AI Article Synopsis
- - Buspirone, MJ-13805, and MJ-13653 were tested in rats and did not cause '5-HT syndrome' even at high doses (up to 20 mg kg-1) and are weak serotonin uptake blockers.
- - These drugs do not inhibit monoamine oxidase types A or B, indicating a different mechanism compared to stronger antidepressants like chlorimipramine.
- - Buspirone did show effects in controlling certain behaviors, such as blocking stereotypy induced by apomorphine and delaying effects from other serotonin-related compounds.
Article Abstract
Buspirone, MJ-13805 and MJ-13653 did not produce a '5-hydroxytryptamine (5-HT) syndrome' in rats at doses up to 20 mg kg-1. These drugs were very weak 5-HT uptake blockers (IC50 much greater than 10 microM) compared to drugs such as chlorimipramine. These drugs did not inhibit either monoamine oxidase (MAO)-A or MAO-B. The Ki values for these agents as inhibitors of [3H]-5-HT and [3H]-ketanserin binding to rat frontal cortex or hippocampal membranes were in the microM range, well above the brain concentrations achieved after an oral dose of 25 mg kg-1. Parenterally administered buspirone blocked apomorphine-induced stereotypy, inhibited the 5-HT syndrome elicited by 5-methoxy-N,N-dimethyltryptamine, and delayed the onset of p-chloroamphetamine induced behaviours.
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Source |
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1916732 | PMC |
| http://dx.doi.org/10.1111/j.1476-5381.1985.tb08940.x | DOI Listing |
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