Pargyline

Pargyline hydrochloride (Eutonyl, (V-methyl-n-propargylbenzylamine hydrochloride) [306-07-0] M 195.7, m 154-155 , 155 , pK 6.9. Recrystd from EtOH-Et20 and dried in vacuo. It is very soluble in H2O, in which it is unstable. The free base has b 101-103°/ 1mm. It is a glucuronyl transferase inducer and a monoamine oxidase inhibitor, [von Braun et al. Justus Liebigs Ann Chem 445 205 1928, Yeh and Mitchell Experientia 28 298 1972 Langslrom et al. Science 225 1480 1984.]... 

CgHijN 103-67-3) see Amidephrine mesilate Epinastine hydrochloride Lercanidipine hydrochloride Oxilofrine Pargyline... 

CjHjBr 106-96- 7) see. Haloprogin Pargyline Parsalmide Pinazepam Selegiline... 

To measure the spontaneous efflux of DA, we preincubated striatal slices (0.4 mm) in a modified Tyrode s buffer containing pargyline... 

The biogenic amines are the preferred substrates of MAO. The enzyme comes in two flavors, MAO-A and MAO-B, both of which, like FMO, rely on the redox properties of FAD for their oxidative machinery. The two isoforms share a sequence homology of approximately 70% (81) and are found in the outer mitochondrial membrane, but they differ in substrate selectivity and tissue distribution. In mammalian tissues MAO-A is located primarily in the placenta, gut, and liver, while MAO-B is predominant in the brain, liver, and platelets. MAO-A is selective for serotonin and norepinephrine and is selectively inhibited by the mechanism-based inhibitor clorgyline (82). MAO-B is selective for /1-phcncthylaminc and tryptamine, and it is selectively inhibited by the mechanism-based inhibitors, deprenyl and pargyline (82) (Fig. 4.32). Recently, both MAO-A (83) and MAO-B (84) were structurally characterized by x-ray crystallography. 

FIGURE 4.32 Structures of the MAO-A substrates (serotonin, norepinephrine), their deaminated metabolites, and its selective inhibitor, clorgyline, as well as the structures of the MAO-B substrates (/3-phenethylamine, trytamine), their deaminated metabolites, and its selective inhibitors, deprenyl and pargyline. 

Fowler CJ, Mantle TJ, Tipton KF. The nature of the inhibition of rat liver monoamine oxidase types A and B by the acetylenic inhibitors clorgyline, 1-deprenyl and pargyline. Biochem Pharmacol 1982 31(22) 3555-3561. 

Pargyline hydrochloride [306-07-0] 2423C I(2)948C, N(2)964A DP6650000, USP... 

Liao PC, Kuo YM, Chang YC, Lin C, Cherng CF, et al. 2003. Striatal formation of 6-hydroxydopamine in mice treated with pargyline, pyrogallol and methamphetamine. J Neural Transm 110 487. 

All the commonly used MAOIs (monoamine oxidase inhibitors), exemplified by phenelzine, isocarboxazid and pargyline, are irreversible inhibitors of both forms of the enzyme, forming covalent bonds with the active sites... 

Figure 13.4 Various LSDl inhibitors. Suicide inactivators pargyline 5 and tranylcypromine 6. Histone H3 tail 21-amino acid peptide analogs 7-11 as reversible and irreversible inibitors. Noncompetitive polyamine inhibitors 12 and 13.

Paranyline, 218 Parapenzolate bromide, 75 Parasympathetic nervous system, 71 Pargyline, 27 Parkinson s disease, 52,... 

L. Maitre, Monoamine oxidase inhibiting properties of SU-11,739 in the rat. Comparison with pargyline, tranylcypromine, and iproniazid, J. Pharmacol. Exp. Ther. 157 (1967) 81-88. 

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