ABET - CAS 119630-77-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Arecaidine But-2-ynyl Ester Tosylate (ABET) is a potent and selective agonist of M2 recceptors in the atrium versus those in the ileum.
White Solid
Arecaidine but-2-ynyl ester tosylate; N-Methyl-1'2'5'6-tetrahydropyridine-3-carboxylic acid but-2-ynyl ester tosylate
Melting Point:
>127°C (dec.)
Canonical SMILES:
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).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related mAChR Products

CAS 123548-16-3 AQ-RA 741

AQ-RA 741
(CAS: 123548-16-3)

AQ-RA 741 has been found to be a muscarinic M2 receptor antagonist and could probably be used in the development of bronchodilator anti-muscarinic agent.

CAS 590-63-6 Bethanechol Chloride

Bethanechol Chloride
(CAS: 590-63-6)

A selective muscarinic receptor stimulant, used to treat cerebral palsy.

CAS 147202-94-6 Arecaidine propargyl ester tosylate

Arecaidine propargyl ester tosylate
(CAS: 147202-94-6)

Arecaidine propargyl ester tosylate is a potent muscarinic receptor agonist. It displays some selectivity for cardiac versus ileal M2 receptors.

CAS 21093-51-6 W-84 dibromide

W-84 dibromide
(CAS: 21093-51-6)

W-84 dibromide is a potent allosteric modulator of muscarinic M2 receptors. W-84 dibromide has been shown to stabilize cholinergic antagonist-receptor complexes...

CAS 320345-99-1 Aclidinium Bromide

Aclidinium Bromide
(CAS: 320345-99-1)

Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (C...

CAS 50-34-0 Propantheline Bromide

Propantheline Bromide
(CAS: 50-34-0)

Propantheline Bromide is an antimuscarinic agent used as an antispasmodic for the treatment of ulcers.

CAS 674-38-4 Bethanechol

(CAS: 674-38-4)

Bethanechol, a synthetic ester structurally and pharmacologically related to acetylcholine, is a selective muscarinic receptor stimulant used to increase smooth...

CAS 98636-73-8 Nitrocaramiphen hydrochloride

Nitrocaramiphen hydrochloride
(CAS: 98636-73-8)

Nitrocaramiphen hydrochloride is a mAChR M1 selective muscarinic antagonist, which exhibits 71-fold selectivity for M1 over M2.

CAS 207679-81-0 (R)-5-Hydroxymethyl tolterodine

(R)-5-Hydroxymethyl tolterodine
(CAS: 207679-81-0)

5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladde...

CAS 180468-39-7 Solifenacin hydrochloride

Solifenacin hydrochloride
(CAS: 180468-39-7)

Muscarinic M3 receptor antagoinst. Used in treatment of urinary incontinence.

CAS 1135243-19-4 VU 0255035

VU 0255035
(CAS: 1135243-19-4)

VU 0255035 is a highly selective M1 muscarinic acetylcholine receptor antagonist (Ki = 14.87 nM) with 75-fold greater selectivity for the M1 orthosteric site ov...

CAS 118290-26-9 AF-DX 384

AF-DX 384
(CAS: 118290-26-9)

AF-DX 384 has been found to be a mAChR M2/M4 selective antagonist.

CAS 153504-70-2 Cevimeline hydrochloride hemihydrate

Cevimeline hydrochloride hemihydrate
(CAS: 153504-70-2)

Cevimeline is a muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and is used to treat the symptoms of dry mouth. Ce...

CAS 51-56-9 Homatropine Bromide

Homatropine Bromide
(CAS: 51-56-9)

Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 1...

CAS 514-65-8 Biperiden

(CAS: 514-65-8)

Biperiden is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker. It is used for the adjunctive treatment of all forms of Park...

CAS 124937-52-6 Tolterodine tartrate

Tolterodine tartrate
(CAS: 124937-52-6)

Tolterodine has a high affinity and specificity for muscarinic receptors in vitro and it exhibits selectivity for the urinary bladder over salivary glands in vi...

CAS 102394-31-0 AF-DX 116

AF-DX 116
(CAS: 102394-31-0)

AF-DX 116 has been found to be a selective mAChR M2 antagonist.

CAS 3717-88-2 Flavoxate hydrochloride

Flavoxate hydrochloride
(CAS: 3717-88-2)

Flavoxate is an anticholinergic with antimuscarinic effects. Its muscle relaxant properties may be due to a direct action on the smooth muscle rather than by an...

CAS 1508-65-2 Oxybutynin chloride

Oxybutynin chloride
(CAS: 1508-65-2)

Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.

CAS 54-71-7 Pilocarpine Hydrochloride

Pilocarpine Hydrochloride
(CAS: 54-71-7)

Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.

Chemical Structure

CAS 119630-77-2 ABET

Quick Inquiry

Verification code

Featured Items