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*  ICI-118,551
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 ... Mauriège P, De Pergola G, Berlan M, Lafontan M (May 1988). "Human fat cell beta-adrenergic receptors: beta-agonist-dependent ... and characterization of beta-adrenergic binding sites on human fat cell membranes with highly selective beta-1 antagonists". ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
*  Sympatholytic
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... ICI-118,551 Highly selective β2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ... ganglion type receptor antagonist) Peripherally acting Guanethidine (Magnesium-ATPase inhibitor) Indoramin (α1 antagonist) ...
*  Alpha-1D adrenergic receptor
Antagonists A-315456 BMY 7378 (also α2C antagonist) Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000171873 - Ensembl, ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... 2004). "Cell surface expression of alpha1D-adrenergic receptors is controlled by heterodimerization with alpha1B-adrenergic ...
*  Penbutolol
... is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Like propanolol and pindolol, it is a serotonin 5-HT1A and 5-HT1B receptor antagonist; this discovery by several groups in the ... Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ... Blocking β adrenergic receptors decreases the heart rate and cardiac output to lower arterial blood pressure. β blockers also ...
*  Butriptyline
... moderate 5-HT2 and α1-adrenergic receptor antagonist, and very weak or negligible monoamine reuptake inhibitor. These actions ... despite the fact that both of these TCAs are far stronger as both 5-HT2 antagonists and serotonin-norepinephrine reuptake ... so is associated with little to no antiadrenergic and adrenergic side effects.[additional citation(s) needed] In vitro, ...
*  Aptazapine
It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been ... January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences. 32 (4): 355-63. doi:10.1016 ... shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the ...
*  Tramadol
... tramadol's analgesic effects are also partially reversed by α2-adrenergic receptor antagonists like yohimbine, the 5-HT3 ... receptor antagonist M1 and M3 muscarinic acetylcholine receptor antagonist α7 nicotinic acetylcholine receptor antagonist NMDA ... In accordance, the 5-HT3 receptor antagonist metoclopramide can be used to treat tramadol-associated nausea and vomiting. ... receptor antagonist ondansetron, and the 5-HT7 receptor antagonists SB-269970 and SB-258719. Pharmacologically, tramadol is ...
*  Para-Fluorophenylpiperazine
pFPP was originally discovered as a metabolite of the hypnotic 5-HT2A and α1-adrenergic receptor antagonist niaprazine in 1982 ...
*  Alpha-2C adrenergic receptor
R)-3-Nitrobiphenyline (also weak antagonist at α2A and α2B) BMY 7378 (also α1D antagonist) JP-1302: selective over α2A, α2B, ... The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes ... a selective alpha2C adrenergic receptor antagonist". Bioorg. Med. Chem. Lett. 18 (20): 5689-93. doi:10.1016/j.bmcl.2008.08.055 ... Park JS, Zhang SY, Jo SH, Seo JB, Li L, Park KW, Oh BH, Park YB, Kim HS (2006). "Common adrenergic receptor polymorphisms as ...
*  Atomoxetine
... but could be potentiated by NMDA or an α1-adrenergic receptor antagonist, suggesting a glutamatergic mechanism. In Sprague ... to increase prefrontal cortex firing rate in anesthetized rats could not be blocked by D1 or α2-adrenergic receptor antagonists ... acting as an antagonist at μ-opioid receptors and a partial agonist at κ-opioid receptors. It is not known whether this ... Atomoxetine has been found to act as an NMDA receptor antagonist in rat cortical neurons at therapeutic concentrations. It ...
*  WB-4101
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... 1969 Mar;12(2):326-9. PMID 5791620 Morrow AL, Creese I. Characterization of alpha 1-adrenergic receptor subtypes in rat brain: ... Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? Farmaco. 1998 Apr;53(4):278-86. ... Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety. Pharmaceutica Acta Helvetiae. 2000 Mar;74(2- ...
*  Isamoltane
It acts as an antagonist at the β-adrenergic, 5-HT1A, and 5-HT1B receptors. It has about five times the potency for the 5-HT1B ... a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain". Naunyn Schmiedebergs Arch Pharmacol. 343 (1 ...
*  Alpha-1 adrenergic receptor
Various heterocyclic antidepressants and antipsychotics are α1-adrenergic receptor antagonists as well. This action is ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... Adrenergic receptor Graham, Robert (May 1, 1996). "α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ...
*  Sympathoadrenal system
In such cases, curative agents such as adrenergic agonists and antagonists are used to modify epinephrine and norepinephrine ...
