2. Academic Validation
  3. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors

BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors

  • Eur J Pharmacol. 1995 Jan 16;272(2-3):R5-6. doi: 10.1016/0014-2999(94)00751-r.
A S Goetz 1,  H K King,  S D Ward,  T A True,  T J Rimele,  D L Saussy Jr
Affiliations

Affiliation

  • 1 Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.
PMID: 7713154 DOI: 10.1016/0014-2999(94)00751-r
Abstract

BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8- azaspiro[4.5]decane-7,9-dione dihydrochloride), a 5-HT1A receptor partial agonist, also binds to alpha 1-adrenoceptors. Competition assays were performed using (+/-)-beta-([125I]iodo-4-hydroxyphenyl)-ethyl-aminomethyl-tetralone ([125I]HEAT), and membranes prepared from Rat-1 fibroblasts expressing hamster alpha 1b-, bovine alpha 1c-, or rat alpha 1d-adrenoceptor, or their respective human homologues. Results indicate that BMY 7378 is selective for the alpha 1D-adrenoceptor subtype (pKi: hamster alpha 1b-adrenoceptor 6.2 +/- 0.03, human alpha 1b-adrenoceptor 7.2 +/- 0.05; bovine alpha 1c-adrenoceptor 6.1 +/- 0.02, human alpha 1c-adrenoceptor 6.6 +/- 0.20; rat alpha 1d-adrenoceptor 8.2 +/- 0.06, human alpha 1d-adrenoceptor 9.4 +/- 0.05) and has high affinity (pA2, 8.9 +/- 0.1) for rat aorta alpha 1-adrenoceptor.

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