Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.
Article Details
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Bymaster FP, Falcone JF
Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.
Eur J Pharmacol. 2000 Mar 3;390(3):245-8.
- PubMed ID
- 10708730 [ View in PubMed]
- Abstract
The binding affinity of olanzapine, clozapine and atropine for muscarinic receptor subtypes in clonal Chinese hamster ovary (CHO) cell lines was compared in intact cells in physiological media to disrupted cells in hypotonic buffer. The affinity of olanzapine and clozapine, but not atropine, for muscarinic receptor subtypes (M(1)-M(5)) was significantly reduced in intact cells in physiological medium compared to disrupted cells in hypotonic buffer. The affinity of olanzapine for muscarinic M(1) receptors was most affected with a reduction of K(i) value from 2.5 to 73 nM in intact cells. These data suggest that the affinity of olanzapine and clozapine for muscarinic receptors have been significantly overestimated.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Clozapine Muscarinic acetylcholine receptor M1 Ki (nM) 31 N/A N/A Details Clozapine Muscarinic acetylcholine receptor M2 Ki (nM) 204 N/A N/A Details Clozapine Muscarinic acetylcholine receptor M3 Ki (nM) 109 N/A N/A Details Clozapine Muscarinic acetylcholine receptor M4 Ki (nM) 27 N/A N/A Details Olanzapine Muscarinic acetylcholine receptor M1 Ki (nM) 73 N/A N/A Details Olanzapine Muscarinic acetylcholine receptor M2 Ki (nM) 96 N/A N/A Details Olanzapine Muscarinic acetylcholine receptor M3 Ki (nM) 132 N/A N/A Details Olanzapine Muscarinic acetylcholine receptor M4 Ki (nM) 32 N/A N/A Details