oxotremorine

Oxotremorine acts as an agonist of mAChR, specifically activating the M1 and M3 acetylcholine receptors. In drug discrimination experiments with macaques, it exhibits effects similar to nicotine.

Oxotremorine sesquifumarate is a muscarinic agonist.

Oxotremorine M iodide (Oxotremorine methiodide) is an agonist of mAChR and potentiates NMDA receptors.

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]

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] .