Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Analogues of Luteinizing Hormone-Releasing Hormone with Modification in Position 3
矢部 裕一郎三浦 千枝子掘越 大能馬場 義彦
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1976 年 24 巻 12 号 p. 3149-3157

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Six analogues of LH-RH, in which the tryptophan residue in position 3 was replaced by nonprotein amino acids, were synthesized and evaluated for their LH-RH activity. The analogues substituted by amino acids having the fused aromatic ring structure in the side-chain retained relatively high biological activity. In particular, the potency of [3- (1-naphthyl)-L-alanine]3-LH-RH was 187.1% of that of synthetic LH-RH. The results demonstrate that the fused aromatic ring structure of the side-chain in position 3 is a favorable factor, and that the indolyl NH group in the Trp residue is not essential.
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© The Pharmaceutical Society of Japan
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