.com)

Alpha-2 receptor agonists decrease adrenaline production in the involuntary nervous system, which lowers blood pressure. (nationaljewish.org)
Central agonists decrease tensing and contractions in the blood vessels to reduce blood pressure. (nationaljewish.org)
16 ] used 2 µg/kg clonidine with 2% lidocaine for retrobulbar block and found increased duration of analgesia and akinesia with a decrease in intraocular pressure and recommended its use. (ispub.com)

alpha-2 and imidazoline receptor agonists. (nih.gov)

A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. (medscape.com)

NB: the inclusion of a drug in each category just indicates the activity of the drug at that receptor, not necessarily the selectivity of the drug (unless otherwise noted). (wikipedia.org)

Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM, KD = 2.5 nM, Bmax = 160 fmol/mg protein) and competition studies indicated that [3H]rauwolscine labeled the alpha 2-receptor. (nih.gov)
Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (springer.com)
Schlessinger J. The epidermal growth factor receptor as a multifunctional allosteric protein. (springer.com)
Belongs to the G-protein coupled receptor 1 family. (abcam.com)
GO annotations related to this gene include G-protein coupled receptor activity and alpha2-adrenergic receptor activity . (genecards.org)
Adrenergic alpha2 receptors (alpha2-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes alpha1A, alpha1B, alpha1D, beta1, beta2 and beta3. (genecards.org)
Functional Characterization of a Series of Mutant G Protein alpha q Subunits Displaying Promiscuous Receptopr Coupling Properties. (patentgenius.com)
G Protein Diversity: A Distinct Class of alpha Subunits isPresent in Vertibrates and Invertebrates. (patentgenius.com)
sub.q protein variants that functionally couple to sensory cell receptors such as taste GPCRs (TRs) and olfactory GPCRs (ORs) in an overly promiscuous manner. (patentgenius.com)
This invention relates to G.alpha.q protein variants and their use in the analysis and discovery of agonists and antagonsists of chemosensory receptors, such as G protein coupled receptors involved in sensing of tastants, olfactants, andpheromones. (patentgenius.com)
Heterotrimeric G proteins, consisting of alpha, beta and gamma subunits, couple ligand-bound seven transmembrane domain receptors (GPCRs or G-protein coupled receptors) to the regulation of effector proteins and production of intracellular secondmessengers such as cAMP, cGMP, and Ca.sup.2+. (patentgenius.com)
subunits also contribute to the specificity of receptor-G protein coupling (Xuet al. (patentgenius.com)

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)

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