Alpha-1 adrenergic receptor - Wikipedia
Piascik, M. T.; Perez, D. M. (2001). "Alpha1-adrenergic receptors: New insights and directions". The Journal of Pharmacology ... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ...https://en.wikipedia.org/wiki/Alpha-1_adrenergic_receptor
Alpha-1-Adrenergic Receptor Subtypes in Non-Failing and Failing Human Myocardium
Nishino Y, Masue T, Miwa K, Takahashi Y, Ishihara S, Deguchi T. Comparison of two alpha1-adrenoceptor antagonists, naftopidil ... expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun ... Alpha1-adrenergic receptor subtype mRNAs are differentially regulated by alpha1-adrenergic and other hypertrophic stimuli in ... Transgenic mice with cardiac overexpression of alpha1B-adrenergic receptors. In vivo alpha1-adrenergic receptor-mediated ...http://pubmedcentralcanada.ca/pmcc/articles/PMC2780440/?lang=en-ca
Phencyclidine-Induced Deficits in Prepulse Inhibition of Startle are Blocked by Prazosin, an Alpha-1 Noradrenergic Antagonist |...
... dopaminergic and serotonergic receptors compared with adrenergic receptors (Bymaster et al., 1996), produces a robust blockade ... The antagonists foralpha-2, for M1 and for GABA-A receptors had no effect on base-line PPI or on PCP-induced disruptions in PPI ... Finally, selective antagonists for eitheralpha-2 (RX821002), muscarinic M1 (pirenzepine) or GABA-A (pitrazepin) receptors had ... In contrast to the results with prazosin, selective antagonists foralpha-2, M1 and GABA-A receptors failed to affect PCP- ...http://jpet.aspetjournals.org/content/283/2/666
Alpha blocker - Wikipedia
However, the most common type of alpha blocker is usually an α1 blocker. Non-selective α-adrenergic receptor antagonists ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... "Alpha-Adrenoceptor Antagonists (Alpha-Blockers)" (PDF). British Hypertension Society. "CV Pharmacology , Alpha-Adrenoceptor ... and alpha 2-adrenergic receptors". The FASEB Journal. 6: 832-839. McKeage, Kate; Plosker, Greg L. (2002-03-01). "Alfuzosin". ...https://en.wikipedia.org/wiki/Alpha_blocker
... surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, ... Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. In: Hardman JG and Limbird L (eds) ... 1988) Molecular cloning and expression of the cDNA for the hamster alpha 1‐adrenergic receptor. Proceedings of the National ... Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key ...http://www.els.net/WileyCDA/ElsArticle/refId-a0000005.html
Adrenergic receptor - Wikipedia
Elliott J (Aug 1997). "Alpha-adrenoceptors in equine digital veins: evidence for the presence of both alpha1 and alpha2- ... "Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Molecular ... ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ...https://en.wikipedia.org/wiki/Adrenergic_receptor
G.alpha..sub.q protein variants and their use in the analysis and discovery of agonists and antagonists of chemosensory...
... functionally couple to sensory cell receptors such as taste GPCRs (TRs) and olfactory GPCRs (ORs) in an overly promiscuous ... In a particular embodiment, the G.alpha..sub.q protein variants can be expressed in mammalian cell lines or Xenopus oocytes, ... The invention provides a series of G.alpha..sub.q protein variants that ... adrenergic receptor, G.alpha..sub.olf-coupled mouse I7 olfactory receptor, G.alpha..sub.i-coupled m2 muscarinic receptor, and ...http://www.patentgenius.com/patent/7291485.html
Probing Receptor Structure/Function with Chimeric G-Protein-Coupled Receptors | Molecular Pharmacology
... second membrane-spanning domain of alpha 1a-adrenergic receptor determines subtype selectivity of dihydropyridine antagonists. ... Key amino acids for differential coupling of alpha1-adrenergic receptor subtypes to Gs. Biochem Biophys Res Commun 299: 142-147 ... of G alpha i via the alpha 2-adrenergic receptor is targeted by receptor-Gi interaction and is independent of receptor ... Kobilka BK, Kobilka TS, Daniel K, Regan JW, Caron MG, and Lefkowitz RJ (1988) Chimeric alpha 2-,beta 2-adrenergic receptors: ...http://molpharm.aspetjournals.org/content/65/6/1323
The α 1-adrenolytic and structural evaluation of new pyridoindole derivatives - Open Medicine - Volume 1, Issue 4 (2006) - PSJD...
