کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2012709 | 1541846 | 2015 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Atypical antipsychotic properties of AD-6048, a primary metabolite of blonanserin
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کلمات کلیدی
EPSACSdlSTBlonanserin - blonanserindorsolateral striatum - striatum dorsolateralAtypical antipsychotic - آنتی سایکوتی غیرطبیعیapo - آپوApomorphine - آپومرفینSchizophrenia - اسکیزوفرنی یا شیزوفرنیMED - باMinimum effective dose - حداقل دوز موثرextrapyramidal side effects - عوارض جانبی ExtrapyramidalHaloperidol - هالوپریدولHal - چیز
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Atypical antipsychotic properties of AD-6048, a primary metabolite of blonanserin Atypical antipsychotic properties of AD-6048, a primary metabolite of blonanserin](/preview/png/2012709.png)
چکیده انگلیسی
Blonanserin is a new atypical antipsychotic drug that shows high affinities to dopamine D2 and 5-HT2 receptors; however, the mechanisms underlying its atypicality are not fully understood. In this study, we evaluated the antipsychotic properties of AD-6048, a primary metabolite of blonanserin, to determine if it contributes to the atypicality of blonanserin. Subcutaneous administration of AD-6048 (0.3-1Â mg/kg) significantly inhibited apomorphine (APO)-induced climbing behavior with an ED50 value of 0.200Â mg/kg, the potency being 1/3-1/5 times that of haloperidol (HAL). AD-6048 did not cause extrapyramidal side effects (EPS) even at high doses (up to 10Â mg/kg, s.c.), whereas HAL at doses of 0.1-3Â mg/kg (s.c.) significantly induced bradykinesia and catalepsy in a dose-dependent manner. Thus, the therapeutic index (potency ratios of anti-APO action to that of EPS induction) of AD-6048 was much higher than that of haloperidol, illustrating that AD-6048 per se possesses atypical antipsychotic properties. In addition, immunohistochemical analysis of Fos protein expression revealed that both AD-6048 and HAL significantly increased Fos expression in the shell part of the nucleus accumbens and the striatum. However, in contrast to HAL which preferentially enhanced striatal Fos expression, AD-6048 showed a preferential action to the nucleus accumbens. These results indicate that AD-6048 acts as an atypical antipsychotic, which seems to at least partly contribute to the atypicality of blonanserin.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacology Biochemistry and Behavior - Volume 138, November 2015, Pages 14-19
Journal: Pharmacology Biochemistry and Behavior - Volume 138, November 2015, Pages 14-19
نویسندگان
Ayaka Tatara, Saki Shimizu, Atsushi Masui, Miyuki Tamura, Shoko Minamimoto, Yuto Mizuguchi, Midori Ochiai, Yusuke Mizobe, Yukihiro Ohno,