Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route

被引：15

作者：

Blagg, Julian ^{[1
]}

Allerton, Charlotte M. N. ^{[1
]}

Batchelor, David V. J. ^{[1
]}

Baxter, Andrew D. ^{[1
]}

Burring, Denise J. ^{[1
]}

Carr, Christopher L. ^{[1
]}

Cook, Andrew S. ^{[1
]}

Nichols, Carly L. ^{[1
]}

Phipps, Joanne ^{[1
]}

Sanderson, Vivienne G. ^{[1
]}

Verrier, Hugh ^{[1
]}

Wong, Stephen ^{[2
]}

机构：

[1] Pfizer Global Res & Dev, Sandwich CT13 9NJ, Kent, England

[2] Pfizer Global Res & Dev, Dept Neurosci Biol, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 24期

关键词：

dopamine D3 receptor agonist; arylmorpholine; synthesis; intranasal delivery; NASAL DRUG-DELIVERY; ERECTILE DYSFUNCTION; APOMORPHINE SL; DOPAMINE; SAFETY;

D O I：

10.1016/j.bmcl.2007.10.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has > 1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6691 / 6696

页数：6

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