Uses
BMY 7378 dihydrochloride is a SR-1A agonist and a selective α1D-AR antagonist.
Biological Activity
5-HT 1A partial agonist and high affinity α 1D adrenoceptor antagonist (K i values are 2, 800 and 600 nM at cloned rat α 1D , rat α 1A and hamster α 1B receptors respectively). Also available as part of the α 1 -Adrenoceptor Tocriset™ .
Biochem/physiol Actions
BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.
IC 50
rat α
1A-adrenergic receptor: 800 nM (Ki); hamster alpha
1B-adrenergic receptor: 600 nM (Ki); rat alpha
1D-adrenergic receptor: 2 nM (Ki); 5-HT
1A Receptor
References
1. yocca fd, hyslop dk, smith dw et al. bmy 7378, a buspirone analog with high affinity, selectivity and low intrinsic activity at the 5-ht1a receptor in rat and guinea pig hippocampal membranes. eur j pharmacol. 1987 jun 4;137(2-3):293-4.2. zemlan fp, zieleniewski-murphy a, maureen murphy r et al bmy 7378: partial agonist at spinal cord 5-ht(1a) receptors. neurochem int. 1990;16(4):515-22.3. goetz as, king hk, ward sd et al. bmy 7378 is a selective antagonist of the d subtype of alpha 1-adrenoceptors. eur j pharmacol. 1995 jan 16;272(2-3):r5-6.4. cleary l, murad k, bexis s et al. the alpha (1d)-adrenoceptor antagonist bmy 7378 is also an alpha (2c)-adrenoceptor antagonist. auton autacoid pharmacol. 2005 oct;25(4):135-41.5. sharp t, backus li, hjorth s et al. further investigation of the in vivo pharmacological properties of the putative 5-ht1a antagonist, bmy 7378. eur j pharmacol. 1990 feb 13;176(3):331-40.
