Protein Information

Name alpha adrenoceptor
Synonyms Alpha 2A Adrenoceptor; ZNF32; ADRA2; ADRA2A; ADRA2R; ADRAR; ALPHA2AAR; Alpha 2A adrenergic receptor…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15145080 Johnson PJ, Bornstein JC: Neurokinin-1 and -3 receptor blockade inhibits slow excitatory synaptic transmission in myenteric neurons and reveals slow inhibitory input. Neuroscience. 2004;126(1):137-47.

They were abolished by the 5-hydroxytryptamine (1A) receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine (NAN-190), but unaffected by phentolamine, an alpha-adrenoceptor antagonist.
31(0,1,1,1) Details
12505530 Astier B, Lambas Senas L, Souliere F, Schmitt P, Urbain N, Rentero N, Bert L, Denoroy L, Renaud B, Lesourd M, Munoz C, Chouvet G: In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity. Eur J Pharmacol. 2003 Jan 10;459(1):17-26.

The aim of the present study was to compare, in chloral-hydrate anaesthetized rats, the alpha (2)-adrenergic properties of the selective 5-HT (1A) receptor agonist, alnespirone (S-20499), with those of buspirone, a 5-HT (1A) receptor agonist exhibiting potent alpha (2)-adrenoceptor antagonist properties via its principal metabolite, 1-(2-pyrimidinyl)-piperazine.
31(0,1,1,1) Details
12591110 Amobi N, Guillebaud J, Kaisary A, Lloyd-Davies RW, Turner E, Smith IC: Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens. Eur J Pharmacol. 2003 Feb 21;462(1-3):169-77.

The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo [2,2,2] octa-2,5-dienylca rbonyl-2-piperazine), an alkylating prazosin analogue that discriminates between alpha (1H)- and alpha (1L)-adrenoceptor subtypes.
4(0,0,0,4) Details
11226402 Rizzo CA, Ruck LM, Corboz MR, Umland SP, Wan Y, Shah H, Jakway J, Cheng L, McCormick K, Egan RW, Hey JA: Postjunctional alpha (2C)-adrenoceptor contractility in human saphenous vein. Eur J Pharmacol. 2001 Feb 16;413(2-3):263-9.

BHT-920-induced contractions were inhibited by the alpha (2)-adrenoceptor antagonist yohimbine (17-Hydroxy-yohimban-16-carboxylic acid methyl ester hydrochloride; pA (2)=8.7+/-0.5), but not by the alpha (1)-adrenoceptor antagonist prazosin (1-[4-Amino-6,7-dimethoxy-2-quinazolinyl]-4-[2-furanylcarbonyl]-piperazine hydrochloride; 300 nM).
Functional antagonist activity estimates (pA (2) or pK (b)) obtained for the alpha-adrenoceptor antagonists ARC 239 (2-[2-(4-(2-Methoxyphenyl) piperazin-1-yl) ethyl]-4,4-dimethyl-1,3-(2H,4H)-i soquinolindione dihydrochloride), WB 4101 (2-(2,6-Dimethoxyphenoxyethyl) aminomethyl-1,4-benzodioxane hydrochloride) and HV 723 (alpha-ethyl-3,4,5-trimethoxy-alpha-(3-((2-(2-methoxyphenoxy) ethyl) amino) propyl) benzeneacetonitrile) against BHT-920-induced human saphenous vein contractions were 7.0+/-0.6, 8.3+/-0.6 and 7.7+/-0.3, respectively.
1(0,0,0,1) Details
15878998 Shafaroudi MM, McBride M, Deighan C, Wokoma A, Macmillan J, Daly CJ, McGrath JC: Two "knockout" mouse models demonstrate that aortic vasodilatation is mediated via alpha2a-adrenoceptors located on the endothelium. J Pharmacol Exp Ther. 2005 Aug;314(2):804-10. Epub 2005 May 5.

In the alpha (2A)-adrenoceptor knockout mouse and the D79N mouse, a functional knockout of the alpha (2A)-adrenoceptor, these relaxant effects of UK-14,304 were lost, indicating the involvement of the alpha (2A)-adrenoceptor.
A fluorescent ligand, quinazoline piperazine bodipy, antagonized the relaxant action of UK-14,304.
2(0,0,0,2) Details
11193002 Ibarra M, Hong E, Villalobos-Molina R: The alpha-adrenoceptor antagonist, zolertine, inhibits alpha1D- and alpha1A-adrenoceptor-mediated vasoconstriction in vitro. J Auton Pharmacol. 2000 Jun;20(3):139-45.

The antagonist effect of zolertine (4-phenyl-1-[2-(5-tetrazolyl) ethyl] piperazine trihydrochloride), on vascular contraction elicited by noradrenaline in aorta, carotid (alpha1D-adrenoceptors), mesenteric (alpha1A/D-adrenoceptors) and caudal arteries (alpha1A-adrenoceptors) from Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats and rabbit aorta (alpha1B-adrenoceptors), was investigated in endothelium-denuded arterial rings. 2.
1(0,0,0,1) Details
15382198 Myers RA, Plym MJ, Signor LJ, Lodge NJ: 1-(2-pyrimidinyl)-piperazine, a buspirone metabolite, modulates bladder function in the anesthetized rat. Neurourol Urodyn. 2004;23(7):709-15.

The effects of 1-PP are likely mediated primarily by alpha2 receptor antagonism.
1(0,0,0,1) Details