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Submit ReviewMK 0343
Description: GABAA partial agonist; displays subtype selectivity
Chemical Name: 7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine
Purity: ≥99% (HPLC)
Biological Activity for MK 0343
MK 0343 is a subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant.
Technical Data for MK 0343
| M. Wt | 397.38 |
| Formula | C19H17F2N7O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 233275-76-8 |
| PubChem ID | 22609888 |
| InChI Key | GOIFCXRIFSYPFG-UHFFFAOYSA-N |
| Smiles | FC(C=CC=C3F)=C3C1=NN=C2N1N=C(OCC5=NC=NN5C)C(C4CCC4)=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for MK 0343
References for MK 0343
References are publications that support the biological activity of the product.
Atack et al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J.Psychopharmacol. 25 314 PMID: 20147571
de Haas et al (2008) Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype-selective agonist, compared to L.pam and placebo in healthy male volunteers. J.Psychopharmacol. 22 24 PMID: 18187530
Atack et al (2010) Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, prima J.Pharmacol.Exp.Ther. 332 17
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Keywords: MK 0343, MK 0343 supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant, GABAA, Receptors, 4415, Tocris Bioscience
Citations for MK 0343
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Currently there are no citations for MK 0343.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.