Literature DB >> 7160439

Serotonin modulates the dissociation of [3H]imipramine from human platelet recognition sites.

L P Wennogle, L R Meyerson.   

Abstract

The dissociation of [3H]imipramine from human platelet membrane recognition sites was studied. Simple exponential dissociation kinetics were observed indicating an apparent homogeneous class of sites which dissociate by a first order rate process. Inclusion of serotonin in the medium dramatically decreased the dissociation rate. At 0 degree C half-times of dissociation were 61.7 and 170 min in the absence and presence of serotonin, respectively. Other biogenic amines were ineffective in altering the dissociation kinetics. It is suggested that serotonin controls [3H]imipramine dissociation from an allosterically coupled site residing on a larger macromolecular complex.

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Year:  1982        PMID: 7160439     DOI: 10.1016/0014-2999(82)90333-8

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  23 in total

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Review 2.  Studies on the serotonin transporter in platelets.

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Review 5.  Escitalopram, an antidepressant with an allosteric effect at the serotonin transporter--a review of current understanding of its mechanism of action.

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6.  Location of the antidepressant binding site in the serotonin transporter: importance of Ser-438 in recognition of citalopram and tricyclic antidepressants.

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Review 8.  Tryptamine: a metabolite of tryptophan implicated in various neuropsychiatric disorders.

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Journal:  Metab Brain Dis       Date:  1993-03       Impact factor: 3.584

9.  Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites.

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10.  Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter.

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