[11C]olanzapine, radiosynthesis and lipophilicity of a new potential PET 5-HT2 and D2 receptor radioligand.

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Gao M, Shi Z, Wang M, Zheng QH

[11C]olanzapine, radiosynthesis and lipophilicity of a new potential PET 5-HT2 and D2 receptor radioligand.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):1953-6. doi: 10.1016/j.bmcl.2013.02.045. Epub 2013 Feb 14.

PubMed ID

23466228 [ View in PubMed

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Abstract

Olanzapine and its precursor desmethyl-Olanzapine were synthesized from malononitrile, propionaldehyde, 1-fluoro-2-nitrobenzene, and substituted piperazine in 4, 4, 5, and 5 steps with 35%, 32%, 26%, and 32% overall chemical yield, respectively. [(11)C]Olanzapine was prepared from desmethyl-Olanzapine with [(11)C]CH3OTf through N-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 40-50% radiochemical yield based on [(11)C]CO2 and decay corrected to end of bombardment (EOB), with 370-740 GBq/mumol specific activity at EOB. The calculated LogP (CLogP) value of [(11)C]Olanzapine is 3.39.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Olanzapine	5-hydroxytryptamine receptor 2A	Ki (nM)	4	N/A	N/A	Details
Olanzapine	5-hydroxytryptamine receptor 2A	IC 50 (nM)	7	N/A	N/A	Details
Olanzapine	5-hydroxytryptamine receptor 2C	Ki (nM)	11	N/A	N/A	Details
Olanzapine	5-hydroxytryptamine receptor 2C	IC 50 (nM)	71	N/A	N/A	Details
Olanzapine	Dopamine D2 receptor	IC 50 (nM)	10	N/A	N/A	Details
Olanzapine	Dopamine D2 receptor	Ki (nM)	11	N/A	N/A	Details