AI Article Synopsis
- Ipsapirone, a potential non-benzodiazepine anxiety medication, is metabolized in rats to a compound called 1-(2-pyrimidinyl)piperazine (1-PP), which builds up in the brain.
- The methods of administration (injection or oral) and long-term use of either ipsapirone or 1-PP did not change the amount of 1-PP in the brain.
- Chronic treatment with either substance did not alter liver enzyme activity related to drug metabolism, suggesting that 1-PP may enhance the drug's effects on certain brain receptors without affecting how it is processed in the body.
Article Abstract
Ipsapirone, a putative non-benzodiazepine anxiolytic, was extensively metabolized in rats to 1-(2-pyrimidinyl)piperazine (1-PP) which accumulated in the brain. Neither the route of administration (i.p. or p.o.), nor prolonged administration of ipsapirone or 1-PP affected their accumulation in the rat brain. The cytochrome P450 level and ethylmorphine N-demethylase activity in rat liver microsomes were unchanged by chronic treatment with ipsapirone or 1-PP. The results indicate that 1-PP may contribute to the alpha 2-adrenoceptor antagonism of ipsapirone in rats and that chronic treatment with the drug does not affect its biotransformation to 1-PP.
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| http://dx.doi.org/10.1111/j.2042-7158.1990.tb06623.x | DOI Listing |
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