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1412458-61-7

中文名稱 阿塞那平鹽酸鹽
英文名稱 Saphris hydrochloride
CAS 1412458-61-7
分子式 C17H17Cl2NO
分子量 322.229
MOL 文件 1412458-61-7.mol
更新日期 2024/12/03 15:40:33
1412458-61-7 結(jié)構(gòu)式 1412458-61-7 結(jié)構(gòu)式

基本信息

中文別名
阿塞那平鹽酸鹽
英文別名
Asenapine HCl
Saphris hydrochloride
Asenapine (hydrochloride)
(3AS,12BS)-5-CHLORO-2-METHYL-2,3,3A,12B-TETRAHYDRO-1H-DIBENZO[2,3:6,7]OXEPINO[4,5-C]PYRROLE HYDROCHLORIDE
(3aS,12bS)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole hydrochloride (1:1)

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 50 mg/mL (155.17 mM; Need ultrasonic)
形態(tài)粉末
顏色White to off-white
阿塞那平鹽酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/02/08HY-16567阿塞那平鹽酸鹽
Asenapine hydrochloride
1412458-61-75 mg406元
2025/02/08HY-16567阿塞那平鹽酸鹽
Asenapine hydrochloride
1412458-61-710mg650元
2025/02/08HY-16567阿塞那平鹽酸鹽
Asenapine hydrochloride
1412458-61-710mM * 1mLin DMSO715元

常見(jiàn)問(wèn)題列表

生物活性
Asenapine hydrochloride,一種抗精神病藥物,同時(shí)是 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) 和 Dopamine (D2,D3,D4) 受體的拮抗劑,對(duì) 5-HT 受體的 Ki 值分別為 0.03-4.0 nM,多巴胺受體的 Ki 值分別為 1.3,0.42,1.1 nM。
靶點(diǎn)

sPLA2

2.5 nM (Ki)

5-HT 2A Receptor

0.06 nM (Ki)

5-HT 2C Receptor

0.03 nM (Ki)

5-HT 7 Receptor

0.13 nM (Ki)

D 2 Receptor

1.3 nM (Ki)

D 3 Receptor

0.42 nM (Ki)

D 4 Receptor

1.1 nM (Ki)

體外研究

Relative to its D2 receptor affinity, Asenapine has a higher affinity for 5-HT 2C , 5-HT 2A , 5-HT 2B , 5-HT 7 , 5-HT 6 , α 2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pK B ) at 5-HT 1A (7.4), 5-HT1B (8.1), 5-HT 2A (9.0), 5-HT 2B (9.3), 5-HT 2C (9.0), 5-HT 6 (8.0), 5-HT 7 (8.5), D2 (9.1), D3 (9.1), α 2A (7.3), α 2B (8.3), α 2C (6.8) and H1 (8.4) receptors.

體內(nèi)研究

Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.

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