mAChR3 Modulator

Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.

Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC₅₀: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia.

ASP8302 is a positive and allosteric muscarinic M3 receptor modulator. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder.

VU0119498 is a pan G_q mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC₅₀s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity.

Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC₅₀: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia.

PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (K_i values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.

Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with K_i of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats.