Olanzapine Inhibitor CAS No. 132539-06-1

Cat. No.	Name	Size	Price	Add Cart
KI0787	Olanzapine	100 mg	$252

Chemical Characteristic

Product Name	Olanzapine
Synonyms	Zyprexa, Zydis, Relprevv
CAS No.	132539-06-1
Molecular Weight	312.43
Formula	C₁₇H₂₀N₄S
Chemical Name	2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine
Smiles	N1c2c(C(=Nc3c1cccc3)N1CCN(CC1)C)cc(s2)C
Chemical Structure

Biological activities

Olanzapine is an antagonist of 5-HT2A and dopamine D2 receptors with Ki values of 4 and 11 nM, respectively.^[1] In Chinese hamster ovary (CHO) cells stably expressing 5-HT2 receptors, olanzapine is devoid of agonism but is an antagonist at all three subtypes 5-HT2A, 5-HT2B and 5-HT2C with IC50 value of 2.5, 47 and 69 nM, respectively. In human embryonic kidney (HEK) cells transiently expressing 5-HT2C receptor isoforms, while lacking agonist activity at the VNI isoform and VSV isoform, olanzapine shows inverse agonism at the INI isoform with an IC50 value of 594 nM, reaching a maximal attenuation of 20%. In addition, olanzapine is a full antagonist at all three isoforms, with a rank order of potency of VNI (IC50, 79 nM)>VSV (IC50, 101 nM)>INI (IC50, 3856 nM).^[2] In vivo, olanzapine (1.25-10 mg/kg, p.o.) antagonizes apomorphine-induced climbing behavior in mice. Olanzapine (2.5-10 mg/kg, p.o.) also antagonizes oxotremorine-induced tremor in mice. In a conditioned avoidance paradigm in rats, olanzapine inhibits the avoidance response with an ED50 of 4.7 mg/kg p.o. In another series of experiments, olanzapine (1.25 mg/kg, i.p.) produces clozapine-appropriate responding in a drug discrimination model in which animals have been trained to discriminate clozapine (5 mg/kg, i.p.) from vehicle.^[3]

References

[1] Huang XF, et al. Olanzapine differentially affects 5-HT2Aand2C receptor mRNA expression in the rat brain. Behav Brain Res. 2006,171(2): 355-362. [2] Zhang JY, et al. Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms. Biochem Pharmacol. 2006, 71(4): 521-529. [3] Moore NA, et al. The behavioral pharmacology of olanzapine, a novel "atypical" antipsychotic agent. J Pharmacol Exp Ther. 1992, 262(2): 545-551.

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