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Apelin is a neuro-vasoactive peptide that plays a major role in the controlof cardiovascular functions and water balance, but has an in-vivo half-life inthe minute range, limiting its therapeutic use. We previously developedLIT01-196, a systemically active metabolically stable apelin-17 analog,produced by chemical addition of a fluorocarbon chain to the N-terminal part ofapelin-17. LIT01-196 behaves as a potent full agonist for the apelin receptorand has an in vivo half-life in the bloodstream of 28 min after intravenous(i.v.) and 156 min after subcutaneous (s.c.) administrations in consciousnormotensive rats. We aimed to investigate the effects of LIT01-196 followingsystemic administrations on arterial blood pressure, heart rate, fluid balanceand electrolytes in conscious normotensive and hypertensive deoxycorticosteroneacetate (DOCA)-salt rats. Acute i.v. LIT01-196 administration, in increasingdoses, dose-dependently decreases arterial blood pressure with ED 50 values of9.8 and 3.1 nmol/kg in normotensive and hypertensive rats, respectively. Thiseffect occurs for both via a nitric oxide-dependent mechanism. Moreover, acutes.c. LIT01-196 administration (90 nmol/kg) normalizes arterial blood pressurein conscious hypertensive DOCA-salt rats for more than 7 h. TheLIT01-196-induced blood pressure decrease remains unchanged after 4 consecutivedaily s.c. administrations of 90 nmol/kg, and does not induce any alteration ofplasma sodium and potassium levels and kidney function as shown by the lack ofchange in plasma creatinine and urea nitrogen levels. Activating the apelinreceptor with LIT01-196 may constitute a novel approach for the treatment ofhypertension.

LIT01-196, a Metabolically Stable Apelin-17 Analog, Normalizes Blood Pressure in Hypertensive DOCA-Salt Rats via a NO Synthase-dependent Mechanism