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Cat. No. Name Size Price Add Cart
KI3300BMY 7378 dihydrochloride50 mg$230

Chemical Characteristic

Product NameBMY 7378 dihydrochloride
CAS No.21102-95-4
Molecular Weight 458.42
FormulaC22H31N3O3.2HCl
Chemical Structure

Biological activities

BMY 7378 is a partial agonist/antagonist for 5-HT1A receptor and multi-targeted antagonist of α2C-adrenoceptor and α1D-adrenoceptor. BMY 7378 is selective for the α1-adrenoceptor subtype including hamster α1b-adrenoceptor, human α1b-adrenoceptor, bovine α1c-adrenoceptor, human α1c-adrenoceptor, rat α1d-adrenoceptor, and human α1d-adrenoceptor with pKi values of 6.2, 7.2, 6.1, 6.6, 8.2, and 9.4, respectively.[1] BMY 7378 has 10-fold selectivity for α2C-adrenoceptor over other α2-adrenoceptors with a pKi of 6.54. BMY 7378 (pA2 of 8.67) shows about 100-fold potentness over yohimbine (pA2 of 6.62) at antagonizing the contractile response to noradrenaline in rat aorta (α1D-adrenoceptor). However, BMY 7378 (pA2 of 6.48) is about 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor).[2] BMY 7378 also inhibits the [3H]prazosin specific binding to the rabbit ventricular membrane fraction in a monophasic manner with a pKi of 7.53.[3] In behavioral studies in the spinal rat, BMY 7378 increases the animals' sensitivity to noxious levels of mechanical stimulation with an ED50 of 295 nmol/kg with no significant difference in the maximal response (Ymax) observed.[4] In vivo, BMY 7378 administration (0.25-5 mg/kg s.c.) reduces to undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT in a dose-dependent manner in the rat. In addition, BMY 7378 at the concentration of 5 mg/kg also significantly attenuates stereotypy and locomotor activity induced by apomorphine in the behavioural experiments. In contrast, BMY 7378 (0.01-1.0 mg/kg s.c.) causes a significant and dose-dependent decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis.[5]

Protocols

In vivo: BMY 7378 is dissolved in saline.[5]

References

[1] Goetz AS, et al. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1995, 272(2-3): R5-R6.
[2] Cleary L, et al. The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist. Auton Autacoid Pharmacol. 2005, 25(4): 135-141.
[3] Yang HT, et al. The safety, Pharmacological evidence for alpha(1D)-adrenoceptors in the rabbit ventricular myocardium: analysis with BMY 7378. Br J Pharmacol. 1997, 122(8): 1541-1550.
[4] Zemlan FP, et al. BMY 7378: Partial agonist at spinal cord 5-HT(1A) receptors. Neurochem Int. 1990, 16(4): 515-522.
[5] Sharp T, et al. Further investigation of the in vivo pharmacological properties of the putative 5-HT1A antagonist, BMY 7378. Eur J Pharmacol. 1990, 176(3): 331-340.
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