862310-66-5
Chemical Structure
MK-3134
- CAS No.: 862310-66-5
- Formula:C25H26F3N3O2
- Molecular Weight:457.49
InChIKey: ZWUFGBNOUKQGBR-UHFFFAOYSA-N
SMILES: O=C1C2=C(C=CC=C2C(F)(F)F)N=C(C)N1C3=CC=C(C=C3)OC4CCN(C5CCC5)CC4
Biological Activity: MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease[1][2][3][4].
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MK-3134 | MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Cho W, et al. Additive effects of a cholinesterase inhibitor and a histamine inverse agonist on scopolamine deficits in humans. Psychopharmacology (Berl). 2011;218(3):513-524. [Content Brief]
- [2]. Van Laere KJ, et al. (11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists. J Nucl Med. 2014 Jan;55(1):65-72. [Content Brief]
- [3]. Jończyk J, et al. Search for multifunctional agents against Alzheimer's disease among non-imidazole histamine H3 receptor ligands. In vitro and in vivo pharmacological evaluation and computational studies of piperazine derivatives. Bioorg Chem. 2019;90:103084. [Content Brief]
- [4]. Łażewska D, et al. Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. Bioorg Med Chem Lett. 2016;26(16):4140-4145. [Content Brief]
Keywords
