THE ANALGESIC EFFECT OF EPIBATIDINE AND ISOMERS

被引：49

作者：

LI, TC

QIAN, CG

ECKMAN, J

HUANG, DF

SHEN, TY

机构：

[1] UNIV VIRGINIA,DEPT CHEM,CHARLOTTESVILLE,VA 22903

[2] CYTOMED INC,CAMBRIDGE,MA 02139

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80759-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The racemic form, d and l-enantiomers and the 7-N-methyl derivative of synthetic epibatidine are equally potent at 10 mug/kg in the tail-flick analgesic model without any enantioselectivity, whereas the endo-stereoisomer is not active at 1 mg/kg. The analgesic response is not antagonized by pretreatment with naloxone.

引用

页码：2759 / 2764

页数：6

共 9 条

[1] TOTAL SYNTHESIS OF EPIBATIDINE
BROKA, CA
[J]. TETRAHEDRON LETTERS, 1993, 34 (20) : 3251 - 3254
[2] Chau TT, 1989, PHARM METHODS CONTRO, P195
[3] D'amour FE, 1941, J PHARMACOL EXP THER, V72, P74
[4] NEW CLASS OF INDOLIZIDINE ALKALOIDS FROM THE POISON FROG, DENDROBATES-TRICOLOR - X-RAY-ANALYSIS OF 8-HYDROXY-8-METHYL-6-(2'-METHYLHEXYLIDENE)-1-AZABICYCLO[4.3.0]NONANE
DALY, JW
TOKUYAMA, T
FUJIWARA, T
HIGHET, RJ
KARLE, IL
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1980, 102 (02) : 830 - 836
[5] DEWEY WL, 1971, J PHARMACOL EXP THER, V179, P652
[6] THE SYNTHESIS OF (+)-EPIBATIDINE AND (-)-EPIBATIDINE
FLETCHER, SR
BAKER, R
CHAMBERS, MS
HOBBS, SC
MITCHELL, PJ
[J]. JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1993, (15) : 1216 - 1218
[7] A VERSATILE TOTAL SYNTHESIS OF EPIBATIDINE AND ANALOGS
HUANG, DF
SHEN, TY
[J]. TETRAHEDRON LETTERS, 1993, 34 (28) : 4477 - 4480
[8] Liu H., UNPUB
[9] EPIBATIDINE - A NOVEL (CHLOROPYRIDYL)AZABICYCLOHEPTANE WITH POTENT ANALGESIC ACTIVITY FROM AN ECUADORIAN POISON FROG
SPANDE, TF
GARRAFFO, HM
EDWARDS, MW
YEH, HJC
PANNELL, L
DALY, JW
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1992, 114 (09) : 3475 - 3478

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