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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[3] A S Goetz, et al. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors
| Related 5-HT Receptor Products |
|---|
| TC-2153
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP). TC-2153 also inhibits 5-HT2A receptor-mediated signaling. |
| Gentisein
Gentisein (NSC-329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM. |
| MM120
MM120 is a synthetic tryptamine that is also a partial agonist at the 5-hydroxytryptamine 2A (5-HT2A) receptor. It can be used in studies related to GAD and attention deficit hyperactivity disorder (ADHD). |
| SB 258741 hydrochloride
SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist for schizophrenia. |
| 5-HT1A antagonist 1
5-HT1A antagonist 1 is a potent and selective 5-HT1A receptor antagonist with a Ki value of 35 nM.5-HT1A antagonist 1 can be used in the study of central nervous system disorders. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
