muscarinic receptor

BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

Darenzepine is a muscarinic receptor inhibitor.

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

PF-03635659 is a potent and long dissociative half-life muscarinic M3 antagonist (Ki: 0.2 nM) that shows potential for the treatment of chronic obstructive pulmonary disease (COPD).

Sabcomeline HCl is an M1 receptor agonist that can be used to study Alzheimer's disease.

Tazomeline is a muscarinic M1 receptor agonist with neuroprotective activity.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

Tiquizium has effective Antimuscarinic effect, and causes significant bronchodilation in patients with chronic obstructive pulmonary disease.

Bethanechol chloride (Carbamyl-β-methylcholine chloride) is a slowly hydrolyzing muscarinic agonist with no nicotinic effects. It is used to increase smooth muscle tone in the GI tract following abdominal surgery or to treat urinary retention without obstruction. Possible side effects include hypotension, heart rate changes, and bronchial spasm.

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.

Piperidolate hydrochloride is an antimuscarinic, could restrain the abnormal activity caused by acetylcholine. inhibits intestinal cramp induced by acetylcholine (rats and dogs).

Velufenacin is an antagonist of muscarinic receptor[1].

Rapacuronium bromide is an allosteric muscarinic acetylcholine receptor (mAChR) modulator.

Xanomeline oxalate (LY246708 oxalate), a potent and selective muscarinic receptor agonist (SMRA), effectively stimulates in vivo phosphoinositide hydrolysis. It is a valuable compound for Alzheimer's disease research.

Scopolamine is a high-affinity (nanomolar level) muscarinic receptor antagonist that can reversibly inhibit 5-HT₃ receptor responses (IC₅₀ = 2.09 μM). It is commonly used to induce animal models of Alzheimer's disease or memory impairment.

Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid) is a potent anticholinergic agent and also have NMDA antagonist properties.

Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Isopropamide iodide is a long-acting anticholinergic drug used for peptic ulcers and other gastrointestinal disorders, and as a muscarinic receptor antagonist for diseases affecting cognition [including Alzheimer's disease].

Guvacoline hydrochloride (Norarecoline hydrochloride) is a muscarinic agonist.

Blarcamesine (AVex-73) is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.