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*  Alpha-2B adrenergic receptor
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 ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in ...
*  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) ...
*  Phentolamine
... (Regitine) is a reversible nonselective α-adrenergic antagonist. Its primary action is vasodilation due to α1 ... In response, the β1 adrenergic receptors on the heart increase its rate, contractility, and dromotropy, which help to offset ... as they can cause unopposed α-adrenergic mediated coronary vasoconstriction, worsening myocardial ischemia and hypertension. It ...
*  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 ...
*  Heart failure
Beta-adrenergic blocking agents (beta blockers) also form part of the first line of treatment, adding to the improvement in ... Mineralocorticoid antagonists in those under 75 years old appear to decrease the risk of death. A recent Cochrane review found ... In people with markedly reduced ejection fraction, the use of an aldosterone antagonist, in addition to beta blockers and ACE-I ... For those with severe disease, aldosterone antagonists, or hydralazine with a nitrate may be used. Diuretics are useful for ...
*  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 ...
*  History of catecholamine research
J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... Lastly, Ahlquist failed to adduce the selectivity of all antagonists known at his time for the α-adrenoceptor as an additional ... It is suggested that this terminology be extended to the realm of adrenergic blocking drugs, e.g., that blocking drugs be ... doi:10.1016/0165-6147(91)90587-I. C. E. Powell; I. H. Slater (1958). "Blocking of inhibitory adrenergic receptors by a dichloro ...
*  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 ...
*  Methylergometrine
... is a partial agonist/antagonist on serotonergic, dopaminergic and alpha-adrenergic receptors. Its specific ... dopaminergic and adrenergic receptors". In Vladimír Křen,Ladislav Cvak. Ergot: the genus Claviceps. CRC Press. pp. 411-440. ...
*  Pelanserin
... is an antagonist of the 5-HT2 and α1-adrenergic receptors. Villalobos-Molina, R; Ibarra, M; Hong, E (1995). "The 5- ... HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro". European Journal of ...
*  Cannabinoid
It acts as an α2-adrenergic receptor agonist, 5-HT1A receptor antagonist, and CB1 receptor antagonist. It also binds to the CB2 ... It is an antagonist of THC at CB1 receptors and attenuates the psychoactive effects of THC. Although cannabidivarin (CBDV) is ... Although it is a full agonist at CB2 and a partial agonist at CB1, it behaves as a CB1 antagonist in vivo. In rats, virodhamine ... It was found to be an antagonist at the putative new cannabinoid receptor, GPR55, a GPCR expressed in the caudate nucleus and ...
*  Apomorphine
... and as an antagonist at 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, α1-adrenergic, and α2-adrenergic. Though its efficacies at D1 ... It also acts as an antagonist of 5-HT2 and α-adrenergic receptors with high affinity. The compound is historically a morphine ... Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal ... Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes". The Journal of Pharmacology and ...
*  Paliperidone
... has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors. It does not bind to ... Paliperidone, sold under the trade name Invega among others, is a dopamine antagonist and 5-HT2A antagonist of the atypical ...
*  Yohimbine
It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a partial agonist ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... "Regulation of pre-synaptic alpha adrenergic activity in the corpus cavernosum". International Journal of Impotence Research. 12 ...
*  Metitepine
It acts as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors and has antipsychotic properties. ...
*  Antiarrhythmic agent
... reduced beta-adrenergic and potassium channel antagonist activities of sotalol in the presence of acute and chronic ... However, in contrast to beta blockers, they allow the body to retain adrenergic control of heart rate and contractility. Class ... They act by blocking the effects of catecholamines at the β1-adrenergic receptors, thereby decreasing sympathetic activity on ... examples included bretylium and adrenergic beta-receptors blocking drugs. This is similar to the modern classification, which ...
*  Alpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 2004). "Cell surface expression of alpha1D-adrenergic receptors is controlled by heterodimerization with alpha1B-adrenergic ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
*  Imiloxan
It acts as a selective antagonist for the α2B adrenergic receptor, and has been useful for distinguishing the actions of the ... Michel AD, Loury DN, Whiting RL (March 1990). "Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist". British ... alpha.2-adrenoceptor antagonists". Journal of Medicinal Chemistry. 25 (6): 666-70. doi:10.1021/jm00348a012. PMID 6124635. ... different α2 adrenergic subtypes. The imidazole portion of imiloxan is prepared by the reaction of an imidate with the diethyl ...
*  Alfuzosin
As an antagonist of the α1 adrenergic receptor, it works by relaxing the muscles in the prostate and bladder neck, making it ...
*  Gepirone
... which is known to act as a potent antagonist of the α2-adrenergic receptor. Gepirone was originally developed by Bristol-Myers ...
*  Receptor theory
Optimal Agonist/Antagonist Combinations Maintain Receptor Response by Preventing Rapid β-adrenergic Receptor Desensitization , ... Whereas antagonists have no preference in their affinity for a receptor state. The fact that receptor conformation (state) ... The del Castillo-Katz mechanism divorces the binding step (that can be made by agonists as well as antagonists) from the ... It was Heinz Otto Schild who made measurement of the equilibrium constant for the binding of an antagonist possible. He ...
*  Chlorophenylbiguanide
... is an allosteric agonist and modulator of the 5-HT3 receptor and an antagonist of the α2A-adrenergic receptor. It has ...
*  5-HT2A receptor
... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ... Other antagonists are MDL-100,907 (prototype of another new series of 5-HT2A antagonists) and cyproheptadine. Pizotifen is a ... Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. Mirtazapine is a 5-HT2A, 5-HT2C ... Although ergot alkaloids are mostly nonspecific 5-HT receptor antagonists, a few ergot derivatives such as metergoline bind ...
*  Pukateine
... with the most prominent effects being as an agonist at the D2 dopamine receptor and antagonist at the α1-adrenergic receptor. ...
*  Esmirtazapine
... including inverse agonist actions at H1 and 5-HT2 receptors and antagonist actions at α2-adrenergic receptors. As of March 2010 ...
*  Vasoactivity
Various vasoactive agents, such as prostanoids, phosphodiesterase inhibitors, and endothelin antagonists, are approved for the ... Important vasoactive substances are angiotensin-11, endothelin-1, and alpha-adrenergic agonists. ...
*  Dopamine receptor D4
... α-adrenergic and serotonergic weak antagonist A-381393: potent, subtype selective antagonist (>2700-fold) FAUC 213 L-745,870 L- ... Lanig H, Utz W, Gmeiner P (April 2001). "Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[ ... selective and competitive antagonist at dopamine D4 receptors: an in vitro and in vivo comparison with L 745,870 (3-(4-[4- ... an antagonist with high affinity and selectivity for the human dopamine D4 receptor". Journal of Medicinal Chemistry. 39 (10): ...