Effect of naftidrofuryl oxalate on 5-HT2 receptors in mouse brain: evaluation based on quantitative autoradiography and head-twitch response
| Autor: | Toshitaka Nabeshima, Kazuyuki Fuji, Masayuki Hiramatsu, Tsutomu Kameyama, Kiriko Niwa |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
Male
Cingulate cortex medicine.medical_specialty Ketanserin Nafronyl Hippocampus Nucleus accumbens Head-twitch response 5-Hydroxytryptophan Mice Cortex (anatomy) Internal medicine medicine Animals Tissue Distribution Brain Chemistry Pharmacology Temporal cortex Binding Sites Behavior Animal Dose-Response Relationship Drug Methysergide Chemistry musculoskeletal neural and ocular physiology musculoskeletal system Naftidrofuryl medicine.anatomical_structure Endocrinology Pargyline Receptors Serotonin Ritanserin Autoradiography medicine.drug |
| Zdroj: | European Journal of Pharmacology. 223:109-115 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(92)94828-j |
| Popis: | The effects of naftidrofuryl oxalate (LS-121) on 5-HT2 receptors in the brain were assessed in mice on the basis of quantitative autoradiography and head-twitch responses. LS-121 inhibited [3H]ketanserin (2 nM) binding in all brain areas assayed in which there were 5-HT2 receptors, such as the frontal cortex, cingulate cortex, parietal cortex, occipital cortex, temporal cortex, nucleus accumbens, caudate-putamen, olfactory tubercle and hippocampus. In the frontal cortex, which has the highest density of 5-HT2 receptors, the Ki value of LS-121 was 6.08 x 10(-8) M. The inhibitory potencies of methysergide and ritanserin for 5-HT2 receptors were about 16- and 60-fold stronger, respectively, than that of LS-121. Moreover, in behavioral studies, LS-121 (12.5-50 mg/kg i.p.) produced dose-dependent and significant inhibitory effects on head twitches induced by 5-hydroxytryptophan (5-HTP) plus pargyline, which is a 5-HT2 receptor-dependent behavior in mice. These results suggest that LS-121 inhibits 5-HTP plus pargyline-induced head twitches by blocking 5-HT2 receptors. |
| Databáze: | OpenAIRE |
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