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.

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

Muscarinic M4 modulator-1 is a positive allosteric modulator of the Muscarinic M4 receptor. It activates the muscarinic M4 receptor with allosteric efficacy (EC50) values of 14 nM in CHO-K1 cells and 3 nM in HEK293 cells. Muscarinic M4 modulator-1 exhibits antipsychotic-like activity and shows potential for research in psychiatric and/or neurological disorders.

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

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

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.

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.

PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.

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

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

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

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.

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

VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).

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

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

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

VU6016235 is a structurally unique, orally available, and highly selective tricyclic M4 muscarinic acetylcholine receptor positive allosteric modulator.

Sofpironium (BBI 4000) tosylate is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). It functions by inhibiting the M3 muscarinic receptors in the exocrine glands of the application site, thereby reducing sweat production. Additionally, Sofpironium tosylate exhibits high affinity for other muscarinic subtypes M1, M2, M4, and M5.

Clozapine (HF 1854) dihydrochloride is utilized for researching psychiatric disorders. This compound exhibits high affinity for numerous neuroreceptors and acts as an effective antagonist of dopamine receptors, with a Ki value of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor, with Ki values of 9.5 nM and 4 nM, respectively. Additionally, Clozapine is a selective agonist of the muscarinic M4 receptor (EC50 = 11 nM).

M1/M4 muscarinic agonist 1 (Compound 41) is a selective muscarinic M4/M1 agonist with EC50 values of 14 nM for M4 receptors and 55 nM for M1 receptors. This compound is utilized in research related to psychiatric disorders, including schizophrenia and delusional disorders.

Compound 43, known as M1/M2/M4 muscarinic agonist 2, functions as an mAChR M1/M2/M4 agonist with respective EC50 values of 30 nM, 200 nM, and 6.2 nM.

VU6002703 (Compound 17) is a brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an EC50 of 0.6 μM for hM4. This compound is useful for researching neuropsychiatric disorders and rare genetic central nervous system conditions.