43 products were found matching "K04132"!

Recombinant CHO-K1 cells stably overexpress human cholinergic receptor muscarinic 4 (M4) on the surface and contain high levels of G protein Galphai to couple with the receptor in downstream signaling pathways.

An M4 muscarinic receptor PAM, selective for M4 mAChRs over a panel of 59 receptors, ion channels, transporters, and enzymes at 10 µM, selectively potentiates ACh-induced activation of the M4 mAChR over M1-M3 and M5 mAChRs in cells expressing the human receptors (EC50s = 12.3, 4,798, >10,000, >10,000, and >10,000...

Methylatropine is an antagonist of muscarinic acetylcholine receptors (IC50 = 12008). It reduces acetylcholine-induced decreases in blood pressure in rats when administered intravenously with an ED50 value of 5.5 µg/kg. Methylatropine reduces salivation, induces mydriasis, and increases heart rate in dogs.Formal...

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:...

An antispasmodic agent.

Aclidinium is an antagonist of muscarinic acetylcholine receptors (mAChRs, Kis = 0.1, 0.14, 0.14, 0.21, and 0.16 for the M1-M5 receptors, respectively). It induces relaxation of precontracted isolated human bronchi when used at a concentration of 0.1 µM. Aclidinium reduces bronchoconstriction induced by ACh...

McNA343 is a partial agonist of muscarinic acetylcholine receptors (Kis = 5, 1, 5, 0.2, and 7.6 µM for M1-5 receptors, respectively, in radioligand binding assays). It induces contraction of isolated human umbilical veins (EC50 = 1.23 µM), an effect that can be reversed by various M1 muscarinic receptor selective...

Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors. It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Cay-15592) in isolated...

Oxybutynin is an antagonist of muscarinic acetylcholine receptors (Kis = 5, 14.5, 3.7, 5.3, and 40 nM for human recombinant M1-5, respectively). It inhibits intracellular calcium mobilization induced by carbamoylcholine (carbachol, Cay-14486) in bladder smooth muscle and submandibular gland cells isolated from...

Cyclopentolate is an antagonist of muscarinic acetylcholine receptors (Kis = 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively). It inhibits carbachol-induced contraction of isolated human iris sphincter, circular ciliary muscle, and longitudinal ciliary muscle (Kbs = 7.9, 15.8, and 12.5 nM,...

Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles. Five subtypes (M1-5) have been identified, which preferentially couple to various effector systems based on their G protein interaction.Tropicamide is a muscarinic acetylcholine receptor (mAChR) antagonist (pKi = 7.2 in...

Atropine is a naturally occurring tropane alkaloid isolated from plants in the Solanaceae family. Atropine is an anticholinergic compound that also exhibits analgesic and antinociceptive activities. Atropine is a competitive inhibitor of muscarinic acetylcholine receptors (mAChRs) that is commonly used for...