Nguyen B N, Johnson J A
Department of Clinical Pharmacy, College of Pharmacy, University of Tennessee, Memphis, USA.
Pharmacotherapy. 1998 Jul-Aug;18(4):706-19.
The endothelin family consists of three structurally similar isopeptides: ET-1, ET-2, and ET-3. The two receptor subtypes, ETA and ETB, have different receptor affinities for the isopeptides. Stimulation of ETA and ETB receptors results in vasoconstriction, and ETB stimulation also causes vasodilation. These receptors may have profound impact on the etiologies of various diseases, including heart failure and hypertension. Studies with endothelin-receptor antagonists in animals and humans with heart failure show promising short- and long-term results. The place of the agents in the treatment of essential hypertension remains controversial, but they may have a greater role in hypertensive blacks and transplant recipients.
ET-1、ET-2和ET-3。两种受体亚型,即ETA和ETB,对这些异肽具有不同的受体亲和力。刺激ETA和ETB受体会导致血管收缩,而刺激ETB受体也会引起血管舒张。这些受体可能对包括心力衰竭和高血压在内的各种疾病的病因产生深远影响。在动物和心力衰竭患者中使用内皮素受体拮抗剂的研究显示出了有前景的短期和长期结果。这些药物在原发性高血压治疗中的地位仍存在争议,但它们可能在黑人高血压患者和移植受者中发挥更大作用。