| Name | alpha2 adrenoceptor (protein family or complex) |
|---|---|
| Synonyms | Alpha adrenoceptor; Alpha adrenoceptor; Alpha adrenergic receptor; Alpha adrenergic receptors; Alpha adrenoceptors; Alpha adrenoceptors; alpha1 Adrenoceptors; alpha1 Adrenoceptor… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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. |
1(0,0,0,1) | Details |
| 15210583 | Deighan C, Woollhead AM, Colston JF, McGrath JC: Hepatocytes from alpha1B-adrenoceptor knockout mice reveal compensatory adrenoceptor subtype substitution. Br J Pharmacol. 2004 Jul;142(6):1031-7. Epub 2004 Jun 21. 1 Alpha1-adrenoceptors (ARs) play an important functional role in the liver; yet little is known about their cellular location. We identified the subtypes present in wild-type (WT) and alpha1B-AR knockout (KO) mice livers at 3 and 4 months of age, and investigated their distribution in hepatocytes. 2 The fluorescent alpha1-AR antagonist quinazolinyl piperazine borate-dipyrromethene (QAPB) was used to visualise hepatic alpha1-ARs and radioligand binding with [3H]-prazosin was used to quantify the alpha1-AR population. 3 QAPB and [3H]-prazosin bound specifically to hepatic alpha1-ARs with nanomolar affinity. |
1(0,0,0,1) | Details |
| 12433595 | Villalobos-Molina R, Gallardo-Ortiz IA, Lopez-Guerrero JJ, Ibarra M: Evidence that NAN-190-induced hypotension involves vascular alpha1-adrenoceptor antagonism in the rat. Eur J Pharmacol. 2002 Nov 22;455(1):59-64. The effect of NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalimido]-butyl] piperazine), described as a mixed 5-HT (1A) receptor agonist/antagonist, on cardiovascular function was studied. |
1(0,0,0,1) | Details |
| 16314688 | Omiya Y, Suzuki Y, Yuzurihara M, Murata M, Aburada M, Kase Y, Takeda S: Antinociceptive effect of shakuyakukanzoto, a Kampo medicine, in diabetic mice. J Pharmacol Sci. 2005 Dec;99(4):373-80. Epub 2005 Nov 26. The spinal alpha2-adrenoceptor-mediated analgesic mechanism was enhanced in diabetic mice, suggesting that shakuyakukanzoto exhibits its effect by activating the descending noradrenergic neurons. |
1(0,0,0,1) | Details |
| 11137626 | Taoda M, Adachi YU, Uchihashi Y, Watanabe K, Satoh T, Vizi ES: Effect of dexmedetomidine on the release of [3H]- from rat kidney cortex slices: characterization of alpha2-adrenoceptor. Neurochem Int. 2001 Apr;38(4):317-22. In contrast, ARC-239 (2-(2,4-(o-piperazine-1-yl)-ethyl-4,4-dimethyl-1,3-(2H, 4H) disoguinolinedione a selective alpha (2B)-antagonist, had no effect on the release and failed to prevent the effect of dexmedetomidine. |
1(0,0,0,1) | Details |
| 16456285 | Zhou X, Wang XB, Kong LY: bonding and pi-pi stacking in 7-{2-[4-(4-methoxyphenyl) piperazin-1-yl] ethoxy}-4-methyl- monohydrate. Acta Crystallogr C. 2006 Feb;62(Pt 2):o58-61. Epub 2006 Jan 14. The piperazine ring adopts an almost perfect chair conformation, and the methoxy group is coplanar with its parent ring. The bioassay results have shown alpha1-adrenoceptor antagonistic activity through in vitro animal experiments. |
1(0,0,0,1) | Details |
| 17505018 | Platt DM, Rowlett JK, Spealman RD: Noradrenergic mechanisms in cocaine-induced reinstatement of drug seeking in squirrel monkeys. J Pharmacol Exp Ther. 2007 Aug;322(2):894-902. Epub 2007 May 15. In test sessions during which the cocaine-paired stimulus was reintroduced but only vehicle was available for self-administration, priming with cocaine, the transport inhibitor 1-[2-[bis-(4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909), and the NE transport inhibitors nisoxetine and talsupram induced dose-dependent reinstatement of drug seeking. |
0(0,0,0,0) | Details |
