machr

M4 mAChR agonist-1 (4-Piperidinecarboxamide, 1-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-) is an effective agonist of M4 mAChR (EC50 >10 μM).

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.

YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

Oxybutynin (Ditropan) is a synthetic anticholinergic agent that is used for treatment of urinary incontinence and overactive bladder syndrome.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Pilocarpine nitrate (Pilagan) is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

Ipratropium bromide monohydrate (Ipratropium bromide hydrate) is a muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

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.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

mAChR-IN-1 hydrochloride is a potent antagonist of muscarinic cholinergic receptors (mAChR) with an IC50 of 17 nM.

mAChR-IN-1 is muscarinic cholinergic receptor(mAChR) antagonist (IC50=17 nM).

M4 mAChR Modulator-1 (compound 23i) acts as a positive allosteric modulator (PAM) of the M4 mAChR. It demonstrates a stronger synergistic effect in β-arrestin recruitment compared to G protein activation when interacting with ACh. Additionally, while its PAM effects are weaker in G protein-mediated responses, they are more potent in β-arrestin recruitment.

Fustin is the phytogenic flavanol component of the plant Rhus verniciflua Stokes. Fustin shows protective effects on 6-hydroxydopamine-induced neuronal cell death.

Compound 4a, a mAChR antagonist, exhibits K i values of 255 nM for M1 and M5 subtypes, and lower values of 121 nM and 158 nM for M3 and M4 subtypes, respectively [1].

Xanomeline tartrate (LY 246708 tartrate) is an M1 and M4 mAChR agonist with antipsychotic-like activity that improves cognition and can be used in studies of schizophrenia and Alzheimer's disease.

Cyclodrine (Cyclopent) is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.

CDD0102 HCl is a selective and potent M1 muscarinic receptor agonist for the treatment of Alzheimer's disease.