STRUCTURE ACTIVITY RELATIONSHIP OF ORALLY ACTIVE ENKEPHALIN ANALOGS AS ANALGESICS

被引：60

作者：

ROEMER, D ^{[1
]}

PLESS, J ^{[1
]}

机构：

[1] SANDOZ LTD,DIV CHEM RES,CH-4002 BASEL,SWITZERLAND

来源：

LIFE SCIENCES | 1979年 / 24卷 / 07期

关键词：

D O I：

10.1016/0024-3205(79)90159-0

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Substitution of glycine in position 2 of the naturally occurring methionine-enkephalin by D-alanine, methylation of tyrosine and phenylalanine i in position 1 and 4 respectively and conversion of the methionine in position 5 to the corresponding alcohol sulfoxide lead to potent orally active enkephalin analogues with marked analgesic properties. © 1979.

引用

页码：621 / 624

页数：4

共 4 条

[1] SUPERACTIVE ANTINOCICEPTIVE PENTAPEPTIDE, (D-MET2,PRO5), ENKEPHALINAMIDE
BAJUSZ, S
RONAI, AZ
SZEKELY, JI
GRAF, L
DUNAIKOVACS, Z
BERZETEI, I
[J]. FEBS LETTERS, 1977, 76 (01) : 91 - 92
[2] D'amour FE, 1941, J PHARMACOL EXP THER, V72, P74
[3] IDENTIFICATION OF 2 RELATED PENTAPEPTIDES FROM BRAIN WITH POTENT OPIATE AGONIST ACTIVITY
HUGHES, J
SMITH, TW
KOSTERLITZ, HW
FOTHERGILL, LA
MORGAN, BA
MORRIS, HR
[J]. NATURE, 1975, 258 (5536) : 577 - 579
[4] SYNTHETIC ENKEPHALIN ANALOG WITH PROLONGED PARENTERAL AND ORAL ANALGESIC ACTIVITY
ROEMER, D
BUESCHER, HH
HILL, RC
PLESS, J
BAUER, W
CARDINAUX, F
CLOSSE, A
HAUSER, D
HUGUENIN, R
[J]. NATURE, 1977, 268 (5620) : 547 - 549

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