| 20118542 | Hess S, Padoani C, Scorteganha LC, Holzmann I, Malheiros A, Yunes RA, Delle Monache F, de Souza MM: Assessment of mechanisms involved in antinociception caused by myrsinoic acid B. Biol Pharm Bull. 2010 Feb;33(2):209-15. The antinociception caused by AMB in the test was significantly attenuated by i.p. treatment of mice with precursor, 600 mg/kg), alpha2 and alpha1-adrenoceptor antagonists (yohimbine, 0.2 mg/kg/prazosin, 0.2 mg/kg), p-chlorophenylalanine (PCPA) an inhibitor of synthesis (100 mg/kg), 1-(2-methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN 190), a 5-HT1 (A) selective receptor antagonist (0.5 mg/kg) and a non-selective cholinergic antagonist (atropine, 10 mg/kg). |
32(0,1,1,2) | Details |
| 11754589 | Peglion JL, Goument B, Despaux N, Charlot V, Giraud H, Nisole C, Newman-Tancredi A, Dekeyne A, Bertrand M, Genissel P, Millan MJ: Improvement in the selectivity and metabolic stability of the 5-HT (1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. J Med Chem. 2002 Jan 3;45(1):165-76. While S 15535 itself presents reasonable selectivity (158-fold) in this respect, trans piperazine derivatives 4-trans,35, 39, 41, 47, 64, 68, 69, 70, 71 displayed even more pronounced selectivity vs alpha1-adrenoceptors, with the nitro derivative 70 being highly selective (1259-fold). |
82(1,1,1,2) | Details |
| 12523493 | Wesolowska A, Borycz J, Paluchowska MH, Chojnacka-Wojcik E: Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice. Pol J Pharmacol. 2002 Jul-Aug;54(4):391-9. In this study, we examined the role of (5-HT) 1A and alpha1-adrenergic receptors in the hypothermia induced by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine (NAN-190) and its analogs, 1-(2-methoxyphenyl)-4-[(4-succinimido) butyl] piperazine (MM77) and trans-1 (2-methoxyphenyl)-4-[4-(2-phthalimido) cyclohexyl] piperazine (MP245), which--like NAN-190--showed a high affinity for 5-HT1A and alpha1-adrenoceptors. |
32(0,1,1,2) | Details |
| 11488433 | Fukuda Y, Fukuta Y, Higashino R, Yoshida K, Ogishima M, Takei M, Kurimoto T: Hormonal effects of Z-350, possessing steroid 5alpha-reductase inhibitory and alpha1-adrenoceptor antagonistic actions, in the rat. Jpn J Pharmacol. 2001 Jul;86(3):323-8. We examined the hormonal effects of Z-350, (S)-4-[3-(4-[1-(4-methylphenyl)-3-[4-(2-methoxyphenyl) piperazine-1-yl] prop oxy] benzoyl) -1-yl] hydrochloride, which has both alpha1-adrenoceptor blocking activity and steroid 5alpha-reductase inhibitory activity, in male and female rats. |
32(0,1,1,2) | Details |
| 19190523 | Foong JP, Bornstein JC: antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig. Neuroreport. 2009 Feb 18;20(3):325-30. |
3(0,0,0,3) | 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 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. Competition binding experiments using the alpha1-adrenoceptor antagonist [3H] prazosin showed a zolertine pKi of 6.81 +/- 0.02 in rat liver (alpha1B-adrenoceptors) and 6.35 +/- 0.04 in rabbit liver (alpha1A-adrenoceptors) membranes. 5. |
2(0,0,0,2) | Details |
| 17882957 | Fu XZ, Tang L, Yuan M, Shi JS: [Design, synthesis and vasorelaxant activity of R, S-1-(substituted phenyl)-4-[3-(naphtha-1-yl-oxy)-2-hydroxypropyl]-piperazine derivatives]. Yao Xue Xue Bao. 2007 Jul;42(7):735-40. According to the results of activity-structure relationship (SAR) studies of alpha1-adrenoceptor antagonists hydantoin-phenylpiperazine and benzimidazo-arypiperazine derivatves, to design and synthesize a series of novel phenylpiperazine alpha1-adrenoceptor antagonists with more potent vasorelaxant activity, active metabolites of naftopidil were used as lead compounds. |
2(0,0,0,2) | Details |
| 15801844 | Lopez-Rodriguez ML, Morcillo MJ, Fernandez E, Benhamu B, Tejada I, Ayala D, Viso A, Campillo M, Pardo L, Delgado M, Manzanares J, Fuentes JA: Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. J Med Chem. 2005 Apr 7;48(7):2548-58. Computational simulation of ligand-receptor interaction of 5-HT (1A) R agonists with selectivity over alpha1-adrenoceptors.. The aryl substituent of the piperazine moiety (Ar) consists of different benzofused rings mimicking the favorable voluminous substituents at ortho and meta positions predicted by 3D-QSAR analysis in the previously reported series I. |
1(0,0,0,1) | Details |