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LY43578 is a nonsteroidal aromatase inhibitor (EC50 = 0.071 µM) and an active metabolite of LY56110.1,2 Neonatal administration of LY43578 (5 mg/kg) increases ambulation and decreases the defecation rate in the open field test, decreases mounts and intromissions, and increases the lordotic quotient in adult male rats, indicating feminine-like behavior.3 However, it does not induce feminine-like behavior in adult male rats when administered on postnatal day 12.4 LY43578 increases sleep time induced by the sedative ethinamate in rats at 10 mg/kg.2
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1. Estrogen synthetase inhibitors. 2. Comparison of the in vitro aromatase inhibitory activity for a variety of nitrogen heterocycles substituted with diarylmethane or diarylmethanol groups. J. Med. Chem. 33(1), 416-429 (1990).
2. Disposition of the aromatase inhibitor LY56110 and associated induction and inhibition studies in rats, dogs, and monkeys. Fundam. Appl. Toxicol. 8(4), 595-604 (1987).
3. Role of monoamines in the male differentiation of the brain induced by androgen aromatization. Pharmacol. Biochem. Behav. 41(4), 733-737 (1992).
4. Injection of an aromatase inhibitor after the critical period of sexual differentiation. Pharmacol. Biochem. Behav. 47(1), 183-186 (1994).