Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
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新型 2β-甲甲氧基-3β-[4-(取代的苯硫基)]苯基托烷的合成和单胺转运蛋白亲和力:发现具有皮摩尔效力的选择性 SERT 拮抗剂。
DOI:
10.1016/j.bmcl.2004.12.014
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发表时间:
2005
期刊:
影响因子:
--
通讯作者:
Baldwin,RonaldM
中科院分区:
文献类型:
--
作者:
Tamagnan,Gilles;Alagille,David;Fu,Xing;Kula,NoraS;Baldessarini,RossJ;Innis,RobertB;Baldwin,RonaldM
Preparation of cocaine analogues has been aimed largely at development of stable compounds with high affinity and selectivity for the dopamine transporter (DAT). We now report the synthesis and monoamine transporter affinity of 10 new 2β-carbomethoxy-3β-[4-(substituted thiophenyl)]phenyltropanes. Among these, compound 4b exhibited very high affinity for the serotonin transporter (SERT: Ki=17pM) and good selectivity over dopamine (DAT: 710-fold) and norepinephrine transporters (NET: 11,100-fold).
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DOI:
--
发表时间:
1983
期刊:
Biochimica et Biophysica Acta
影响因子:
--
作者:
D. Quissell;K. Barzen;L. M. Deisher
通讯作者:
L. M. Deisher
DOI:
10.1016/s0021-9258(19)44348-2
发表时间:
1973
期刊:
The Journal of biological chemistry
影响因子:
--
作者:
D. Garbers;N. First;H. Lardy
通讯作者:
H. Lardy
影响因子:
2.4
作者:
G. Ronquist;I. Brody;A. Gottfries;B. Stegmayr
通讯作者:
G. Ronquist;I. Brody;A. Gottfries;B. Stegmayr
DOI:
--
发表时间:
1987
期刊:
Biochemistry international
影响因子:
--
作者:
Wilson,MJ
通讯作者:
Wilson,MJ
DOI:
10.1016/0009-8981(82)90032-8
发表时间:
1982
期刊:
Clinica chimica acta; international journal of clinical chemistry
影响因子:
--
作者:
C. Laurell;H. Weiber;K. Ohlsson;G. Rannevik
通讯作者:
G. Rannevik