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BMY 7378_Molecular_structure_CAS_21102-95-4)
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BMY 7378

Catalog No. S2691 Name Selleck Chemicals
CAS Number 21102-95-4 Website http://www.selleckchem.com
M. F. C22H33Cl2N3O3 Telephone (877) 796-6397
M. W. 458.42172 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 73169


IUPAC name
8-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione dihydrochloride
IUPAC Traditional name
8-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione dihydrochloride


CAS Number 21102-95-4


Target Serotonin receptor
Salt Data dihydrochloride
Storage Condition -20°C


Description (English)
Biological Activity
Description BMY 7378 is a multiple inhibitors of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively.




6.54 (pKi) [1]

8.2 (pKi) [2]

In Vitro BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. [1] 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 [2] BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. [3]
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).[1] 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. [4]
Clinical Trials
Combination Therapy

BMY 7378 inhibits 5-HT release induced by 8-OH-DPAT, but this effect is attenuated by pretreatment with the 5-HT1 receptor/beta-adrenoceptor antagonist pindolol (8 mg/kg s.c.), while the effect is not alter by pretreatment with a combination of the beta 1- and beta 2-adrenoceptor antagonists metoprolol (4 mg/kg s.c.) and ICI 118 551 (4 mg/kg s.c.). [4]

[1] Cleary L, et al. Auton Autacoid Pharmacol, 2005, 25(4), 135-141.
[2] Goetz AS, et al. Eur J Pharmacol, 1995, 272(2-3), R5-6.
[3] Greuel JM, et al. Eur J Pharmacol, 1992, 211(2), 211-219.
[4] Sharp T, et al. Eur J Pharmacol, 1990, 176(3), 331-40.