Differential regional and dose-related effects of asenapine on dopamine receptor subtypes
| العنوان: | Differential regional and dose-related effects of asenapine on dopamine receptor subtypes |
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| المؤلفون: | Erik H. F. Wong, Taylor Moran-Gates, Mohammed Shahid, Brian Henry, Frank I. Tarazi |
| المصدر: | Psychopharmacology. 198:103-111 |
| بيانات النشر: | Springer Science and Business Media LLC, 2008. |
| سنة النشر: | 2008 |
| مصطلحات موضوعية: | Male, medicine.medical_specialty, Caudate nucleus, Hippocampus, Dibenzocycloheptenes, Heterocyclic Compounds, 4 or More Rings, Receptors, Dopamine, Rats, Sprague-Dawley, Internal medicine, Basal ganglia, Image Processing, Computer-Assisted, medicine, Animals, Asenapine, Psychopharmacologic agent, Receptor, Brain Chemistry, Cerebral Cortex, Pharmacology, Dose-Response Relationship, Drug, Receptors, Dopamine D2, Chemistry, Receptors, Dopamine D1, Putamen, Receptors, Dopamine D4, Receptors, Dopamine D3, Rats, Neostriatum, Endocrinology, Dopamine receptor, Autoradiography, Antipsychotic Agents, medicine.drug |
| الوصف: | The novel psychopharmacologic agent, asenapine, has high affinity for a range of receptors including the dopaminergic receptors.We examined the long-term effects of multiple doses of asenapine on dopamine receptor subtypes: D(1)-like (D(1) and D(5)), D(2), D(3), and D(4).Rats were given asenapine 0.03, 0.1, or 0.3 mg/kg (subcutaneously, twice daily) or vehicle for 4 weeks. Receptor binding was determined by autoradiography from brain sections collected from the medial prefrontal cortex (mPFC), dorsolateral frontal cortex, caudate putamen (CPu), nucleus accumbens (NAc), and hippocampus (HIP).Four weeks of asenapine at 0.3 mg/kg significantly (P0.05) increased D(1)-like binding in the mPFC (by 26%), NAc (59%), and CPu (55%). Asenapine (0.1 and 0.3 mg/kg) also increased D(2) binding in mPFC (43% and 55%, respectively). All doses of asenapine dose-dependently increased D(2) binding in HIP (by 32%, 45%, and 63%, respectively). In contrast, only 0.3 mg/kg of asenapine significantly (P0.05) increased D(2) binding in the NAc (32%) and CPu (41%). Repeated treatment with 0.1 and 0.3 mg/kg of asenapine increased D(4) binding in the NAc (36% and 71%), CPu (27% and 70%), and HIP (48% and 77%). However, asenapine, at the doses tested, did not significantly alter D(3) binding in the brain regions examined in this study.These results indicate that asenapine has region-specific and dose-dependent effects on dopamine receptor subtypes in rat forebrain, which may contribute to asenapine's unique psychopharmacological properties. |
| تدمد: | 1432-2072 0033-3158 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d460182ae3377a4faa67b6d8ebae3531 https://doi.org/10.1007/s00213-008-1098-7 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....d460182ae3377a4faa67b6d8ebae3531 |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 14322072 00333158 |
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