ABET - CAS 119630-77-2
Category: Inhibitor
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Molecular Formula:
C18H23NO5S
Molecular Weight:
365.444
COA:
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Targets:
mAChR
Description:
Arecaidine But-2-ynyl Ester Tosylate (ABET) is a potent and selective agonist of M2 recceptors in the atrium versus those in the ileum.
Appearance:
White Solid
Synonyms:
Arecaidine but-2-ynyl ester tosylate; N-Methyl-1'2'5'6-tetrahydropyridine-3-carboxylic acid but-2-ynyl ester tosylate
MSDS:
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Melting Point:
>127°C (dec.)
InChIKey:
GKPXMGUNTQSFGA-UHFFFAOYSA-N
InChI:
InChI=1S/C11H15NO2.C7H8O3S/c1-3-4-8-14-11(13)10-6-5-7-12(2)9-10;1-6-2-4-7(5-3-6)11(8'9)10/h6H'5'7-9H2'1-2H3;2-5H'1H3'(H'8'9'10)
Canonical SMILES:
CC#CCOC(=O)C1=CCCN(C1)C.CC1=CC=C(C=C1)S(=O)(=O)O
1.Maturation of stretch-induced contractile activity and its muscarinic regulation in isolated whole bladder strips from rat.
Gevaert T;Owsianik G;Hutchings G;Everaerts W;Nilius B;De Ridder D Neurourol Urodyn. 2010 Jun;29(5):789-96. doi: 10.1002/nau.20553.
AIM: ;Besides the establishment of neural reflex pathways, developmental changes in local bladder properties probably also contribute to the onset of mature voiding reflexes. Here we explored the behavior of stretch-induced contractile activity (SIC) and its muscarinic regulation in neonatal and adult rat bladders.;METHODS: ;SIC was studied in bladder strips from D0, D7, D28 rat pups and adult rats (15 weeks). The responses to a non-selective [Carbachol (CA), 10(-8.5)-10(-6) M] and an M(2)-selective muscarinic agonist [arecaidine but-2-ynyl ester tosylate (ABET), 10(-9.5)-10(-7) M] were studied. The expression of M(2) and M(3) mRNA was investigated using quantitative PCR in whole bladders. The response of SIC to KCl (50 mM) and to the non-adrenergic non-cholinergic (NANC) drugs Substance P (1 microM) and alpha,beta-Methyleneadenosine 5'-triphosphate lithium salt (MATP) (1 microM) were also studied.;RESULTS: ;We found evidence for an enhanced response to the muscarinic agonists CA and ABET in neonatal bladders. This might be due to the onset of a direct contractile role for M(2), given the moderate M(2)-properties of ABET and the absence of ABET-effects on adult bladder strips. Further data showed an increased expression of both M(2) and M(3) at the mRNA level and a changed response of SIC to NANC drugs in neonatal bladder.
2.Muscarinic M1 acetylcholine receptors regulate the non-quantal release of acetylcholine in the rat neuromuscular junction via NO-dependent mechanism.
Malomouzh AI;Mukhtarov MR;Nikolsky EE;Vyskočil F J Neurochem. 2007 Sep;102(6):2110-2117. doi: 10.1111/j.1471-4159.2007.04696.x. Epub 2007 Jun 11.
Nitric oxide (NO), previously demonstrated to participate in the regulation of the resting membrane potential in skeletal muscles via muscarinic receptors, also regulates non-quantal acetylcholine (ACh) secretion from rat motor nerve endings. Non-quantal ACh release was estimated by the amplitude of endplate hyperpolarization (H-effect) following a blockade of skeletal muscle post-synaptic nicotinic receptors by (+)-tubocurarine. The muscarinic agonists oxotremorine and muscarine lowered the H-effect and the M1 antagonist pirenzepine prevented this effect occurring at all. Another muscarinic agonist arecaidine but-2-ynyl ester tosylate (ABET), which is more selective for M2 receptors than for M1 receptors and 1,1-dimethyl-4-diphenylacetoxypiperidinium (DAMP), a specific antagonist of M3 cholinergic receptors had no significant effect on the H-effect. The oxotremorine-induced decrease in the H-effect was calcium and calmodulin-dependent. The decrease was negated when either NO synthase was inhibited by N(G)-nitro-L-arginine methyl ester or soluble guanylyl cyclase was inhibited by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one. The target of muscle-derived NO is apparently nerve terminal guanylyl cyclase, because exogenous hemoglobin, acting as an NO scavenger, prevented the oxotremorine-induced drop in the H-effect.
3.Electrophysiological characterization of cardiac muscarinic acetylcholine receptors: different subtypes mediate different potassium currents.
Shi H;Yang B;Xu D;Wang H;Wang Z Cell Physiol Biochem. 2003;13(2):59-74.
To characterize electrophysiologically the K+ currents mediated by various mAChR subtypes, we performed detailed whole-cell patch-clamp studies in canine atrial myocytes. I(KACh) was induced by 1 mM ACh (acetylcholine) or by arecaidine but-2-ynyl ester tosylate (100 nM, an M2 receptor selective agonist) and was blocked by methoctramine (20 nM, an M2 receptor selective antagonist). Tetramethylammonium (0.5 mM) activated a K+ conductance with delayed rectifying properties (I(KM3)) and the currents were highly sensitive to 4-diphenylacetoxy-N-methylpiperidine methiodide (2 nM, an M3 receptor inhibitor). 4-aminopyridine (1 mM) induced a delayed rectifier-like current (I(K4AP)) which was selectively suppressed by tropicamide (200 nM, an M4 receptor blocker). The current waveforms, I-V relationships, steady-state voltage-dependence, kinetics and pharmacological properties of these three currents were different from one another and distinct from the classical delayed rectifier K+ currents (I(Kr) and I(Ks)). Both I(KACh) and I(K4AP) were sensitive to pertussis ntoxin, whereas I(KM3) was not. Isoproterenol (1 mM) markedly depressed I(KM3), but increased I(K4AP) and did not alter I(KACh). The effects of isoproterenol were reversed by propranolol (1 mM); and ACh completely suppressed I(KM3) and I(K4AP).
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CAS 119630-77-2 ABET

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