1432729-22-0

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)	t_1/2 (h)	Cl_obs (mL·min/kg)	V_{ss_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

Hazard Information

Uses

in vivo

References

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