m2 receptor

Pimethixene maleate (Pimetixene maleate) is a potent 5-HT2B receptor antagonist with sedative and antitussive activity.Pimethixene maleate inhibits 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2, and can be used in studies of dry and irritant cough in children. irritant cough in children.

Oxybutynin chloride (Oxybutynin HCl) is an anticholinergic medication used to relieve urinary and bladder difficulties. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

Solifenacin (YM905 free base) (YM905 free base) is a novel muscarinic receptor antagonist, its pKis for M1, M2 and M3 receptors is of 7.6, 6.9 and 8.0, respectively.

PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.

VU0238441 is agonist of Muscarinic acetylcholine receptor M5 (human) with EC50 of 2.1μM.

Regorafénib N-oxyde M2 is an active metabolite of Regorafenib, a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13/4.2/46, 1.5, 22, 7, and 2.5 nM).

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Solifenacin D5 hydrochloride is a deuterium-labeled Solifenacin hydrochloride, which acts as an antagonist of muscarinic receptors with pKis of 7.6, 6.9, and 8.0 for M1, M2, and M3 receptors, respectively.

Terodiline hydrochloride is an antagonist of M1-selective muscarinic receptor (mAChR)(Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively).

Otenzepad (AF-DX 116) is a selective M2 mAChR antagonist with IC50 values of 386 nM in rat heart and 640 nM in rabbit peripheral lung.

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

Tarafenacin is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

AE9C90CB is an antagonist of the muscarinic receptor (muscarinic receptor) with greater affinity for M3 muscarinic receptors (M3 muscarinic receptors), exhibiting a pKi of 9.90. Its selectivity for M3 receptors is 20 times higher than for M2 muscarinic receptors.

Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with notable antimuscarinic activity. As a selective antagonist of the muscarinic M1 receptor, Oxomemazine demonstrates a 20-fold difference in affinity at high (histamine H1-receptor=84 nM, M1 receptor) and low (histamine H1-receptor=1.65 μM, M2 receptor) affinity sites. It serves as an antihistamine and anticholinergic agent used in cough-related research studies.

SCH 211803 is a selective antagonist of the M2 muscarinic receptor. It shows potential for research in cardiovascular and neurological diseases.

VU0467319 (Compound VU319) is a highly selective positive allosteric modulator of the M1 receptor, capable of crossing the blood-brain barrier and orally active, with an EC50 of 492 nM. It demonstrates selectivity in humans and rats (EC50 > 30 μM) compared to M2-5 receptors. This compound improves cognitive deficits associated with Alzheimer's disease (AD) through central M1 muscarinic receptor activation and does not induce cholinergic adverse effects, highlighting its potential in AD research.

AF-DX 384 free base is a selective and efficient M2 muscarinic acetylcholine receptor (M2 mAChR) and M4 muscarinic acetylcholine receptor (M4 mAChR) antagonist. It can be used for research on neurodegenerative diseases like Parkinson's.

Oxotremorine sesquifumarate is a muscarinic agonist.

(S)-(+)-Dimethindene maleate is an orally available, selective muscarinic M2 receptor and histamine H1 receptor antagonist that also inhibits muscarinic M1, M3, and M4 receptors.

W-84 dibromide (HDMPPA) is a M2-receptor selective modulator.