84 products were found matching "K04129"!

Metixene is an antagonist of muscarinic acetylcholine receptors (mAChRs, Ki = 15 nM for the rat receptor). It also inhibits bovine acetylcholinesterase (AChE) by 43% when used at the concentration 10 µM and butyrylcholinesterase (BChE, IC50 = 1.6 µM for the horse enzyme) in cell-free assays. Metixene reduces the...

Atropine is a naturally occurring tropane alkaloid extracted from plants of the family Solanaceae including deadly nightshade (A. belladonna). It is a non-selective, competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4, and M5 (pKBs range from 8.9-9.8). Atropine increases firing of...

An anticholinergic agent.

Trospium is an antagonist of muscarinic (M) receptors (Kis = 0.50-2.3 nM for human M1-5 recombinant receptors, respectively). Formulations containing antimuscarinics, including trospium, are used to manage overactive bladder by relieving urgency, frequency, and incontinence.Formal Name:...

Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles. Xanomeline (oxalate) is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively). It has antipsychotic-like activities in rats and Cebus...

Arecoline is a natural alkaloid that is found in the betel nut of the Areca palm. It is an agonist of the muscarinic acetylcholine receptors with EC50 values of 7, 95, 11, 410, and 69 nM for M1, M2, M3, M4, and M5, respectively. Generally, arecoline causes smooth muscle contraction. Arecoline and other muscarinic...

Benztropine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 0.59 nM in rat brain membranes). It is selective for M1 receptors over the serotonin transporter (Ki = 5,150 nM), however, it also binds to the dopamine transporter and inhibits dopamine reuptake (Kis = 237 and 130 nM, respectively)....

BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR), as it dose-dependently reduces the concentration of acetylcholine required to activate the M1 receptor. The effective range for potentiation of M1 in cells by BQCA is 0.1 to 100 µM with an inflection point...

Tolterodine is an antagonist of muscarinic acetylcholine receptors (Kis = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1-5 receptors, respectively). It reduces intracellular calcium mobilization induced by carbachol (carbamoylcholine, Cay-14486) in bladder smooth muscle cells and submandibular gland cells isolated from...

Propantheline is an anticholinergic agent. It inhibits contraction of isolated guinea pig ileum induced by acetylcholine (Cay-23829) and reduces intensity of vagal-stimulated gastric contractions in rats. Propantheline (5 mg/kg, s.c.) increases gastric pH and prevents pyloric ligature-induced gastric ulcer formation...

Oxotremorine M is a non-selective muscarinic (M) acetylcholine receptor agonist that induces phosphoinositide hydrolysis in mouse ileum isolated from wild-type, M2, M3, and M2/M3 knockout mice (EC50s = 0.36, 0.52, 1.62, and 1.48 µM, respectively). It also increases M4-induced inhibition of calcium currents in...

Diphenidol is an antagonist of muscarinic acetylcholine receptors (mAChRs, Kis = 0.43, 2.8, 1.1, 0.91, and 1.28 µM in CHO cell membranes expressing M1-5 receptors, respectively). It also inhibits Kv channels in Neuro2A cells (IC50 = 28.2 µM), as well as L-type voltage-gated calcium channels in differentiated NG...