pargyline


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pargyline

Eutonyl Pharmacology An MAOI with antidepressant activity; it is less effective than TCAs; it requires abstinence from foods with tyramine; interacts metabolically with other drugs; its use is limited to Pts unresponsive to TCAs and tetracyclic antidepressants and Pts with atypical depression. See Monoamine oxidase inhibitor, Tricyclic antidepressants.
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MAO-dependent oxidation was defined as sensitive to inhibition by 1 mM pargyline, whereas SSAO-dependent oxidation was abolished by 1 mM semicarbazide.
It was tested whether the response to tyramine was sensitive to reference inhibitors: pargyline (MAO-selective) and semicarbazide (SSAO-selective).
Figure 3(a) shows that benzylamine-induced hydrogen peroxide release was inhibited by 1 mM semicarbazide while being resistant to pargyline. Again, the combination of pargyline and semicarbazide did not inhibit further than the SSAO inhibitor semicarbazide alone, leaving unaltered 20% proportion of the signal.
Figure 5 shows that pargyline inhibited the MAO-dependent [[sup.14]C]-tyramine oxidation by hAT.
Aliquots of striatal synaptosomes (50 [micro]l) were warmed for 4 min at 37[degrees]C and incubated for 5 min at 37[degrees]C in glass test-tubes (500 [micro]l final incubation volume) with 500 nM dopamine (0.09 [micro]Ci/ml [[sup.3]H]dopamine was used as trace with unlabeled dopamine) and 1 [micro]M pargyline (to prevent dopamine metabolization by MAO).
Previously, we were able to establish the possibility of artificially creating protracted depressive states in experimental animals by the induction of auto-antibodies to the psycho-stimulant with antidepressive effects sydnophen, as well as to exogenous inhibitors of monoamine oxidase (MAO), antidepressants, pargyline, and deprenyl (Ashmarin, Danilova, Mashkovskii, et al., 1990; Ashmarin, Danilova, Mel'nik, et al.
Immunization was accompanied by the formation of antibodies to pargyline or deprenyl, increased activity of MAO, and changes in the concentration of biogenic amines.
The present study shows that the induction of auto-antibodies following the active immunization of rats with endogenous (isatin) and some exogenous (pargyline, deprenyl) monoamine oxidase inhibitors leads to a depressed state with elements of anxiety in experimental animals.
An open trial of pargyline in the treatment of attention deficit disorder, residual type.
Guilbeau-Frugier et al., "Pargyline reduces renal damage associated with ischaemia-reperfusion and cyclosporin," Nephrology Dialysis Transplantation, vol.
Synaptosomes were suspended in Krebs' buffer (in mM: 115.0 NaCl, 5.0 KC1, 1.0 Ca[Cl.sub.2], 1.2 MgS[O.sub.4], 1.2 K[H.sub.2]P[O.sub.4], 25.0 NaHC[O.sub.3], 11.0 glucose; pH 7.4) plus ascorbic acid (0.1%) and pargyline ([10.sup.-4] M) at 37 [degrees]C, and incubated with the tested fractions ([10.sup.-7]-3 x [10.sup.-4]g/ml) for 10 min before incubation of the radiolabelled amines (GE Healthcare, USA): [[.sup.3.H]]5-HT (102 Ci/mmol - 8nM, 3 min), or [[.sup.3.H]]NA (12 Ci/mmol - 25 nM, 3 min) or [[.sup.3.H]]DA (9.2 Ci/mmol - 25 nM, 1 min).
The I[C.sub.50] values of positive control, L-deprenyl (an MAO-B inhibitor) and pargyline (a nonselective MAO inhibitor), were 0.31 and 1.14 [micro]M and the Ki values were 0.002 and 0.008 [micro]M, respectively (Table 3).