product name BMY 7378
Description: BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3. BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. BMY 7378 blocks the inhibition on forskolin-stimulated adenylate cyclase activity in rat hippocampus induced by the 5-HT1A agonist, 8-OHh-DPAT.
References: Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41.
458.42
Formula
C22H31N3O3.2HCl
CAS No.
21102-95-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 92 mg/mL (200.7 mM)
Water: 92 mg/mL (200.7 mM)
Ethanol: 20 mg/mL (43.6 mM)
Solubility (In vivo)
Saline: 15 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398549
| In Vitro |
In vitro activity: BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4 BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | BMY 7378 (pA2 of 8.67) is approximately 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor). BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in 0.9% sodium chloride solution; 0.25-5 mg/kg; s.c. injection |
| References | Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. |
Related Posts
product name BMY 7378
Description: BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3. BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. BMY 7378 blocks the inhibition on forskolin-stimulated adenylate cyclase activity in rat hippocampus induced by the 5-HT1A agonist, 8-OHh-DPAT.
References: Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41.
458.42
Formula
C22H31N3O3.2HCl
CAS No.
21102-95-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 92 mg/mL (200.7 mM)
Water: 92 mg/mL (200.7 mM)
Ethanol: 20 mg/mL (43.6 mM)
Solubility (In vivo)
Saline: 15 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398549
| In Vitro |
In vitro activity: BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4 BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | BMY 7378 (pA2 of 8.67) is approximately 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor). BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in 0.9% sodium chloride solution; 0.25-5 mg/kg; s.c. injection |
| References | Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. |