Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 23, Pages 5319-5323Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.033
Keywords
phenylethanolamine-N-methyltransferase; inhibitor; alpha(2)-adrenoceptor; selectivity; blood-brain barrier
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Funding
- NHLBI NIH HHS [HL 34193] Funding Source: Medline
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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 alpha(2)-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 a2-adrenoceptor affinity. (c) 2005 Elsevier Ltd. All rights reserved.
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