Résumé
To investigate the disposition and tissue distribution of ML12 after intravenous (iv) ad- ministration in rats, the compound in plasma or in tissue was extracted into ethyl acetate under basic condition and was determined by HPLC after extracted by dilute sulfuric acid. Excitation wavelength and emission wavelength of fluorescence detection were 278 nm and 307 nm, respectively. The data were processed with the software 3P97 to calculate the main pharmaceutical parameters of ML12, At dose of 5 and 10 mg/kg, the elimination of the drug from plasma was found to be kinetically linear, but when the dosage was 20 mg/kg, a non-linear feature was observed. The highest level of MLI2 was found in the kidney. Distribution of MLI2 after iv administration was extensive and the concentration-time profile was found to he fitted to an open two-compartment model.
Résumé
<p><b>AIM</b>To investigate the effect of 5-hydroxytryptamine (5-HT) on spontaneous unit discharges of primary somatosensory cortex (SI-SUD) and the role of 5-HT1A receptor in 5-HT inhibitory effect on SI-SUD in rat.</p><p><b>METHODS</b>The SI-SUD was recorded before and during microiontophoresis of 5-HT and 8-OH-DPAT (the selective agonist for 5-HT1A receptor. The changes of mean of interspike interval (MISI) of SI-SUD were analysed and handled with the statistics.</p><p><b>RESULTS</b>(1) Effects of 5-HT on SI-SUD may be inhibitory (48/96), excitatory (26/96) or non-responsive (22/96), and the major effect is inhibitory. (2) In 20 of 5-HT inhibited units, 17 are also inhibited with microiontophoresis of 8-OH-DPAT, but 3 have no obvious response to 8-OH-DPAT.</p><p><b>CONCLUSION</b>The major effect of 5-HT on SI-SUD is inhibitory. In majority of 5-HT inhibited units, 5-HT1A receptor may be existence, which may involve in the inhibition of 5-HT on SI-SUD.</p>