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GMC 1-116
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C18H20N4O
- MW: 308.38
Description
GMC 1-116 is a clozapine analogue and metabolite with weak 5-HT2 affinity, high human M1 muscarinic receptor affinity and reported lack of dopamine and α1-adrenoceptor affinity. The reported data include an M1 IC50 value of 27 nM.
Clozapine metabolites and analogues are valuable for identifying receptor interactions linked to atypical antipsychotic effects. GMC 1-116 is particularly useful for studying muscarinic M1 engagement independent of strong dopamine or α1-adrenoceptor binding.
Another analogue and metabolite of clozapine, with a 2-hydroxy moiety, GMC1-165 (Axon 1152), is also available.
Key Features
- Clozapine analogue and metabolite
- High human M1 receptor affinity with IC50: 27 nM
- Weak 5-HT2 affinity
- Reportedly devoid of dopamine and α1-adrenoceptor affinities
Applications
- Clozapine metabolite profiling
- Muscarinic M1 receptor pharmacology
- Atypical antipsychotic mechanism studies
- Receptor selectivity and SAR research
More Information
| Parent CAS No. | 63687-94-5 |
|---|---|
| Chemical Name | 11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-8-ol |
| SMILES | N1C2C=CC=CC=2C(N2CCN(C)CC2)=NC2C=C(O)C=CC1=2 |
| MFCD | MFCD10565934 |
| InChi | InChI=1S/C18H20N4O/c1-21-8-10-22(11-9-21)18-14-4-2-3-5-15(14)19-16-7-6-13(23)12-17(16)20-18/h2-7,12,19,23H,8-11H2,1H3 |
| InChiKey | JLYQCLIQUFEFFL-UHFFFAOYSA-N |
| CID | 135508767 |
| Short Description | Clozapine analogue |
References
- Liao, Y. et al. Synthesis and pharmacological evaluation of triflate-substituted analogues of Clozapine: Identification of a novel atypical neuroleptic. J. Med. Chem. 1997, 40, 4146-4153.
- Y. Liao et al. New sulfonyloxy piperazinyldibenzazapines as potential atypical antipsychotics: chemistry and pharmacological evaluation. J. Med. Chem. 1999,42, 2235-2244.
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