Hartrodt B, Neubert K, Jakubke H D, Baláspiri L, Telegdy G
Pharmazie. 1982 Dec;37(12):821-4.
The authors describe the synthesis of a shorter-chained somatostatin analogue in which the ring size of the native molecule is largely preserved by incorporation of S-carboxymethyl-L-homocysteinamid and ring closure via its side-chain function. This synthesis involves the linkage of Boc-Phe-D-Trp-Lys[Z(pCl)]-Thr-Phe-Thr-Ser-OH to H-Hcy(CH2-CO-Lys[Z(oCl)]-Asn-Phe-OMe)-NH2 and subsequent azide cyclization. In contrast to somatostatin, the somatostatin analogue thus obtained produces, when applied intracerebroventricularly to rats, a decrease in the dopamine content of the striatum.
作者描述了一种短链生长抑素类似物的合成方法，其中通过掺入S-羧甲基-L-高半胱氨酸酰胺并经由其侧链功能进行环化，在很大程度上保留了天然分子的环大小。该合成涉及将Boc-Phe-D-Trp-Lys[Z(pCl)]-Thr-Phe-Thr-Ser-OH与H-Hcy(CH2-CO-Lys[Z(oCl)]-Asn-Phe-OMe)-NH2连接，随后进行叠氮化物环化。与生长抑素相比，如此获得的生长抑素类似物经脑室内注射给大鼠后，会使纹状体中的多巴胺含量降低。
