Cat.No. | Name | Information |
---|---|---|
M3470 | Oxybutynin | Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. |
M3190 | PNU-282987 | PNU-282987 is a highly selective α7 nAChR agonist with Ki of 27 nM. |
M29233 | VU6000918 | VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4. |
M29105 | VU6004256 | VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia. |
M28777 | ML352 | ML352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively. |
M28716 | ML380 | ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR. |
M28713 | ML381 | ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies. |
M28633 | Ubretid | Ubretid is a potent inhibitor of plasma cholinesterase. Ubretid therefore delays the hydrolysis of suxamethonium and prolongs its action, similar to the effects shown by other anticholinesterase agents, such as pyridostigmine and donepezil. Ubretid has the potential for the research of urinary retention prolongs the effect of suxamethonium. Ubretid is commonly prescribed for the research of myasthenia gravis and for difficulty in emptying the bladder. |
M28597 | Rivanicline | Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). |
M28529 | ML375 | ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4. |
M28479 | VU0467485 | VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity. |
M28478 | VU0467154 | VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively. |
M28424 | VU0453595 | VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia. |
M28421 | (S)-UFR2709 | (S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction. |
M28130 | Piperidolate hydrochloride | Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs). |
M28038 | Pitofenone hydrochloride | Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively. |
M27992 | Itopride | Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD). |
M27864 | Tarafenacin D-tartrate | Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. |
M27841 | PQCA | PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease. |
M27657 | Lupanine hydrochloride | Lupanine (D-Lupanine) hydrochloride is a natural ketonic derivative of Sparteine ((+)-Sparteine) with a ganglioplegic activity. Lupanine hydrochloride shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM. |
M27607 | CHF5407 | CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity. |
M22086 | Cevimeline hydrochloride | Cevimeline hydrochloride is a quinidine derivative of acetylcholine and a selective, orally active agonist of muscarinic acetylcholine receptors M1 and M3, with a spirocyclic moiety in its structure, which crosses the blood-brain barrier. |
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