caa a22 4500 46912167X CHVBK 20180323133140.0 cr unu---uuuuu 170328e19920201xx s 000 0 eng 10.1007/BF02246225 doi (NATIONALLICENCE)springer-10.1007/BF02246225 Biochemistry and pharmacology of moclobemide, a prototype RIMA [Elektronische Daten] [W. Haefely, W. Burkard, A. Cesura, R. Kettler, H. Lorez, J. Martin, J. Richards, R. Scherschlicht, M. Da Prada] RIMA is a term for reversible inhibitors of monoamine oxidase (MAO) with preference for MAO-A; moclobemide is a prototype of this new class of antidepressants and is a highly selective inhibitor of MAO-A in vitro. This inhibition is reversible by dialysis in vitro, which accounts for the dose-dependent duration of in vivo enzyme inhibition of 12-24 h. Moclobemide increases the content of serotonin, noradrenaline and dopamine in the brain, and decreases that of their deaminated metabolites. Its biochemical, neurological and behavioural effects indicate that it increases the extracellular concentration of the classic monoamine neurotransmitters/neuromodulators — in particular 5-HT. Potentiation of the cardiovascular effects of tyramine is less pronounced after taking moclobemide than after irreversible MAO-A inhibitors. Understanding of the physiological role of MAO and of the events that link inhibition of the enzyme with modulation of neuronal activities in the CNS remains incomplete. A major physiological role of intraneuronal MAO is to keep cytosolic amine concentration very low, to enable the neuronal monoamine carriers to produce a net inward transport of monoamines, and thereby to act as the first step in the termination of action of extracellular monoamines. MAO is likely to have a similar function in non-monoaminergic cells with respect to the monoamine carriers they contain. In addition to the classic monoamines, "trace” amines may become functionally active after MAO inhibition. An alternative role for MAO is that of a scavenger, preventing natural substrates from accumulating in monoaminergic neurons and interacting with storage, release, uptake and receptor function of monoamines. Springer-Verlag, 1992 MAO-A inhibitor nationallicence Moclobemide nationallicence Antidepressant biochemistry nationallicence Pharmacology nationallicence Monoamines nationallicence Haefely W. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Burkard W. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Cesura A. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Kettler R. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Lorez H. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Martin J. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Richards J. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Scherschlicht R. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Da Prada M. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut Psychopharmacology Springer-Verlag 106(1992-02-01), S6-S14 0033-3158 106<S6 1992 106 213 https://doi.org/10.1007/BF02246225 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02246225 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Haefely W. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Burkard W. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Cesura A. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Kettler R. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Lorez H. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Martin J. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Richards J. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Scherschlicht R. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Da Prada M. Pharmaceutical Research Department CNS, F. Hoffmann-La Roche Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 106(1992-02-01), S6-S14 0033-3158 106<S6 1992 106 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer