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生长抑素(SS)在许多组织中合成,它抑制某些激素或其他细胞产物的分泌。但SS血浆半减期<2分钟,这限制了它的临床应用。为克服上述缺点,Sandoz公司1982年合成了长效SS类似物SMS201-995。该药商品名为Sandostatin,已被FDA批准作为类癌综合征和血管活性肠肽(VIP)瘤的对症治疗药。药理学 SMS201-995为一8肽,其氨基酸排列顺序如下: (D)Phe-Cys-Phs-(D)Trp-Lys-Thr-Cys-Thr(ol) (?) 肽链中间的4个氨基酸残基与SS的一个片断相同,二硫键的环化减少了降解,使其血浆
Somatostatin (SS) is synthesized in many tissues and it inhibits the secretion of certain hormones or other cellular products. However, SS plasma half-time reduction <2 minutes, which limits its clinical application. To overcome these shortcomings, Sandoz company in 1982 synthesized long-acting SS analogs SMS201-995. The drug, Sandostatin, has been approved by the FDA as a symptomatic treatment for carcinoid syndrome and vasoactive intestinal peptide (VIP) tumors. Pharmacological SMS201-995 is an 8-mer peptide whose amino acid sequence is as follows: (D) 4 amino acids in the middle of Phe-Cys-Phs- (D) Trp-Lys-Thr-Cys- Thr (ol) The residue is identical to a fragment of SS, and the disulfide bridge cyclization reduces degradation to make it plasma