CAS:85650-56-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to off-white Solid
Asenapine maleate是 5-HT和 D2 的拮抗剂。
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Asenapine maleateCAS:85650-56-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to off-white Solid
CAS | 85650-56-2 |
Chinese Name | 阿塞那平马来酸盐 |
English Name | Asenapine maleate |
Synonyms | Org 5222;马来酸阿塞那平 |
Molecular Formula | C17H16ClNO·C4H4O4 |
Molecular Weight | 401.84 |
Solubility | Soluble in DMSO |
Purity | ≥99% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 288-064-8 |
MDL | MFCD00002090 |
SMILES | CN1C[C@]2([H])C3=CC=CC=C3OC4=CC=C(Cl)C=C4[C@]2(C1)[H].O=C(O)/C=C\C(O)=O |
Target Point | 5-HT Receptor |
Passage | Neuronal Signaling;GPCR & G Protein |
Background | Asenapine maleate is a 5-HT and D2 antagonist. |
Biological Activity | Asenapine maleate是 5-HT(1A, 1B, 2A, 2B, 2C, 5A, 6, 7) 和 D2 的拮抗剂,Ki 值分别为 0.03-4.0 nM, 1.3 nM。同时也是一种抗精神病药物。[1-4] |
In Vitro | 相对于其D2受体亲和力,阿塞那平对5-HT2C,5-HT2A,5-HT2B,5-HT7,5-HT6,α2B和D3受体具有更高的亲和力,表明这些靶标在治疗剂量下更强的接合。阿塞那平在5-HT1A(7.4),5-HT1B(8.1),5-HT2A(9.0),5-HT2B(9.3),5-HT2C(9.0),5-HT6(8.0)中表现为强效拮抗剂(pKB)。),5-HT7(8.5),D2(9.1),D3(9.1),α2A(7.3),α2B(8.3),α2C(6.8)和H1(8.4)受体[2]。 |
In Vivo | 阿塞那平是一种非典型抗精神病药,目前可用于治疗精神分裂症和I型双相情感障碍。与大鼠中的其他药物相比,阿塞那平对焦虑症状的治疗效果更好[3]。阿塞那平在EPM和小鼠的防御性大理石埋藏试验中具有抗焦虑作用[4]。 |
Animal Experiment | 大鼠:马来酸阿塞那平悬浮在10%羟丙基-β-环糊精中,并以1mL/kg体重的体积给药。在Skinner盒中使用电击足单独地恐惧大鼠。在冷冻行为评估前30分钟,用阿塞那平,氯氮平,奥氮平,丁螺环酮或SB242084腹膜内(ip)注射动物[3]。小鼠:用0.1或0.3mg/kg注射阿塞那平反复治疗雄性ICR小鼠,然后在一系列与焦虑相关的行为测试中进行测试,包括开放场测试,高架十字迷宫(EPM),防御性大理石埋藏和低位吞咽测试[4]。 |
Data Literature Source | [1]. Stoner SC,et al. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. [2]. Shahid M,et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. [3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. [4]. Ene HM,et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91. |
Unit | Bottle |
Specification | 10mg 50mg 100mg |
Asenapine maleate是 5-HT和 D2 的拮抗剂。