Title of article
Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity
Author/Authors
Joanne M. Caine and Gary L. Grunewald، نويسنده , , Jian Lu، نويسنده , , Kevin R. Criscione، نويسنده , , Cosmas O. Okoro، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
5319
To page
5323
Abstract
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the α2-adrenoceptor. Although their PNMT inhibitory potency decreased compared with corresponding 3-methyl-, 3-hydroxymethyl- or 3-unsubstituted-THIQs, some of them showed good selectivity due to their extremely low α2-adrenoceptor affinity.
Keywords
?2-Adrenoceptor , Selectivity , inhibitor , Phenylethanolamine-N-methyltransferase , Blood–brain barrier
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796182
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