2- isopropenyl-2-methyladamantane

Lists of the reported inhibitors of P450 2B6 have been compiled by Rendic. Orphenadine had been utilized in some work with microsomes but does not appear to be particularly selective More recently 2-isopropenyl-2-methyladamantane and 3-isopropenyl-3-methyldiamantane have been reported as selective inhibitors of P450 2B6 (ref [368]). Triethylenethiophosphoramide has also been reported to be a selective inhibitor of P450 2B6 (ref [369]). 

B6 (iS)Mephenytoin Af-demethylation 7-Ethoxy-4-trifluoromethylcoumarin 0-deethylation" Bupropion hydroxylation Phenobarbital 2- Isopropenyl-2-methyladamantane 3- Isopropenyl-3-methyldiadamantane Triethylenethiophosphoramide" Ticlopidine Clopidogrel 5-Mephenytoin "... 

The arrow indicates the inhibitor site that is metabolically activated by that P450 isoform resulting in mechanism-based inactivation (MBl) of the enzyme that is either irreversible (suicide, S) or quasi-irreversible (Ql). inhibitor acts competitively by coordinating to the P450 heme-iron and/or ligation to the protein at the active site. 2-PMADA, 2-isopropenyl-2-methyladamantane. 

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See also in sourсe #XX -- [ , , ]

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