MK-6884

Names

[ Name ]:
MK-6884

Biological Activity

[Description]:

MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

[Target]

M4 muscarinic receptor[1]

[In Vitro]

MK-6884 (compound 13; 0-22 µM) is a PAM of ACh function in a cell-based Ca2+ mobilization assay, with an EC50 of 27 nM[1].

[In Vivo]

[11C]MK-6884 (compound 13) shows non-displaceable binding potential (BPND) of 0.83 in rhesus monkeys[1]. [11C]MK-6884 (approximately 185 MBq, <2 μg; single intravenous) distributes on the known presence of M4 receptors in the rhesus monkeys brain[1]. [11C]MK-688 can penetrate the blood-brain barrier in monkeys[1].

[References]

[1]. Tong L, et al. Discovery of [¹¹C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases. J Med Chem. 2020;63(5):2411-2425.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₅N₅O

[ Molecular Weight ]:
411.50

MK-6884

Names

Biological Activity

Chemical & Physical Properties

Related Compounds