BMY 7378

BMY 7378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist with Ki values of 2.8 and 0.6 μM for cloned rat rat α1A and hamster α1B receptors, respectively. BMY 7378 has high selectivity for the alpha 1D-adrenoceptor subtype with pKi values of 6.2 ± 0.03, 7.2 ± 0.05, 6.1 ± 0.02, 6.6 ± 0.20, 8.2 ± 0.06 and 9.4 ± 0.05 for hamster alpha 1b-adrenoceptor, human alpha 1b-adrenoceptor, bovine alpha 1c-adrenoceptor, human alpha 1c-adrenoceptor ; rat alpha 1d-adrenoceptor and human alpha 1d-adrenoceptor, respectively. In addition, BMY 7378 has high affinity with pA2 of 8.9 ± 0.1 for rat aorta alpha 1-adrenoceptor.