muscarinic m1 receptor binding

Fustin is the phytogenic flavanol component of the plant Rhus verniciflua Stokes. Fustin shows protective effects on 6-hydroxydopamine-induced neuronal cell death.

PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res

M4mAChRModulator-2 is an orally active and selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4mAChR) capable of crossing the blood-brain barrier, with an EC50 of 513 nM. It demonstrates high target selectivity, showing minimal affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2), while specifically binding to M4mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. Additionally, M4mAChRModulator-2 can reverse the hyperlocomotion induced by Dizocilpine (MK-801) in mice and is applicable for schizophrenia research.

RS 67333 hydrochloride (RO5203648) is a potent, selective partial agonist of the 5-HT4 receptor (5-HT4R) with a pKi value of 8.7 in guinea-pig striatum. It demonstrates lower binding affinities for other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1 and D2, and muscarinic M1-M3 receptors. Notably, RS 67333 hydrochloride exhibits neuroprotective properties, rendering it useful in Alzheimer's disease research.

Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).

Tiotropium Bromide hydrate (BA-679 BR hydrate) is a potent anticholinergic and bronchodilator, serving as a muscarinic receptor antagonist, specifically targeting mAChR. It is developed for treating chronic obstructive airways disease (COPD), demonstrating novel and long-lasting effects. Binding studies with [3H]tiotropium bromide in human lung reveal its high potency and equivalent affinity for M1-, M2-, and M3-receptors, making it roughly 10 times more effective than ipratropium bromide. It notably inhibits cholinergic nerve-induced contraction of both guinea-pig and human airways more potently than atropine or ipratropium bromide, albeit with a slower onset. Tiotropium bromide uniquely presents slow dissociation from M3-receptors on airway smooth muscle and rapid dissociation from M2 autoreceptors on cholinergic nerve terminals. As a quaternary ammonium derivative, it shows high affinity and special kinetic selectivity towards muscarinic receptors across M1-, M2-, and M3-subtypes, due to its slower dissociation from M1- and M3-receptors compared to M2-receptors.