This nonselective P450 inhibitor (FWfree-base = 353.50 g/mol; CAS 302-33-0;
62-68-0 for the HCl salt), also known as SKF-525A, b-diethylaminoethyl
2,2-diphenylpropylacetate, and N,N-diethylaminoethyl 2,2-
diphenylvalerate, blocks glibenclamide-sensitive K+ channels, including
ATP-sensitive inward rectifier potassium channel 8 (KIR6.1). As a
nonselective inhibitor of cytochrome P450 systems, proadifen also inhibits
drug metabolism, thereby potentiating the action of many pharmaceuticals.
For example, proadifen inhibits the demethylation of 2-methoxyestrogens
. Target (s) : aldehyde oxidase; alkanal monooxygenase, FMN-
linked; aromatase, or CYP19; bacterial luciferase, or alkanal
monooxygenase, FMN-linked; benzoate 4-monooxygenase;
bromomethane monooxygenase7; calcium influx8; ent-copalyl-diphosphate
synthase; CYPC211; cytochrome P450; diamine N-
acetyltransferase; N,N-dimethylaniline demethylase; ecdysone 20-
monooxygenase; ethoxyresorufin O-deethylase; flavin-containing
monooxygenase, or dimethylaniline-N-oxide aldolase; glyceollin
synthase; 2-hydroxyisoflavanone synthase; 25-hydroxyvitamin D3
24-monooxygenase; isopentenyl-diphosphate D-isomerase, or
isopentenyl-pyrophosphate D-isomerase; ent-kaurene synthase;
leukotriene B4 20-hydroxylase; (S) -limonene 3-monooxygenase;
(S) -limonene 6-monooxygenase; (S) -limonene 7-monooxygenase;
methane monooxygenase; monoamine oxidase;
NADPH:cytochrome P450 reductase; nitric-oxide synthase, neuronal
; pentoxyresorufin O-depentylase; phenol O-methyltransferase
; progesterone 11a-monooxygenase; steroid 11b-monooxygenase
; steroid 21-monooxygenase, or CYP21A1, weakly inhibited;
sterol 14-demethylase, or CYP51; styrene monooxygenase; thiol
S-methyltransferase; thromboxane production; and
trimethylamine-oxide aldolase.
