M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4[1].
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM[1].
Camylofin is an antimuscarinic, is a smooth muscle relaxant
Oxitropium bromide is an mAChR antagonist used as an anticholinergic bronchodilator drug for the treatment of asthma and chronic obstructive pulmonary disease.
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Methscopolamine (Pamine) is a muscarinic acetylcholine receptor blocker. Target: mAChRMethylscopolamine is an oral medication used along with other medications to treat peptic ulcers by reducing stomach acid secretion. With the advent of proton pump inhibitors and antihistamine medications it is rarely used for this. It can also be used for stomach or intestinal spasms, to reduce salivation, and to treat motion sickness. From Wikipedia.Methscopolamine (Pamine), an anti-acetylcholine drug, prevented ulcer formation, reduced further volume and acid output but produced a 3-4 fold increase in hexosamine concentration. Tissue (corpus and antrum) hexosamine was moderately reduced by restraint. In the corpus, this was counteracted by methscopolamine but antrum hexosamine was not influenced by this drug. The anti-ulcer property of methscopolamine may be due not only to its effect on acid secretion but also to the rise in gastric mucus concentration that it produced [1].
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i[1].
Ethybenztropine (Ponalid) is a muscarinic receptor blocker. Ethybenztropine is an anticholinergic and antihistaminergic agent[1].
ML375 (VU-0483253) is a potent, highly selective M5 NAM with submicromolar potency (human M5 IC50=300 nM, rat M5 IC50=790 nM, M1-M4 IC50> 30 uM), exhibts excellent multispecies PK, high CNS penetration, and enantiospecific inhibition.
Olanzapine(LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.IC50 Value:Target: 5-HT ReceptorOlanzapine is a thienobenzodiazepine that blocks especially the serontonin (5-hydroxytryptamine [5-HT]) 5-HT2A and the dopamine D2 receptors (Ki values are 4 and 11 nM respectively) as well as muscarinic (M1), histamine (H1), 5-HT2C, 5-HT3 to 5-HT6, adrenergic (α(l)), and D4 receptors. Atypical antipsychotic for the treatment of schizophrenia. Olanzapine displays anticholinergic properties.
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.
Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders.
Octamylamine is an anticholinergic and antispasmodic agent[1].
Bethanechol Chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.Target: mAChRBethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Unlike acetylcholine, bethanechol is not hydrolyzed by cholinesterase and will therefore have a long duration of action. Oral bethanechol significantly improves contraction pressures and bolus transit in the smooth muscle portion of the esophagus in patients with severe IEM [1]. Bethanechol has potential benefit in the treatment of cerebral palsy [2].
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
Metixene hydrochloride hydrate is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM[1].
BQCA a highly selective allosteric modulator of the M1 mAChR.
Clozapine (HF 1854) is an antipsychotic used to treat schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for M1 receptor.
Muscarine ((+)-Muscarine) chloride is a toxin that can stimulate the parasympathetic nervous system. Muscarine is a prototype muscarinic acetylcholine receptor agonist[1][2].
L-Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine.Target: mAChRHyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care [1].
Peimisine (Ebeiensine) hydrochloride non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine hydrochloride excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma[1].
DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility[1].
LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect[1][2].
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
MK-7622 is a muscarinic M1 receptor positive allosteric modulator.Target: M1 receptorMK-7622 is useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders.
(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence[1].