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Development of specific and non-specific somatostatin analogs.
Horm Metab Res. 1986 Feb; 18(2):98-102.HM

Abstract

Biological activity of six somatostatin analogs has been investigated. In these analogs, disulfide bond is replaced by ethylene bond cyclized with alpha-amino suberic acid. In addition, they contain unique D-configuration in both Trp8 and Cys14 moiety with dicarba substitution. An analog of the short chain length, C omega 7-cyclo (Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11-D-Asu14) (analog 4) has suppressive effect for GH, but not for other hormones. Analog 6, C omega 9-cyclo(Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Ph e11-Thr12-D-Asu14), has suppressed GH and insulin secretion, but not for gastrin and glucagon. Analog 1, C omega 11-cyclo (Lys4-Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11- Thr12-Ser13-D-Asu14] and 5, C omega 9-cyclo (Lys4-Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11-D-+ ++Asu14) have broad suppressive effect for GH, gastrin, insulin and glucagon release after arginine infusion. The shortest analog, analog 2, C omega 5-cyclo (Phe7-D-Trp8-Lys9-Thr10-D-Asu14) has weak suppressive effect of GH, insulin and glucagon secretion, and it is suggested that Phe6 and Phe11 are necessary for the appearance of suppressive effect of GH. Specific analog, analog 4, may be useful for the future treatment for acromegaly and diabetic retinopathy. Nonspecific analogs, 1 and 5 are candidates for the clinical application of wide variety.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

2870971

Citation

Nakano, T, et al. "Development of Specific and Non-specific Somatostatin Analogs." Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Metabolisme, vol. 18, no. 2, 1986, pp. 98-102.
Nakano T, Harano Y, Emura J, et al. Development of specific and non-specific somatostatin analogs. Horm Metab Res. 1986;18(2):98-102.
Nakano, T., Harano, Y., Emura, J., Kimura, T., Sakakibara, S., & Shigeta, Y. (1986). Development of specific and non-specific somatostatin analogs. Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Metabolisme, 18(2), 98-102.
Nakano T, et al. Development of Specific and Non-specific Somatostatin Analogs. Horm Metab Res. 1986;18(2):98-102. PubMed PMID: 2870971.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of specific and non-specific somatostatin analogs. AU - Nakano,T, AU - Harano,Y, AU - Emura,J, AU - Kimura,T, AU - Sakakibara,S, AU - Shigeta,Y, PY - 1986/2/1/pubmed PY - 1986/2/1/medline PY - 1986/2/1/entrez SP - 98 EP - 102 JF - Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme JO - Horm Metab Res VL - 18 IS - 2 N2 - Biological activity of six somatostatin analogs has been investigated. In these analogs, disulfide bond is replaced by ethylene bond cyclized with alpha-amino suberic acid. In addition, they contain unique D-configuration in both Trp8 and Cys14 moiety with dicarba substitution. An analog of the short chain length, C omega 7-cyclo (Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11-D-Asu14) (analog 4) has suppressive effect for GH, but not for other hormones. Analog 6, C omega 9-cyclo(Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Ph e11-Thr12-D-Asu14), has suppressed GH and insulin secretion, but not for gastrin and glucagon. Analog 1, C omega 11-cyclo (Lys4-Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11- Thr12-Ser13-D-Asu14] and 5, C omega 9-cyclo (Lys4-Asn5-Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11-D-+ ++Asu14) have broad suppressive effect for GH, gastrin, insulin and glucagon release after arginine infusion. The shortest analog, analog 2, C omega 5-cyclo (Phe7-D-Trp8-Lys9-Thr10-D-Asu14) has weak suppressive effect of GH, insulin and glucagon secretion, and it is suggested that Phe6 and Phe11 are necessary for the appearance of suppressive effect of GH. Specific analog, analog 4, may be useful for the future treatment for acromegaly and diabetic retinopathy. Nonspecific analogs, 1 and 5 are candidates for the clinical application of wide variety. SN - 0018-5043 UR - https://www.unboundmedicine.com/medline/citation/2870971/Development_of_specific_and_non_specific_somatostatin_analogs_ L2 - https://www.thieme-connect.com/DOI/DOI?10.1055/s-2007-1012241 DB - PRIME DP - Unbound Medicine ER -