Olanzapine-d8 is intended for use as an internal standard for the quantification of olanzapine by GC- or LC-MS. Olanzapine is an atypical antipsychotic that binds to dopamine D1, D2, and D4 receptors (Kis = 31, 11, and 27 nM, respectively) as well as the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2C, and 5-HT3 (Kis = 4, 11, and 57 nM, respectively). It also binds to M1 muscarinic acetylcholine, α1-adrenergic, and histamine H1 receptors (Kis = 2, 19, and 7 nM, respectively).[1] Olanzapine (0.5 mg/kg, i.p.) decreases immobility time in the forced swim test in non-stressed and prenatally-stressed rats, indicating antidepressant-like activity. [2]It also decreases the number of avoidances made in the conditioned avoidance response test in rats when administered at doses of 0.5 and 1 mg/kg. [3] Formulations containing olanzapine have been used in the treatment of schizophrenia and bipolar disorder.
Reference:
[1]. Bymaster, F.P., Calligaro, D.O., Falcone, J.F., et al. Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology 14(2), 87-96 (1996).
[2]. Nowakowska, E., Kus, K., Ratajczak, P., et al. The influence of aripiprazole, olanzapine and enriched environment on depressant-like behavior, spatial memory dysfunction and hippocampal level of BDNF in prenatally stressed rats. Pharmacol. Rep. 66(3), 404-411 (2014).
[3]. Ashby, D.M., Lapish, C.C., and Phillips, A.G. Stability of avoidance behaviour following repeated intermittent treatment with clozapine, olanzapine or D,L-govadine. Behav. Pharmacol. 26(1-2), 133-138 (2015).