(-)deprenyl and (-)1-phenyl-2-propylaminopentane, [(-) PPAP], act primarily as potent stimulants of action potential - Transmitter release coupling in the catecholaminergic neurons

J. Knoll, Ildikó Miklya, Berta Knoll, Raissa Markó, Károly Kelemen

Research output: Contribution to journalArticle

47 Citations (Scopus)

Abstract

The activity of the catecholaminergic neurons in the rat brain is enhanced significantly 30 min after the subcutaneous injection of very small doses of (-)deprenyl (threshold doses: 0.01 mg/kg for noradrenergic neurons and 0.025 mg/kg for dopaminergic neurons). As a catecholaminergic activity enhancer (CAE) substance (-)deprenyl is about ten times more potent than its parent compound, (-)methamphetamhie. While the (+)methamphetamine is 3-5 times more potent than (-)methamphetamine in releasing catecholamines, the (-)methamphetamine is the more potent CAE substance. The mechanism of the CAE effect of (-)deprenyl and (-)PPAP, a deprenyl-derived substance devoid of MAO inhibitory potency, was studied in rats by measuring: a) the release of catecholamines from striatum, substantia nigra, tuberculum olfactorium and locus coeruleus; b) the stimulation induced release of 3H-noradrenaline from the isolated brain stem; and c) the antagonistic effect against tetrabenazine-induced depression of learning in the shuttle box. The CAE effect was found to be unrelated: a) to the inhibition of MAO activity; b) to the inhibition of presynaptic catecholamine receptors; c) to the inhibition of the uptake of catecholamines; and d) to the release of catecholamines. It was concluded that (-)deprenyl and (-)PPAP act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons of the brain. We show that both (-)deprenyl and (-)PPAP enhance the inward Ca2+ current in sino-auricular fibers of the frog heart. (-)PPAP was much more potent than either (+)PPAP or (-)deprenyl hi this test.

Original languageEnglish
Pages (from-to)817-827
Number of pages11
JournalLife Sciences
Volume58
Issue number10
DOIs
Publication statusPublished - Feb 2 1996

Fingerprint

Selegiline
Action Potentials
Neurons
Transmitters
Catecholamines
Methamphetamine
Brain
Monoamine Oxidase
Rats
Catecholamine Receptors
Tetrabenazine
Presynaptic Receptors
Adrenergic Neurons
Locus Coeruleus
Dopaminergic Neurons
Substantia Nigra
Subcutaneous Injections
Anura
Brain Stem
Norepinephrine

Keywords

  • (-)deprenyl
  • (-)methamphetamine
  • (-)PPAP
  • Catecholaminergic activity enhancer effect

ASJC Scopus subject areas

  • Pharmacology

Cite this

(-)deprenyl and (-)1-phenyl-2-propylaminopentane, [(-) PPAP], act primarily as potent stimulants of action potential - Transmitter release coupling in the catecholaminergic neurons. / Knoll, J.; Miklya, Ildikó; Knoll, Berta; Markó, Raissa; Kelemen, Károly.

In: Life Sciences, Vol. 58, No. 10, 02.02.1996, p. 817-827.

Research output: Contribution to journalArticle

@article{13597d4ed3f648d5a5b707b6de092969,
title = "(-)deprenyl and (-)1-phenyl-2-propylaminopentane, [(-) PPAP], act primarily as potent stimulants of action potential - Transmitter release coupling in the catecholaminergic neurons",
abstract = "The activity of the catecholaminergic neurons in the rat brain is enhanced significantly 30 min after the subcutaneous injection of very small doses of (-)deprenyl (threshold doses: 0.01 mg/kg for noradrenergic neurons and 0.025 mg/kg for dopaminergic neurons). As a catecholaminergic activity enhancer (CAE) substance (-)deprenyl is about ten times more potent than its parent compound, (-)methamphetamhie. While the (+)methamphetamine is 3-5 times more potent than (-)methamphetamine in releasing catecholamines, the (-)methamphetamine is the more potent CAE substance. The mechanism of the CAE effect of (-)deprenyl and (-)PPAP, a deprenyl-derived substance devoid of MAO inhibitory potency, was studied in rats by measuring: a) the release of catecholamines from striatum, substantia nigra, tuberculum olfactorium and locus coeruleus; b) the stimulation induced release of 3H-noradrenaline from the isolated brain stem; and c) the antagonistic effect against tetrabenazine-induced depression of learning in the shuttle box. The CAE effect was found to be unrelated: a) to the inhibition of MAO activity; b) to the inhibition of presynaptic catecholamine receptors; c) to the inhibition of the uptake of catecholamines; and d) to the release of catecholamines. It was concluded that (-)deprenyl and (-)PPAP act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons of the brain. We show that both (-)deprenyl and (-)PPAP enhance the inward Ca2+ current in sino-auricular fibers of the frog heart. (-)PPAP was much more potent than either (+)PPAP or (-)deprenyl hi this test.",
keywords = "(-)deprenyl, (-)methamphetamine, (-)PPAP, Catecholaminergic activity enhancer effect",
author = "J. Knoll and Ildik{\'o} Miklya and Berta Knoll and Raissa Mark{\'o} and K{\'a}roly Kelemen",
year = "1996",
month = "2",
day = "2",
doi = "10.1016/0024-3205(96)00014-8",
language = "English",
volume = "58",
pages = "817--827",
journal = "Life Sciences",
issn = "0024-3205",
publisher = "Elsevier Inc.",
number = "10",

