muscarinic achr

Biperiden (Bipariden) is a muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.

(Rac)-VU 6008667 is a selective negative allosteric modulator of the muscarinic acetylcholine receptor subtype 5 (M5 NAM), with an IC50 of 1.8 μM and a pIC50 of 5.75, exhibiting high CNS penetration.

Iperoxo (Iperoxo iodide) is an agonist of Muscarinic AChR and can be used to probe activation-related conformational transitions of muscarinic receptors.

Syn-Ake acetate (Dipeptide diaminobutyroyl benzylamide) is a muscarinic acetylcholine receptor antagonist.

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.

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.

Diphenmanil methylsulfate (Diphemanil mesylate), a quaternary ammonium anticholinergic, binds muscarinic acetylcholine receptors and thus decreases secretory excretion of stomach acids, sweat, and saliva.

Flavoxate hydrochloride (DW61) , a muscarinic AChR antagonist, is used in the therapy of various urinary syndromes and as an antispasmodic.

Trihexyphenidyl hydrochloride (Benzhexol hydrochloride) is an antiparkinsonian agent of the antimuscarinic class.

Benzetimide hydrochloride (R4929) is an antagonist of muscarinic acetylcholine receptor.treatment neuroleptic-induced parkinsonism.

Gallamine triethiodide (Benzkurin), a synthetic inhibiting drug, is nondepolarizing.

L-Hyoscyamine (Daturine) 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. Hyoscyamine is a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. 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.

Oxyphencyclimine Hydrochloride (Ulcociclinina) is a synthetic tertiary amine and antimuscarinic agent with antispasmodic and antisecretory activities.

Anagyrine hydrochloride ((-)-Anagyrine hydrochloride), a quinolizidine alkaloid discovered in Lupinus albus, interacts with both muscarinic and nicotinic acetylcholine receptors, demonstrating IC50 values of 132 and 2096 µM, respectively. This compound is recognized for its potent and direct ability to desensitize nAChR without the need for metabolic activation [1] [2] [3].

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