INT83829

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Context Info
Confidence 0.57
First Reported 1999
Last Reported 2001
Negated 0
Speculated 0
Reported most in Abstract
Documents 3
Total Number 3
Disease Relevance 0
Pain Relevance 0.26

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

cytosol (PNMT) small molecule metabolic process (PNMT) methyltransferase activity (PNMT)
cellular nitrogen compound metabolic process (PNMT)
Anatomy Link Frequency
brain 1
PNMT (Homo sapiens)
Pain Link Frequency Relevance Heat
Clonidine 3 98.48 Very High Very High Very High

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Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated as inhibitors of phenylethanolamine N-methyltransferase (PNMT) and as inhibitors of the binding of clonidine at the alpha(2)-adrenoceptor.
Negative_regulation (inhibitors) of PNMT associated with clonidine
1) Confidence 0.57 Published 1999 Journal J. Med. Chem. Section Abstract Doc Link 10464018 Disease Relevance 0 Pain Relevance 0.10
Compounds 14 and 16 are also quite lipophilic due to the 3-trifluoromethyl moiety and represent promising new leads for the development of new highly selective inhibitors of PNMT, which should be sufficiently lipophilic to penetrate the blood-brain barrier.
Negative_regulation (inhibitors) of PNMT in brain
2) Confidence 0.42 Published 1999 Journal J. Med. Chem. Section Abstract Doc Link 10464018 Disease Relevance 0 Pain Relevance 0.06
A small series of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines (4-fluoro-THBAs; 12-15) were synthesized and evaluated as inhibitors of phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28) and as inhibitors of the binding of clonidine at the alpha(2)-adrenoceptor. 4-Fluoro-THBAs 13-15 displayed selectivity ratios (alpha(2) K(i)/PNMT K(i)) greater than 75 and 4-fluoro-8-nitro-THBA (13) was found to be one of the most selective inhibitors of PNMT known, with a selectivity ratio of greater than 900.
Negative_regulation (inhibitors) of PNMT associated with clonidine
3) Confidence 0.41 Published 2001 Journal J. Med. Chem. Section Abstract Doc Link 11495596 Disease Relevance 0 Pain Relevance 0.10

General Comments

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