Losulazine

Losulazine is an orally active antihypertensive agent. Losulazine modulates acid phosphatase, 3β-hydroxysteroid dehydrogenase, and 17β-hydroxysteroid dehydrogenase activity. Losulazine can be used for the research of hypertension^{[1][2][3][4][5][6]}. In Vivo:Losulazine (1-5 mg/kg; i.p.; daily; 13 days) exerts dose-dependent biphasic effects on testicular steroidogenesis and accessory sex gland function in adult male Wistar rats^[1].
Losulazine (4-32 mg/kg; p.o.; daily; 1 year or 30 weeks) induces dosage-dependent reversible decreased fertility, dosage-dependent reduced body weight gain and food consumption, non-dosage-related minimal to mild testicular lesions, and increased relative organ weights in male Sprague-Dawley rats^[2].
Losulazine (10 mg/kg; p.o.; single dose or daily for 15-27 days) causes complete anestrus in female Sprague-Dawley rats via hypothalamic catecholamine depletion and subsequent hyperprolactinemia^[3].
Losulazine (2-8 mg/kg; p.o.; daily) dose-dependently impairs fertility and reproductive performance in both sexes of Sprague-Dawley rats^[4].
Losulazine (2.5-10 mg/kg; i.p.; single dose) produces marked, sustained catecholamine depletion in brain and pituitary regions outside the blood-brain barrier, with modest, transient dopamine reductions in barrier-protected regions, and increases plasma prolactin and α-melanocyte-stimulating hormone concentrations transiently in rats^[5].
Losulazine (2.5 mg/kg; i.p.; single dose; or daily for 12 days) causes estrous cycle disruption in female rats, produces sustained catecholamine depletion in barrier-free brain and pituitary regions without tolerance, and has cumulative dopamine-depleting effects in the striatum, while sparing central 5-hydroxytryptaminergic neurons^[5].
Losulazine exerts hypotensive activity in conscious monkeys by modulating sympathetic nerve activity without causing orthostatic hypotension^[6].