85 products were found matching "K04129"!

ML-137 is a positive allosteric modulator (PAM) of M1 muscarinic acetylcholine receptors (mAChRs). It is selective for M1 over M2-M5 mAChRs at 30 µM. ML-137 potentiates ACh-induced activation of the M1 muscarinic receptor (EC50 = 0.83 µM).Formal Name:...

Propiverine N-oxide is an active metabolite of the muscarinic acetylcholine receptor antagonist propiverine (Cay-36049). In vivo, propiverine N-oxide (0.422 mg/kg) reduces sacral anterior root stimulation-induced bladder contractions and salivary flow in mini pigs.Formal Name:...

Organism: Homo sapiens (Human). Source: E.coli. Expression Region: 210-366aa. Protein Length: Partial. Tag Info: N-terminal 10xHis-tagged. Target Protein Sequence: RIYRETENRA RELAALQGSE TPGKGGGSSS SSERSQPGAE GSPETPPGRC CRCCRAPRLL QAYSWKEEEE EDEGSMESLT SSEGEEPGSE VVIKMPMVDP EAQAPTKQPP RSSPNTVKRP TKKGRDRAGK GQKPRGKEQL...

Organism: Rattus norvegicus (Rat). Source: E.coli. Expression Region: 210-366aa. Protein Length: Cytoplasmic Domain. Tag Info: N-terminal 6xHis-tagged. Target Protein Sequence: RIYRETENRA RELAALQGSE TPGKGGGSSS SSERSQPGAE GSPESPPGRC CRCCRAPRLL QAYSWKEEEE EDEGSMESLT SSEGEEPGSE VVIKMPMVDS EAQAPTKQPP KSSPNTVKRP...

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...