}

TY - JOUR

T1 - (-)deprenyl and (-)1-phenyl-2-propylaminopentane, [(-) PPAP], act primarily as potent stimulants of action potential - Transmitter release coupling in the catecholaminergic neurons

AU - Knoll, J.

AU - Miklya, Ildikó

AU - Knoll, Berta

AU - Markó, Raissa

AU - Kelemen, Károly

PY - 1996/2/2

Y1 - 1996/2/2

N2 - The activity of the catecholaminergic neurons in the rat brain is enhanced significantly 30 min after the subcutaneous injection of very small doses of (-)deprenyl (threshold doses: 0.01 mg/kg for noradrenergic neurons and 0.025 mg/kg for dopaminergic neurons). As a catecholaminergic activity enhancer (CAE) substance (-)deprenyl is about ten times more potent than its parent compound, (-)methamphetamhie. While the (+)methamphetamine is 3-5 times more potent than (-)methamphetamine in releasing catecholamines, the (-)methamphetamine is the more potent CAE substance. The mechanism of the CAE effect of (-)deprenyl and (-)PPAP, a deprenyl-derived substance devoid of MAO inhibitory potency, was studied in rats by measuring: a) the release of catecholamines from striatum, substantia nigra, tuberculum olfactorium and locus coeruleus; b) the stimulation induced release of 3H-noradrenaline from the isolated brain stem; and c) the antagonistic effect against tetrabenazine-induced depression of learning in the shuttle box. The CAE effect was found to be unrelated: a) to the inhibition of MAO activity; b) to the inhibition of presynaptic catecholamine receptors; c) to the inhibition of the uptake of catecholamines; and d) to the release of catecholamines. It was concluded that (-)deprenyl and (-)PPAP act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons of the brain. We show that both (-)deprenyl and (-)PPAP enhance the inward Ca2+ current in sino-auricular fibers of the frog heart. (-)PPAP was much more potent than either (+)PPAP or (-)deprenyl hi this test.

AB - The activity of the catecholaminergic neurons in the rat brain is enhanced significantly 30 min after the subcutaneous injection of very small doses of (-)deprenyl (threshold doses: 0.01 mg/kg for noradrenergic neurons and 0.025 mg/kg for dopaminergic neurons). As a catecholaminergic activity enhancer (CAE) substance (-)deprenyl is about ten times more potent than its parent compound, (-)methamphetamhie. While the (+)methamphetamine is 3-5 times more potent than (-)methamphetamine in releasing catecholamines, the (-)methamphetamine is the more potent CAE substance. The mechanism of the CAE effect of (-)deprenyl and (-)PPAP, a deprenyl-derived substance devoid of MAO inhibitory potency, was studied in rats by measuring: a) the release of catecholamines from striatum, substantia nigra, tuberculum olfactorium and locus coeruleus; b) the stimulation induced release of 3H-noradrenaline from the isolated brain stem; and c) the antagonistic effect against tetrabenazine-induced depression of learning in the shuttle box. The CAE effect was found to be unrelated: a) to the inhibition of MAO activity; b) to the inhibition of presynaptic catecholamine receptors; c) to the inhibition of the uptake of catecholamines; and d) to the release of catecholamines. It was concluded that (-)deprenyl and (-)PPAP act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons of the brain. We show that both (-)deprenyl and (-)PPAP enhance the inward Ca2+ current in sino-auricular fibers of the frog heart. (-)PPAP was much more potent than either (+)PPAP or (-)deprenyl hi this test.

KW - (-)deprenyl

KW - (-)methamphetamine

KW - (-)PPAP

KW - Catecholaminergic activity enhancer effect

UR - http://www.scopus.com/inward/record.url?scp=0029670154&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029670154&partnerID=8YFLogxK

U2 - 10.1016/0024-3205(96)00014-8

DO - 10.1016/0024-3205(96)00014-8

M3 - Article

VL - 58

SP - 817

EP - 827

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

IS - 10

ER -