| Hazard Information | Back Directory | [Uses]
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability. | [in vivo]
MK-8768 has a preferred administration of intramuscular (i.m.)[1].
MK-8768 (3 mg/kg, i.m., twice weekly) improves object retrieval following scopolamine impairment obviously which mains a good executive function and attention in the Rhesus monkey ORD model[1].
Pharmacokinetic Analysis[1]
| Species | Route | Dose (mg/kg) | t1/2 (h) | Clobs (mL·min/kg) | Vss_obs (mL/kg) | F (%) | | Rat | i.v. | 1 | 3.3 | 24 | 7.3 | 32 | | Dog | i.v. | 0.25 | 3.3 | 24 | 7.3 | 34 | | Monkey | i.v. | 0.5 | 1.7 | 22 | 3.2 | / |
| Animal Model: | Rhesus monkey ORD model[2] | | Dosage: | 3 mg/kg | | Administration: | Intramuscular (i.m.), 2 times weekly | | Result: | Improved object retrieval following scopolamine impairment obviously at the concentration of 0.3 mg/ml. |
| [References]
[1] Michael T. Rudd, et al. Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator. ACS Med. Chem. Lett.. 2023，14，8. DOI:10.1021/acsmedchemlett.3c00210
[2] Sean M Smith, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.Neuropharmacology, 2013 Jan;64:215-23. DOI:10.1016/j.neuropharm.2012.06.013 |
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