Pijacka Wioletta, Moraes Davi J A, Ratcliffe Laura E K, Nightingale Angus K, Hart Emma C, da Silva Melina P, Machado Benedito H, McBryde Fiona D, Abdala Ana P, Ford Anthony P, Paton Julian F R
School of Physiology, Pharmacology &Neuroscience, Biomedical Sciences, University of Bristol, Bristol, UK.
Department of Physiology, School of Medicine of Ribeirao Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil.
Nat Med. 2016 Oct;22(10):1151-1159. doi: 10.1038/nm.4173. Epub 2016 Sep 5.
In view of the high proportion of individuals with resistance to antihypertensive medication and/or poor compliance or tolerance of this medication, new drugs to treat hypertension are urgently needed. Here we show that peripheral chemoreceptors generate aberrant signaling that contributes to high blood pressure in hypertension. We discovered that purinergic receptor P2X3 (P2rx3, also known as P2x3) mRNA expression is upregulated substantially in chemoreceptive petrosal sensory neurons in rats with hypertension. These neurons generate both tonic drive and hyperreflexia in hypertensive (but not normotensive) rats, and both phenomena are normalized by the blockade of P2X3 receptors. Antagonism of P2X3 receptors also reduces arterial pressure and basal sympathetic activity and normalizes carotid body hyperreflexia in conscious rats with hypertension; no effect was observed in rats without hypertension. We verified P2X3 receptor expression in human carotid bodies and observed hyperactivity of carotid bodies in individuals with hypertension. These data support the identification of the P2X3 receptor as a potential new target for the control of human hypertension.
鉴于对抗高血压药物有抗性和/或对该药物依从性差或耐受性差的个体比例很高,迫切需要治疗高血压的新药。我们在此表明,外周化学感受器产生异常信号,这在高血压中导致血压升高。我们发现,在高血压大鼠的化学感受性岩神经节感觉神经元中,嘌呤能受体P2X3(P2rx3,也称为P2x3)的mRNA表达大幅上调。这些神经元在高血压(而非正常血压)大鼠中产生紧张性驱动和反射亢进,并且这两种现象都通过P2X3受体的阻断而恢复正常。P2X3受体的拮抗作用还可降低高血压清醒大鼠的动脉血压和基础交感神经活动,并使颈动脉体反射亢进恢复正常;在无高血压的大鼠中未观察到效果。我们在人颈动脉体中验证了P2X3受体的表达,并观察到高血压个体的颈动脉体活动亢进。这些数据支持将P2X3受体鉴定为控制人类高血压的潜在新靶点。