m5 machr

VU 0238429 (SCR-1481B1) is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5)( EC50 : 1.16 μM).

VU 0365114 is a positive allosteric modulator of mAChR M5 (EC50: 2.7 μM).

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

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

Cyclopentolate Hydrochloride is a muscarinic acetylcholine receptors antagonist with Kis of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.

PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling

VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR ( IC 50 =36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) [1] [2] .

ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).

Aclidinium bromide (LAS-W 330) is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Aclidinium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.

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].

muscarinic receptor ligand

LAS190792 (AZD8999) is a dual-action chemical compound that simultaneously acts as a strong muscarinic antagonist and β2-adrenoceptor agonist. It exhibits significant potency across a range of receptors, with pIC50 values of 8.9 for M1, 8.8 for M2, 8.8 for M3, 9.2 for M4, 8.2 for M5, 7.5 for β1, 9.1 for β2, and 5.6 for β3. Its effectiveness across these receptors makes LAS190792 a viable candidate for bronchodilator applications [1].