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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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | rats |
| Formulation | sterile 0.9% sodium chloride solution |
| Dosages | 0.25-5 mg/kg |
| Administration | Inject subcutaneously at a single dose |
| Molecular Weight | 458.42 |
| Formula | C22H31N3O3.2HCl |
| CAS Number | 21102-95-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] A S Goetz, et al. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors
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