Benzphetamine

Reduction of phenylacetone in the presence of methylamine rather than ammonia gives methamphetamine (53), an agent similar in action to the primary amine. Alkylation of 53 with benzyl chloride affords the analog, benzphetamine (54). ... 

Benzethonium chloride Benzphetamine HCI Bephenium hydroxynaphthoate Bufeniode Diazoxide Ifenprodil tartrate Phenoxybenzamine HCI Propoxyphene HCI Tiopronin T ribenoside... 

Hydroxydione sodium succinate d-Desoxyephedrine HCI Benzphetamine HCI 11 -Desoxy-17-hydroxycorticosterone Hydrocortisone 3 -Diacetoxyacetophenone Fenoterol hydrobromide Metaproterenol sulfate 3,17-Diacetoxy-5a-androstane-2,16-diene... 

Chemical Structures. Figure 1 shows the chemical structures for 14 phenylethylamine compounds. Nine of these compounds are used clinically as anorectics (ii-amphetamine, phentermine, diethylpropion, phenmetrazine, phendimetrazine, clotermine, chlorphentermine, benzphetamine, and fenfluramine). Four of these compounds are not approved for clinical use and are reported to have hallucinogenic properties (MDA, PMA, DOM, and DOET). The final compound ( /-ephedrine) is used clinically for bronchial muscle relaxation, cardiovascular, and mydriatic effects. Figure 2 shows the chemical structure for MDMA, the methyl analog of MDA. MDMA is not approved for clinical use and has been reported to produce both LSD-like and cocaine-like effects. 

Figure 3 presents the mean levels of self-infusion for the 14 phenylethyl-amines shown in figure 1. Of all the drugs tested, injection rates were... 

W. I. Higuchi and W. E. Hamlin, Release of drug from a self-coating surface Benzphetamine pamoate pellet, J. Pharm. Sci., 52, 575-579 (1963). 

People who are obese, and who have diabetes, often find they initially cannot control their blood sugar well. Therefore, these patients must increase the number of times each day they monitor their blood sugar. Benzphetamine, out of the entire amphetamine class, causes less stimulant activity this quality could make it more attractive to doctors. But tolerance (the body s ability to resist the effects of the drug) can develop quickly and adequate weight loss has not been observed beyond six months. 

A biosensor based on mediator-free CYP2B4 catalysis by immobilizing monomer-ized CYP2B4 in montmorillonite was studied by Shumyantseva [222], When substrates were added to air saturated buffer solution, there was an increase in the reduction current. A typical concentration dependence measured in chronamperometry is shown for aminopyrine and benzphetamine (Fig. 17.4). The reaction was inhibited by metyrap-one. This indicates the catalytic activity of CYP2B4 in the presence of substrate. 

In this study, P-450-related enzyme activities (benzphetamine N-demethylase, 7-ethoxycoumarin O-deethylase) were also measured in liver homogenates (prepared 24 hours after the last treatment) from rats treated orally with MEK for 1-7 days and compared to the activity obtained with phenobarbital treatment (80 mg/kg intraperitoneally for 3 days) (Robertson et al. 1989). Total cytochrome P-450 was also measured. No consistent change was noted in benzphetamine N-demethylase activity as the result of MEK treatment, while 7-ethoxycoumarin O-deethylase was over 3 times higher than controls and comparable to phenobarbital induction. Total P-450 levels were increased to approximately 150-200% of controls with MEK and to 570% of control by phenobarbital. The authors concluded that the potentiating effects of MEK on the neurotoxicity of -hexane appear to arise, at least in part, from the activating effects of MEK on selected microsomal enzymes responsible for -hexane activation. 

Stevens JT, Chernoff N, Farmer JD, et al. 1979. Perinatal toxicology of mirex administered in the diet II. Relation of hepatic mirex levels to induction of microsomal benzphetamine N-demethylase activity. Toxicol Lett 4(4) 269-274. 

Arylhydrocarbon (benzo[a]pyrene) hydroxylase, benzphetamine-N-demethylation, ethylmorphine-N-demethylation, ethoxycoumarin-0-deethylation and ethoxyresorufin-0-deethylation were performed by published procedures (31,32,33,34), but optimized for use with trout microsomes as described previously (30, 35). Hemoprotein P-450 was determined by the procedure of Estabrook et al. (36) to avoid spectral interference by hemoglobin. Microsomal protein content was estimated either by the method of Ross and Shatz (37) or Lowry et al. (38), using bovine serum albumin standards. 

Ethylmorphine and benzphetamine are N-demethylated specifically by rodent cytochrome(s) P-450 (as opposed to cytochrome(s) P] -450) in the rat phenobarbital and the polyhalogenated biphenyls induce these demethylation reactions. However, it is clear that no such stimulation occurred in the rainbow trout (Table II). 

In this study, we have utilized 2,2, 4,4 -tetrachlorobiphenyl and 3,3, 4,4 -tetrachlorobiphenyl as representative non-coplanar and coplanar isomers respectively. The 3,3, 4,4 -tetrachlordbi-phenyl isomer (0.3mmole/kg) induced ethoxycoumarin-and ethoxy-resorufin-O-deethylations in the rainbow trout to a similar extent as did Aroclor 1242 (Table III). However, the non-coplanar 2,2 -4,4 -tetrachlorobiphenyl was without effect upon any of the monooxygenase activities examined. Cytochrome P -450-like activity as determined by ethoxyresorufin-O-deethylation was increased by the planar 3,3, 4,4 -tetrachlorobiphenyl while cytochrome P-450-like activity (benzphetamine-N-demethylation) was unaffected. 

BENZPHETAMINE HYDROCHLORIDE Initiate dosage with 25 to 50 mg once/day increase according to response. Dosage ranges from 25 to 50 mg, 1 to 3 times/day. DIETHYLPROPION HYDROCHLORIDE ... 

Pregnancy (Category X - benzphetamine hydrochloride Category C - sibutramine, phentermine, phendimetrazine Category B - diethylpropion). 

The binding of sulfur and/or an activated intermediate of the phosphorus-containing portion of the parathion molecule to the endoplasmic reticulum leads to a decrease in the amount of cytochrome P-450 detectable as its carbon monoxide complex and to a decrease in the rate of metabolism of substrates such as benz-phetamine ( 19). Neither paraoxon nor any other isolatable metabolite of parathion decreases the amount of cytochrome P-450 or inhibits the ability of microsomes to metabolize substrates such a benzphetamine (19). 

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