Successful Virtual Screening for Antagonists of the Alpha1A Adrenergic Receptor", J. Med. Chem., Vol. 48, (2005), pp. 1088-1097 ... 2] R.M. De Marinis, M. Wise, J.P. Hieble and R.R. Ruffolo, Jr.: The alpha-1 Adrenergic Receptor, Humana Press, New Jersey, 1987 ... "Ligand Design for Alpha1 Adrenoceptors", Current Medicinal Chemistry Vol. 8, (2001), pp. 607-620. [Crossref] ... 3] J.B. Bremner, B. Coban and R. Griffith: "Pharmacophore development for antagonists at α1adrenergic receptor subtypes", J. ...http://psjd.icm.edu.pl/psjd/element/bwmeta1.element.-psjd-doi-10_2478_s11536-006-0033-8
The Latent Inhibition Model of Schizophrenia | SpringerLink
... and alpha(2)-adrenergic receptors: II. Functional profile and a multiparametric comparison with haloperidol, clozapine, and 11 ... potential antipsychotic displaying marked antagonist properties at alpha(1)- and alpha(2)-adrenergic receptors: I. Receptorial ... potential antipsychotic displaying marked antagonist properties at alpha(1)- ... Meltzer, H.Y. and Nash, J.F. (1991) Effects of antipsychotic drugs on serotonin receptors. Pharmacol Rev. 43: 587-604.PubMed ...https://link.springer.com/chapter/10.1007/978-1-4757-4860-4_12
Poisons and Toxins
Alpha-adrenergic receptor antagonists are antidotal.. Atiparnizole administered at 50 mcg/kg IM reverses signs within 10 ... Mechanism of action Amitraz acts at alpha 2- adrenergic receptor sites in the CNS and at both alphal and alpha 2-adrenergic ... The action produced by each compound depends on the adrenergic receptor or receptors that are activated. Phenylpropanolamine ... adrenergic agonists though phenylpropanolamine also produces mild beta, -adrenergic receptor stimulation and acts indirectly by ...http://maxshouse.com/Poisons.html
Analysis of Full and Partial Agonists Binding to β2-Adrenergic Receptor Suggests a Role of Transmembrane Helix V in Agonist...
Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and ... Thus, most β-adrenergic agonists and antagonists have a positively charged amine or ethanolamine groups ("tails") which has ... Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor ... β2-adrenergic receptor. GPCR. G protein-coupled receptor. RMSD. root mean square deviation. TM. transmembrane. Maxn. maximum ...http://pubmedcentralcanada.ca/pmcc/articles/PMC2693451/?lang=en-ca
Beta-3 adrenergic receptor - Wikipedia
Beta-3 adrenergic receptor has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... adrenergic receptor antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Mol. Pharmacol ...https://en.wikipedia.org/wiki/Beta-3_adrenergic_receptor
Yohimbe bark extract (Pausinystalia johimbe) | Plant Profiler | Sigma-Aldrich
The alpha 2-adrenergic receptor antagonist yohimbine inhibits epinephrine-induced platelet aggregation in healthy subjects. ... Alpha-2 Adrenergic Antagonist Effects: Yohimbine acts as an alpha-2 adrenoceptor antagonist. It is significantly more active at ... Assessment of alpha 2 adrenergic autoreceptor function in humans: effects of oral yohimbine. Life Sci 1982;30(23):2033-2041. ... Alpha 2-antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male ...https://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/pausinystalia-johimbe.html
Atiprosin - Wikipedia
Atiprosin (AY-28,228) is an antihypertensive agent which acts as a selective α1-adrenergic receptor antagonist. It also ... possesses some antihistamine activity, though it is some 15-fold weaker in this regard than as an alpha blocker. It was never ... ISBN 0-412-46630-9. Jirkovsky I, Santroch G, Baudy R, Oshiro G (February 1987). "Octahydropyrazino[2',3':3,4]pyrido[1,2-a] ... Prazosin Ketanserin David J. Triggle (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. ...https://en.wikipedia.org/wiki/Atiprosin
Patent US7403819 - Parasympathetic nerve stimulation for control of AV conduction - Google Patents
Adrenergic antagonists (indirect action) include beta-blockers such as proranolol and alpha-blockers such as phentolamine that ... such as alpha receptors and beta receptors, receive chemicals emitted by postganglionic nerves. Alpha receptors are the most ... In general, cardiac receptors that lead to a neural response are classified as "A" or "B" receptors. B receptors are the ... Beta receptors are also adrenergic and include beta-1, beta-2 and beta-3 receptors. Cardiac sympathetic receptors are mostly ...http://www.google.com/patents/US7403819?dq=4316055
Biological Profile of L-745,870, a Selective Antagonist with High Affinity for the Dopamine D4 Receptor | Journal of...
