Jain Kishor S, Bariwal Jitender B, Kathiravan Muthu K, Phoujdar Manisha S, Sahne Rajkumari S, Chauhan Bishram S, Shah Anamik K, Yadav Mange Ram
Sinhgad College of Pharmacy, Pune 411041, India.
Bioorg Med Chem. 2008 May 1;16(9):4759-800. doi: 10.1016/j.bmc.2008.02.091. Epub 2008 Mar 4.
Hypertension is one of the most serious health problems of the modern world with a continuous rise in the number of patients. Selective alpha(1)-adrenoreceptor antagonists though have many advantages and uses in the management of arterial hypertension, their lack of specificity at the level of alpha(1)-adr subtypes leads to multiple side effects. Existence of multiple alpha(1)-adr subtypes holds great promise for the discovery and development of more specific and selective drug molecules, targeting only one alpha(1)-adr subtype at a time and thus relative freedom from side effects. Herein, the research done on the discovery and evaluation of a variety of chemically diverse structures as selective antagonists of alpha(1)-adr and alpha(1)-adr subtypes in recent years has been reviewed.
高血压是现代社会最严重的健康问题之一,患者数量持续上升。选择性α(1)-肾上腺素能受体拮抗剂尽管在动脉高血压的治疗中有许多优点和用途,但它们在α(1)-肾上腺素能受体亚型水平上缺乏特异性,会导致多种副作用。多种α(1)-肾上腺素能受体亚型的存在为发现和开发更具特异性和选择性的药物分子带来了巨大希望,这些药物分子一次仅作用于一种α(1)-肾上腺素能受体亚型,从而相对避免副作用。本文综述了近年来针对多种化学结构各异的化合物作为α(1)-肾上腺素能受体及α(1)-肾上腺素能受体亚型选择性拮抗剂的发现和评估所开展的研究。