*  Buspirone/testosterone
... α2-adrenergic receptor antagonist, and D2 autoreceptor antagonist, and testosterone, an androgen or androgen receptor agonist, ...
*  Mepiprazole
It acts as a 5-HT2A and α1-adrenergic receptor antagonist and inhibits the reuptake and induces the release of serotonin, ... Cohen ML, Fuller RW, Kurz KD (1983). "Evidence that blood pressure reduction by serotonin antagonists is related to alpha ... dopamine, and norepinephrine to varying extents, and has been described as a serotonin antagonist and reuptake inhibitor (SARI ...
*  5-HT1A receptor
The sympatholytic antihypertensive drug urapidil is an α1-adrenergic receptor antagonist and 5-HT1A receptor agonist, and it ... Lorens SA, Van de Kar LD (1987). "Differential effects of serotonin (5-HT1A and 5-HT2) agonists and antagonists on renin and ... Consequently, novel NK1 receptor antagonists are now in use for the treatment of nausea and emesis, and are also being ... Conversely, 5-HT1A receptor antagonists such as lecozotan have been shown to facilitate certain types of learning and memory in ...
*  List of investigational sexual dysfunction drugs
... nicotinic acetylcholine receptor antagonist, 5-HT2A receptor antagonist, α1-adrenergic receptor antagonist, weak serotonin ... oxytocin receptor antagonist [22] OnabotulinumtoxinA (botulinum toxin A, Botox) - acetylcholine release inhibitor[23] Tramadol ... and 5-HT2C receptor antagonist [24] Vilazodone (Viibryd, EMD-68843, SB-659746A) - 5-HT1A receptor partial agonist and serotonin ...
*  Setiptiline
... acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, ...
*  Fluparoxan
... beta-adrenergic, muscarinic or 5-HT1-receptor-blocking effects. Fluparoxan showed α2-adrenoceptors antagonist activity in vivo ... pyrrole hydrochloride hemihydrate is a potent α2-adrenergic receptor antagonist (pKB = 7.9) with excellent α2/α1 selectivity ( ... It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an ... The same is true for other α2-adrenoceptor antagonists in depression and it is now generally agreed that the original ...
*  S32212
It behaves as a selective, combined 5-HT2C receptor inverse agonist and α2-adrenergic receptor antagonist (at all three ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ... and lacks any apparent affinity for the monoamine reuptake transporters or for the α1-adrenergic, H1, or mACh receptors. This ...
*  Fear processing in the brain
... beta-adrenergic receptor antagonist) prevented the behavioral changes following repeated stressor exposure thus halting long ... Recent studies have demonstrated that the blockade of norepinephrine β-adrenergic receptors (β-ARs) in the lateral nucleus of ... Blockade by Infusion of an NMDA Antagonist into the Amygdala". The Journal of Neuroscience. 12 (3): 854-63. PMID 1347562. ... region's neurons that received auditory inputs also received unconditioned stimulus inputs and broad spectrum NMDAR antagonists ...
*  Beta blocker
Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, ... β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are located mainly in the ... β3-adrenergic receptors are located in fat cells. Beta receptors are found on cells of the heart muscles, smooth muscles, ... Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta ...
*  Buspirone
... and is known to act as a potent α2-adrenergic receptor antagonist. It may be responsible for the increased noradrenergic and ... Borsini F, Giraldo E, Monferini E, Antonini G, Parenti M, Bietti G, Donetti A (1995). "BIMT 17, a 5-HT2A receptor antagonist ... In addition to binding to serotonin receptors, buspirone is an antagonist of the dopamine D2 receptor with weak affinity. It ... However, buspirone has been reported to have shown "significant and selective intrinsic efficacy" at the α1-adrenergic receptor ...
*  Rhinitis medicamentosa
Adrenergic Agonists and Antagonists, McGraw-Hill, New York. Passali D, Salerni L, Passali G, Passali F, Bellussi L (2006) Nasal ... Adrenergic Agonists and Antagonists, McGraw-Hill, New York. Elwany SS, Stephanos WM: Rhinitis medicamentosa. An experimental ... Lacroix J (1989) Adrenergic and nonadrenergic mechanisms in sympathetic vascular control of the nasal mucosa. Acta Physiol ... Direct acting sympathomimetic amines, such as phenylephrine stimulate alpha adrenergic receptors, while mixed-acting agents, ...
*  Idazoxan
It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor. Idazoxan has ...
*  Alpha-2 blocker
α2-blockers are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ... Haapalinna A, Leino T, Heinonen E (November 2003). "The alpha 2-adrenoceptor antagonist atipamezole potentiates anti- ...