Why the study?
Does SAR407899 inhibit endothelin-1-induced constriction of renal resistance arteries more effectively than Y27632?
Does SAR407899 inhibit endothelin-1-induced constriction of renal resistance arteries more effectively than Y27632?
The Rho kinase inhibitor SAR407899 shows greater efficacy in inhibiting ET-1-induced vasoconstriction in renal vessels compared to Y27632, potentially explaining its higher antihypertensive potency.
May support SAR407899 development in diabetic vasculopathy; leaves open translation to human hypertension therapy.
ET-1-induced vasoconstriction is more ROCK-dependent in renal than in nonrenal resistance arteries. SAR407899 causes a greater inhibition of ET-1-induced vasoconstriction in renal resistance arteries from ZDF rats and patients than Y27632. The greater efficacy in renal vessels may contribute to the higher antihypertensive potency of SAR407899 compared with Y27632.
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Grisk et al. (2012) studied this question.
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