Stereoselectivity of satropane, a novel tropane analog, on iris muscarinic receptor activation and intraocular hypotension
Stereoselectivity of satropane, a novel tropane analog, on iris muscarinic receptor activation and intraocular hypotension
复制标题
沙托烷（一种新型托烷类似物）对虹膜毒蕈碱受体激活和低眼压的立体选择性
DOI：
10.1111/j.1745-7254.2008.00722.x
复制
发表时间：
2008-02
期刊：
影响因子：
--
通讯作者：
Ren, Qiu-shi
中科院分区：
文献类型：
--
作者：
Zheng, Pei-li;Wei, Pi-jing;Wang, Hao;Chen, Hong-zhuan;Niu, Yin-yao;Yang, Li-min;Zhu, Liang;Cui, Yong-yao;Lu, Yang;Ren, Qiu-shi
摘要
目的：研究一种新型托烷类似物——沙特罗烷（3 - 对甲基苯磺酰氧基 - 6 - 乙酰氧基托烷）对虹膜毒蕈碱受体激活和眼内降压的立体选择性。
方法：放射性配体 - 受体结合测定……
AbstractAim:To study the stereoselectivity of satropane (3-paramethylbenzene sulfonyloxy-6-acetoxy tropane), a novel tropane analog, on iris muscarinic receptor activation and intraocular hypotension.Methods:The assays for radioligand-receptor binding, the contractile responses of isolated iris muscle, the miosis response, and the intraocular hypotension of the enantiomers of satropane were investigated.Results:In the binding analysis, S(-)satropane (lesatropane) completely competed against the [3H]quinuclydinyl benzilate-labeled ligand at muscarinic receptors in the iris muscle, whereas R(+)satropane failed to completely compete. In an isolated iris contractile assay, R,S(±)satropane and S(-)satropane produced a concentration-dependent contractile response with similar efficacy and potency to that of carbachol. R(+)satropane did not induce any contractile response. In the pupil diameter measurement assay in vivo, S(-)satropane induced miosis much more effectively than pilocarpine, while R(+)satropane failed to produce any miosis. In the water loading-induced and methylcellulose-induced ocular hypertensive models, S(-)satropane, but not R(+)satropane, significantly suppressed intraocular pressure at a much lower concentration than pilocarpine.Conclusion:The agonistic and hypotensive properties of satropane on rabbit eyes are stereoselective, with the S(-)isomer being its active form.
登录
查看更多内容
影响因子：
7.3
作者：
T. Cembala;J. D. Sherwin;M. Tidmarsh;B. Appadu;D. Lambert
通讯作者：
T. Cembala;J. D. Sherwin;M. Tidmarsh;B. Appadu;D. Lambert
DOI：
--
发表时间：
1981-08
期刊：
Acta pharmaceutica Sinica
影响因子：
--
作者：
Yao Tr;Chen Za;Yi Dn;Xu Gy
通讯作者：
Yao Tr;Chen Za;Yi Dn;Xu Gy
影响因子：
3.5
作者：
C. Bucolo;G. Campana;R. Toro;S. Cacciaguerra;S. Spampinato
通讯作者：
C. Bucolo;G. Campana;R. Toro;S. Cacciaguerra;S. Spampinato
影响因子：
5
作者：
M. Waelbroeck;X. Hou;J. Wehrle;E. Mutschler;E. V. van Tilburg;W. Menge;H. Timmerman;G. Lambrecht
通讯作者：
M. Waelbroeck;X. Hou;J. Wehrle;E. Mutschler;E. V. van Tilburg;W. Menge;H. Timmerman;G. Lambrecht
DOI：
10.1016/s0736-5748(01)00043-0
发表时间：
2001-10-01
影响因子：
1.8
作者：
Pereira, SPF;Medina, SV;Araujo, EG
通讯作者：
Araujo, EG