Abstract:
:1,2,3,4-Tetrahydropyrazino[1,2-a]indoles are described as a novel class of I(2) imidazoline receptor ligands. In particular, 8-methoxy-1,2,3,4-tetrahydropyrazino[1,2-a]indole (8-OMe THPI; 3c) binds with high affinity at I(2) imidazoline receptors (K(i)=6.2 nM) and with exceptional (> or =1000-fold) selectivity relative to its affinity for I(1) imidazoline receptors, alpha(2)adrenergic receptors, and 5-HT(2A) and 5-HT(2C) serotonin receptors.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Chang-Fong J,Tyacke RJ,Lau A,Westaway J,Hudson AL,Glennon RAdoi
10.1016/j.bmcl.2003.12.033subject
Has Abstractpub_date
2004-02-23 00:00:00pages
1003-5issue
4eissn
0960-894Xissn
1464-3405pii
S0960894X03013209journal_volume
14pub_type
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