Targeting TMEM16A-encoded Ca(2+)-activated Cl(-) channels: a new paradigm for antihypertensive therapy?

靶向TMEM16A编码的Ca(2+)激活Cl(-)通道:抗高血压治疗的新范式?

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Abstract

Hypertension is the leading risk factor for the development of heart diseases and stroke. Many hypertensive patients experience undesirable side effects to conventional antihypertensive pharmacotherapy. Cil et al. documented the antihypertensive profile of a novel molecule, TM(inh)-23 (2-bromodifluoroacetylamino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid o-tolylamide), in the spontaneously hypertensive rat model of systemic hypertension. They showed that this agent reduces blood pressure by inhibiting transmembrane member 16A-encoded calcium-activated chloride channels in vascular myocytes from resistance arteries. If validated, TM(inh)-23 could become a useful clinical tool.

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