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L-1,2,3,4-四氢-8-甲氧基-5-(甲硫基)-2-萘胺:一种强效且选择性的α1肾上腺素能受体激动剂。

l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: a potent and selective agonist at alpha 1-adrenoceptors.

作者信息

DeMarinis R M, Hieble J P

出版信息

J Med Chem. 1983 Sep;26(9):1215-8. doi: 10.1021/jm00363a002.

DOI:10.1021/jm00363a002
PMID:6136611
Abstract

1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine (SK&F-89748) has been resolved into d and l enantiomers and characterized pharmacologically. The more active isomer is the l, which has the S configuration as established by single-crystal X-ray diffraction studies. This compound is a potent and selective alpha 1-agonist with an EC50 in the isolated perfused rabbit ear artery of 9 +/- 2 nM. In several preparations, it has shown an alpha 1/alpha 2 selectivity ratio of over 100 and will be a useful tool for characterizing receptor subtypes.

摘要

1,2,3,4-四氢-8-甲氧基-5-(甲硫基)-2-萘胺(SK&F-89748)已被拆分为d型和l型对映体并进行了药理学表征。活性更强的异构体是l型,通过单晶X射线衍射研究确定其具有S构型。该化合物是一种强效且选择性的α1-激动剂,在离体灌注兔耳动脉中的EC50为9±2 nM。在几种制剂中,它的α1/α2选择性比率超过100,将成为表征受体亚型的有用工具。

相似文献

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l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: a potent and selective agonist at alpha 1-adrenoceptors.L-1,2,3,4-四氢-8-甲氧基-5-(甲硫基)-2-萘胺:一种强效且选择性的α1肾上腺素能受体激动剂。
J Med Chem. 1983 Sep;26(9):1215-8. doi: 10.1021/jm00363a002.
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引用本文的文献

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Naunyn Schmiedebergs Arch Pharmacol. 1984 Nov;328(1):44-50. doi: 10.1007/BF00496105.
3
Effects of the irreversible alpha-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in pithed rats.
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