... compared to other dopamine receptor subtypes and had moderate affinity for 5HT2, sigma andalpha adrenergic receptors(IC50 , 300 ... 1993) Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur. J. ... The pituitary contains a high density of dopamine D2 receptors and compounds that possess D2 receptor antagonist activity ... sigma and alphaadrenergic receptors (IC50 , 300 nM). It has been postulated that ion channel blocking properties of some ...http://jpet.aspetjournals.org/content/283/2/636
YOHIMBE: Uses, Side Effects, Interactions and Warnings - WebMD
The alpha 2-adrenergic receptor antagonist yohimbine inhibits epinephrine-induced platelet aggregation in healthy subjects. ... Motulsky, H. J., Shattil, S. J., and Insel, P. A. Characterization of alpha 2-adrenergic receptors on human platelets using [ ... Evidence for activation of both adrenergic and cholinergic nervous pathways by yohimbine, an alpha 2-adrenoceptor antagonist. ... Brodde, O. E., Anlauf, M., Arroyo, J., Wagner, R., Weber, F., and Buck, K. D. Hypersensitivity of adrenergic receptors and ...https://www.webmd.com/vitamins-supplements/ingredientmono-759-yohimbe.aspx
Haloperidol decanoate (UK PID)
... weak antagonist activity at muscarinic, histamine H1, alpha-adrenergic, and serotonin receptors (Dollery 1991). Mechanism of ... The various receptor antagonist actions of haloperidol result in extrapyramidal reactions, orthostatic hypotension, a reduction ... Haloperidol is also a potent antagonist of opiate receptors, and has ... sympathomimetics with mixed alpha and beta adrenergic effects (e.g. adrenaline or dopamine) should not be used as they may ...http://www.inchem.org/documents/ukpids/ukpids/ukpid23.htm
William & Mary - Robin Looft-Wilson
Antagonists of the 20-HETE pathway inhibit rat small mesenteric artery tone. Microvasc. Res. 64: 349-352, 2002. ... Alpha(1)-adrenergic-mediated eNOS phosphorylation in intact arteries. Vascular Pharmacology, 58:112-117, 2013. ... Pannexin1 regulates a1-adrnergic receptor-mediated vasoconstriction. Circulation Research, 109: 80-85, 2011. ... 3: 61-62, 1996.. *Greenleaf, J.E., T. Hutchinson, M. Schaffer-Bailey, and R. Looft-Wilson. Exercise thermoregulation after 6 h ...https://www.wm.edu/as/kinesiology/faculty/looft_r.php
Alpha-1 blocker - Wikipedia
Taylor, Fletcher; Raskind, Murray A. (February 2002). "The alpha1-adrenergic antagonist prazosin improves sleep and nightmares ... Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ... DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic Blockers at the US National Library of Medicine Medical ... Silodosin is the most selective for alpha-1a receptors. The affinity and selectivity for alpha-1 receptors seems to be ...https://en.wikipedia.org/wiki/Alpha-1_blocker
Christos E. Constantinou | Stanford Medicine Profiles
Similarly alpha-adrenergic antagonists did not affect corporal stiffness in a statistically significant manner. These results ... In this investigation, we examined the impact of the alpha1 adrenoceptor (alpha1-ADR) antagonist prazosin on the urodynamic ... To examine the effects of N-methyl-D-aspartate (NMDA) receptor antagonists on the frequency/volume (F/V) characteristics of ... The alpha 2 antagonist atipamezole significantly increased the compliance of all prostates, including controls, while the alpha ...https://med.stanford.edu/profiles/christos-constantinou
It is a 5-HT2 and 5-HT3 receptor antagonist, a histamine- 1 receptor antagonist, a moderate peripheral alpha-1 adrenergic ... antagonist, and a moderate muscarinic receptor antagonist. It is a noradrenergic and specific serotonergic antidepressant ( ... 2,1-A) pyrido (2,3-C) benzazepine o 6-Azamianserin o Mepirzepine o ORG 3770 o Molecular Formula: C17-H19-N3 o CAS 61337-67-5 * ... The interaction was probably a result of postsynaptic serotonin receptor supersensitization caused by low central serotonin ...http://antidepressantsfacts.com/remeron.htm
Alpha-1B adrenergic receptor - Wikipedia
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... 2005). "Yeast two-hybrid screening for proteins that interact with alpha1-adrenergic receptors". Acta Pharmacol. Sin. 25 (11): ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ...https://en.wikipedia.org/wiki/Alpha-1B_adrenergic_receptor
F 11440, a Potent, Selective, High Efficacy 5-HT1AReceptor Agonist with Marked Anxiolytic and Antidepressant Potential |...
Role of 5-HT1A receptors in the ability of mixed 5-HT1A receptor agonist/dopamine D2 receptor antagonists to inhibit ... adrenergic: alpha-2, β1, β2; GABA-ergic: GABAA, GABAB; benzodiazepine; opiate; histaminergic: H2, H3; acetylcholinergic: ... 1989) Use of 5-HT receptor agonists and antagonists for the characterization of their respective receptor sites. Drugs Tools ... 1993) Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that ...http://jpet.aspetjournals.org/content/287/1/266.long