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METHYLAPLYSINOPSIN: A NATURAL PRODUCT OF MARINE ORIGIN WITH EFFECTS ON SEROTONERGIC NEUROTRANSMISSION
Author(s) -
BairdLambert J.,
Davis P.A.,
Taylor K.M.
Publication year - 1982
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.1982.tb00798.x
Subject(s) - serotonergic , neurotransmission , natural product , natural (archaeology) , neuroscience , chemistry , serotonin , biology , biochemistry , paleontology , receptor
SUMMARY 1. Methylaplysinopsin is an indolyl‐methylene derivative of creatinine which was isolated from a sponge collected on the Great Barrier Reef. 2. It is a potent inhibitor of tetrabenazine‐induced responses in rats and mice and appears to act through several mechanisms, each of which enhances central serotonergic function. 3.As a reversible inhibitor of type A monoamine oxidase (MAO) methylaplysinopsin is relatively short‐acting and has a K i of 0.2 μmol/l when serotonin is the substrate used. 4.Methylaplysinopsin (10 ‐4 mol/1) also releases [ 3 H]‐serotonin from prelabelled synaptosomes, but has little effect on release of [ 3 H]‐noradrenaline ([ 3 H]‐NA) from a similar preparation. 5. In blocking uptake of [ 3 H]‐serotonin into cerebral cortical synaptosomes, methylaplysinopsin has a potency similar to that of imipramine ( K i =2 × 10 ‐7 mol/1 cf. 5 × 10 ‐7 mol/1), but it is considerably less potent in blocking [ 3 H]‐NA uptake. 6. Methylaplysinopsin is a weak displacer of [ 3 H]‐serotonin specific binding (IC 50 = 160 μmol/l for hippocampal membrane preparations and 66 μmol/1 for crude homogenates of rat brain). 7.Thus, methylaplysinopsin has effects on various aspects of serotonergic function. Whilst some of these effects are weak, they appear relatively selective for this neurochemical system.