Clidinium bromide is an anticholinergic (specifically a muscarinic antagonist) drug, may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines.
Pilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Atropine sulfate is a competitive muscarinic acetylcholine receptor antagonist.IC50 value:Target: mAChRAtropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. Atropine is a competitive antagonist of the muscarinic acetylcholine receptors (acetylcholine being the main neurotransmitter used by the parasympathetic nervous system). Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions [1].
Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.
M1/M2/M4 muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 3.2 nM, 32 nM and 1.7 nM, respectively[1].
Desmethylclozapine-d8 (Norclozapine-d8) hydrochloride is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.Target: PDE4; mACHRIrsogladine treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3% (P < 0.02, P < 0.001), in tPA-deficient mice by 42.6 and 46% (P < 0.001, P < 0.001), and in uPA-deficient mice by 27.2 and 46% (P < 0.05, p < 0.001), respectively. Irsogladine inhibits bFGF-induced angiogenesis in wild-type, tPA-knockout, and uPA-knockout mice [1]. Irsogladine up-regulates GJIC between PC cells via regulation of the PKA pathway. It also suggests a useful adjuvant of Irsogladine to pancreatic cancer therapy [2]. irsogladine produces the increase of intracellular cAMP content via non-selective inhibition of PDE isozymes, which may be a key mechanism involved in its gastroprotective actions [3].
VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity[1].
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.IC50 value: 0.19 nM (Ki) [1]Target: M3 muscarinic receptorin vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [2].in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].
Cimetropium Bromide is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (Ki: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers[1][2][3].
Choline (bitartrate) is an essential nutrient, often associated with the B vitamins but not yet officially defined as a B vitamin[1]. Choline (bitartrate) plays an important role in synthesis of the neurotransmitter acetylcholine[2].
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively)[1]. AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine[2].
Temiverine hydrochloride is a synthesized drug that is expected to have anticholinergic action.
(R)-VU 6008667, an active enantiomer of VU6008667, is a orally active acetylcholine receptor subtype 5 (M5 NAM) inhibitor with IC50 values of 1.2 μM (human) and 1.6 μM (rat), respectively. (R)-VU6008667 is selective for M5 over M1-4, high CNS penetration[1].
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.IC50 value: 0.19 nM (Ki) [1]Target: M3 muscarinic receptorin vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [2].in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].
Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR[1][2].
Tolterodine Tartrate(PNU-200583E; Kabi-2234) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. IC50 Value:Target: mAChRin vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors [1].in vivo: Tolterodine was extensively metabolized in vivo [2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased [3].
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo[1][2][3].
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.IC50 value:Target: M3 receptor
(R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities[1].
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR[1][2][3].
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively[1].
Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.
Clozapine-d4 (HF 1854-d4) is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
Solifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist.IC50 value:Target: muscarinic receptorSolifenacin succinate (YM905; Vesicare) is a prescription medication used to treat certain bladder problems.