VU0357017 hydrochloride is a highly selective M1 agonist. VU0357017 hydrochloride acts at an allosteric site to activate the receptor. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 HCl induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 HCl enhances performance in Morris water maze and contextual fear conditioning in rats.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 24 mg/mL|
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
Digby GJ, et al. ACS Chem Neurosci. 2012 Dec 19;3(12):1025-36. PMID: 23259038.
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.
Digby GJ, et al. J Neurosci. 2012 Jun 20;32(25):8532-44. PMID: 22723693.
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.
Lebois EP, et al. ACS Chem Neurosci. 2010;1(2):104-121. PMID: 21961051.
|Related AChR/AChE Products|
|Scopolamine hydrobromide trihydrate
Scopolamine hydrobromide trihydrate is a competitive muscarinic acetylcholine receptor with an IC50 of 55.3 ± 4.3 nM.
Choline Glycerophosphate is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue.
MK-7622 is a cholinesterase inhibitor, it is also a muscarinic M1 receptor positive allosteric modulator.
Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE).
Huperzine A is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor extracted from traditional Chinese herb.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.