Olanzapine-d8

CAS: 1093380-13-2 F: C17H12D8N4S W: 320.48

Olanzapine-d8 is a deuterated labeled Olanzapine. Olanzapine (LY170053) is a selective, orally active monoaminergic anta

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Bioactivity	Olanzapine-d8 is a deuterated labeled Olanzapine[1]. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic[2][3].
Invitro	氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。Olanzapine 弱结合 GABAA、苯二氮卓 (BZD) 和 β-肾上腺素能受体 (Ki>10 μM)[2][3]。 Olanzapine 诱导人SH-SY5Y神经细胞系自噬[4]。 Olanzapine (1-100 μM，血清饥饿 144 小时) 对胶质母细胞瘤细胞系和胶质瘤干细胞样细胞具有显著的抗增殖作用[5]。 Olanzapine 还增强 Temozolomide (HY-17364) 对胶质母细胞瘤细胞系的抗肿瘤活性[5]。 Olanzapine 诱导胶质母细胞瘤细胞系的凋亡和坏死[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Olanzapine-d8 相关抗体:
In Vivo	Olanzapine (0.75、1.5 和 3 mg/kg) 评估小鼠的体重和宫周脂肪量，以及胰岛素、非酯化脂肪酸、甘油三酯和葡萄糖水平[6]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	1093380-13-2
Formula	C17H12D8N4S
Molar Mass	320.48
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Vucicevic L, et al. Autophagy inhibition uncovers the neurotoxic action of the antipsychotic drug olanzapine. Autophagy. 2014;10(12):2362-78. [3]. APPROVED AGREED-UPON LABELING. [4]. Karpel-Massler G, et al. Olanzapine inhibits proliferation, migration and anchorage-independent growth in human glioblastoma cell lines and enhances temozolomide's antiproliferative effect. J Neurooncol. 2015 Mar;122(1):21-33. [5]. Olanzapine for Injection, powder, for solution for intramuscular use. [6]. Coccurello R, et al. Chronic administration of olanzapine induces metabolic and food intake alterations: a mousemodel of the atypical antipsychotic-associated adverse effects. Psychopharmacology (Berl). 2006 Jul;186(4):561-71.