α-Human atrial natriuretic peptide (α-hANP) was synthesized by assembling six peptide fragments in solution followed by deprotection with HF and subsequent air-oxidation. The trimethylbenzyl group was employed as an S-protecting group of cysteine. The HF-dimethylselenide-m-cresol system was employed as a final deprotecting reagent and, at the same time, as a reducing reagent of Met(O). Syntheric α-hANP elicited potent diuretic and natriuretic activity in rats.
α-人心房利
钠肽(α-hANP)是通过在溶液中组装六个肽片段,然后用
氢氟酸脱保护并随后进行空气
氧化合成的。三
甲基苄基被用作半胱
氨酸的 S 保护基团。
氢氟酸-
二甲基硒-
间甲酚体系被用作最终的
脱保护试剂,同时也是 Met(O) 的还原试剂。合成的 α-hANP 对大鼠具有强效的利尿和利
钠活性。