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Literature summary for 2.1.1.28 extracted from

  • Grunewald, G.L.; Lu, J.; Criscione, K.R.; Okoro, C.O.
    Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity (2005), Bioorg. Med. Chem. Lett., 15, 5319-5323.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines several 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines and some enantiomers of 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines. For the phenylethanolamine N-methyltransferase inhibitory potency of different 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines, compounds bearing a lipophilic 7-substituent show higher potency than compounds bearing a hydrophilic 7-substituent. Comparison to the inhibitory activity of the entantiomers of the most potent racemates show that the R-enantiomers are approximately 4fold as potent as their corresponding S-enantiomers. Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
the phenylethanolamine N-methyltransferase inhibitory potency of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline is lower than the of other 1,2,3,4-tetrahydroisoquinolines, some of them show good selectivity due to their extremely low alpha2-adrenoceptor affinity
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Synonyms

Synonyms Comment Organism
PNMT
-
Homo sapiens