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.
|Formulation||sterile 0.9% sodium chloride solution|
|Administration||Inject subcutaneously at a single dose|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
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