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PROADIFEN HYDROCHLORIDE

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PROADIFEN HYDROCHLORIDE Basic information

Product Name:
PROADIFEN HYDROCHLORIDE
Synonyms:
  • SKF-525A HYDROCHLORIDE >98% (PROADIFEN)
  • ALPHA-PHENYL-ALPHA-PROPYLBENZENEACETIC ACID 2-[DIETHYLAMINO]ETHYL ESTER, HCL
  • ALPHA-PHENYL-ALPHA-PROPYLBENZENEACETIC ACID 2-[DIETHYLAMINO]ETHYL ESTER HYDROCHLORIDE
  • SK AND F 525A HYDROCHLORIDE
  • SKF-525A HCL
  • SKF-525A, HYDROCHLORIDE
  • diethylaminoethanolesterofdiphenylpropylaceticacidhydrochloride
  • nsc39690
CAS:
62-68-0
MF:
C23H32ClNO2
MW:
389.96
EINECS:
688-917-8
Product Categories:
  • Inhibitors
  • All Inhibitors
  • Amines
  • Aromatics
  • CLORINE
Mol File:
62-68-0.mol
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PROADIFEN HYDROCHLORIDE Chemical Properties

Melting point:
122-123°C
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
Soluble in DMSO (up to 20 mg/ml)
form 
White solid
color 
Lustrous crystals from Me2CO/pet ether
Water Solubility 
Soluble in methanol or water
Stability:
Store in Freezer
EPA Substance Registry System
Proadifen hydrochloride (62-68-0)
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Safety Information

Hazard Codes 
Xn
Risk Statements 
22
Safety Statements 
36-24/25
WGK Germany 
3
RTECS 
YV7175000
HS Code 
29221990
Toxicity
LD50 oral in rat: 2140mg/kg

MSDS

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PROADIFEN HYDROCHLORIDE Usage And Synthesis

Description

SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM. It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes). SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools. It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).

Chemical Properties

Off-White Crystalline Solid

Uses

anti-infective

Uses

An inhibitor of NOS1, AChR, cytochrome P-450, and KIR6.1.

Uses

Cytochrome P-459 inhibitor; blocks glibenclamide-sensitive K+ channels; inhibits neuronal nitric oxide synthetase; stimulates endothelial cell prostacyclin while inhibiting platelet thromboxane synthesis

Uses

Proadifen hydrochloride is an inhibitor of NOS1, AChR, cytochrome P-450, and KIR6. Proadifen hydrochloride bind to the protein moiety of P-450, also reduced the hypoxic response. of Proadifen hydrochloride have good antiarrhythmic effects. SKF-525A substantially reduced the depletion of cardiac norepinephrine.

Safety Profile

Poison by intraperitoneal, subcutaneous, and intravenous routes. Moderately toxic by ingestion. Experimental reproductive effects. When heated to decomposition it emits very toxic fumes of NOx and HCl.

in vitro

previous study found that when incubated with human liver microsomes, skf525a could undergo cyp-dependent oxidative n-deethylation to its secondary amine metabolite skf8742. in addition, skf525a and its metabolite and primary amine analog all inhibited cyp2b6-, cyp2c9-, cyp2c19-, cyp2d6-, as well as cyp3a-selective reactions to various degrees but had little effect on cyp1a2, cyp2a6, and cyp2e1 reactions [1].

in vivo

animal study found that skf 525a at 1.5-9 mg/kg could reduce or abolish the hypertensive effect of mcn-a-343, dmpp and nicotine, but could neither noticeably affect the hypertensive effect of tyramine, adrenaline and noradrenaline, nor the hypotensive effect of acetylcholine and orciprenaline. thus, skf 525a was able to block the rat sympathetic ganglia and the adrenal medulla and such blockade was non-specific. moreover, the blockade might result from the stabilizing effect of skf 525a on postsynaptic membranes of the sympathetic ganglia and the adrenal medulla [2].

IC 50

in the μm range when tested using human liver microsomes

References

1) Franklin and Hathaway (2008)?2-Diethylaminoethyl-2,2-diphenylvalerate-HCL (SKF525A) revisited: comparative cytochrome P450 inhibition in human liver microsomes by SKF525A, its metabolites, and SKF-acid and SKF-alcohol;?Drug Metab. Dispos,?36?2539 2) Suarez-Kurtz and Bianchi (1970)?Sites of action of SKF-525A in nerve and muscle;?J. Pharmacol. Exp. Ther.,?172?33 3) Spitzmaul?et al. (2009)?The local anesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms; Br. J. Pharmacol.,?157?804 4) Prince and Sine (1999)?Acetylcholine and epibatidine binding to muscle acetylcholine receptors distinguish between concerted and uncoupled models; J. Biol. Chem.,?274?19623 5) Sakust and Yoneda (1994)?Inhibition by SKF 525A and quinacrine of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes; Eur. J. Pharmacol.,?252?117

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