m5 machr

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

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

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.

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

Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

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.

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).

AE9C90CB is an antagonist of the muscarinic receptor (muscarinic receptor) with greater affinity for M3 muscarinic receptors (M3 muscarinic receptors), exhibiting a pKi of 9.90. Its selectivity for M3 receptors is 20 times higher than for M2 muscarinic receptors.

muscarinic receptor ligand

ML381 (VU0488130) is a highly selective, central nervous system-penetrant mAChR M5 orthogonal antagonist with nanomolar potency that exhibits instability in rat plasma, limiting its in vivo utility while establishing its primary value as a molecular probe for in vitro pharmacological characterization and electrophysiological studies of M5 receptor function.

Lu AE51090 is a highly selective agonist of the muscarinic M1 receptor, displaying minimal off-target activity across other muscarinic subtypes and a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, making Lu AE51090 a valuable pharmacological tool for studying muscarinic receptor function and selective receptor modulation.

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] .

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].

mAChR antagonist 1 (Compound 4a), an mAChR antagonist, exhibited Ki values of 255 nM, 121 nM, 158 nM and 255 nM for the M1, M3, M4 and M5 subtypes, respectively.

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.

M3mAChRagonist 1 is a dual positive allosteric modulator (PAM) that primarily targets the M3 subtype of M3/M5 mAChRs. It demonstrates high subtype selectivity over other mAChR subtypes, including M1, M2, and M4. By modulating the M3 muscarinic acetylcholine receptor, M3mAChRagonist 1 enhances the signaling pathway, leading to increased contraction of isolated rat bladder strips.

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

(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.

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