muscarinic-m4

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.

Compound 40 is a selective M1 M4 muscarinic antagonist with an IC50 of 19 nM for M1 receptors and 42 nM for M4 receptors [1].

Compound 42, also known as M1 M2 M4 muscarinic agonist 1, is a muscarinic M4 M1 M2 agonist exhibiting EC50 values of 6.5, 26, and 210 nM for M4, M1, and M2 respectively. This compound is utilized in research focused on mental disorders, including schizophrenia and delusion [1].

Muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1 M2 M4 agonist with EC50 values of 3.2 nM, 32 nM, and 1.7 nM, respectively [1].

Compound 44, identified as an M1 M4 muscarinic agonist, exhibits potent activity with EC50 values of 31 nM at M1 and 9.3 nM at M4 mAChRs, respectively [1].

(Rac)-Sabcomeline ((Rac)-SB-202026) is an M1 M4 muscarinic agonist used in the study of neurologic disorders such as schizophrenia.

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.

Diphenidol hydrochloride (Difenidol hydrochloride), a muscarinic antagonist, is employed as an anti-vertigo and as an antiemetic drug.

Tropicamide (Ro 1-7683) is a synthetic muscarinic antagonist with anticholinergic properties similar to atropine. Upon ocular administration, it binds to and blocks muscarinic receptors in the sphincter and ciliary muscles, inhibiting cholinergic responses and causing pupil dilation and ciliary muscle paralysis. Tropicamide is used as a diagnostic agent to induce short-duration mydriasis and cycloplegia.

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

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

VU0152099 is a potent and selective M4 mAChR allosteric potentiator(EC50 = 380 ± 93 nM).

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (M4 mAChR).

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs with ED50 values of 38 and 81 nmol/kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M.[3]

Emraclidine (CVL-231) is a novel, highly selective allosteric modulator of the muscarinic M4 receptor positive receptor for the study of neurological diseases.

VU6005806 is a potent positive allosteric modulator (PAM) of muscarinic acetylcholine receptor subtype 4 (M4) (EC50s: 94 nM, 28 nM, 87 nM, and 68 nM for human, rat, dog, and cyno M4, respectively), and used in the study of neuropsychiatric disorders.

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.

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

VU0467485 is a potent and selective muscarinic acetylcholine receptor 4 positive allosteric modulator. VU0467485 potentiates the activity of ACh at M4 (EC50s: 26.6 nM and 78.8 nM at the rat and human M4 receptors, respectively). VU0467485 displays selecti

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).

Muscarinic toxin 3 (MT3), a potent non-competitive antagonist of mAChR and adrenoceptors, exhibits pIC50 values of 6.71 for M1, 8.79 for M4, 8.86 for α1A, 7.57 for α1B, 8.13 for α1D, 8.49 for α2A, <6.5 for α2B, and 7.29 for α2C receptors. MT3 notably demonstrates significant adrenoceptor activity [1].

Direclidine is a positive allosteric modulator of the muscarinic M4 receptor (muscarinic M4 receptor).

Thiochrome is a selective enhancer of M4 muscarinic receptor of acetylcholine (ACh) affinity.