Identification | Back Directory | [Name]
Delequamine hydrochloride | [CAS]
119942-75-5 | [Synonyms]
RS15385 RS-15385 RS 15385 Delequamine HCl Delequamine hydrochloride | [Molecular Formula]
C18H27ClN2O3S | [MOL File]
119942-75-5.mol | [Molecular Weight]
386.94 |
Hazard Information | Back Directory | [Uses]
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction[1]. | [in vivo]
Delequamine (0.4-6.4 mg/kg; oral, single dose) hydrochloride can increase the sexual behavior score in a dose-dependent manner in a model where untrained male rats are exposed to estrogen-progesterone-treated, sexually receptive female rats. Furthermore, the combination of Delequamine (0.4 mg/kg; oral, single dose) hydrochloride and 8-OH-DPAT (HY-112061) (0.1 mg/kg; subcutaneous injection) can increase the percentage of mounts, intromissions, and ejaculations in rats, shorten the ejaculation latency, and reduce the number of intromissions[1]. | [IC 50]
α2-adrenergic receptor: 9.5 (pKi); α1-adrenergic receptor: 5.3 (pKi) | [References]
[1] Tallentire D, et al. Modulation of sexual behaviour in the rat by a potent and selective alpha 2-adrenoceptor antagonist, delequamine (RS-15385-197). Br J Pharmacol. 1996;118(1):63-72. DOI:10.1111/j.1476-5381.1996.tb15367.x |
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