carbachol

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

SB 203186 hydrochloride is a potent 5-HT4 receptor antagonist

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor that distinguishes between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1) Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) and has an IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells.

Ro 25-1553 is a 31-amino acid analog of vasoactive intestinal peptide (VIP) that functions as an agonist for the VIP2 receptor (VPAC2 receptor). In guinea pig models, Ro 25-1553 exhibits bronchodilator effects on tracheal smooth muscle contraction induced by neural stimuli or Carbachol.

BMS-195270 is a tissue-specific inhibitor of bladder muscle tone and spontaneous contraction in rats. It can inhibit Carbachol-induced tone and inhibit calcium flux in isolated rat bladder tissue strips in an isolated bladder model.

TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%).

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

(R)-Oxybutynin (Aroxybutynin) is an orally active muscarinic receptor antagonist, which exhibits antimuscarinic, antispasmodic, and anticholinergic activity. This compound, being the (R)-isomer of Oxybutynin, competitively antagonizes Carbachol-induced contractions. It is particularly useful in researching neurogenic bladder dysfunction-related incontinence [1] [2] [3].

Pirmenol hydrochloride functions by inhibiting I_K.ACh through the blockade of muscarinic receptors, demonstrating a potent effect with an IC_50 value of 0.1 μM for the inhibition of Carbachol-induced I_K.ACh.

Proadrenomedullin N-terminal 12 peptide (PAMP-12), an endogenous fragment originating from the adrenal medulla and spanning amino acids 9-20 of human PAMP-20, plays a role in causing hypotension. It functions as an agonist for the MAS-related G protein-coupled receptor family member X2 (MRGPRX2), inhibiting forskolin-stimulated cAMP accumulation in CHO cells expressing human MRGPRX2 (EC50 = 57.2 nM) and selectively prompting calcium mobilization in these cells (EC50 = 41 nM), but not in cells expressing MRGPRX1, MRGPRX3, or MRGPRX4 at 1 µM. As an antagonist of nicotinic acetylcholine receptors (nAChRs), PAMP-12 obstructs carbachol-triggered catecholamine release and the influx of calcium and sodium (IC50s = 1.3, 0.39, and 0.87 µM, respectively) in primary bovine adrenal chromaffin cells, with no effect on histamine-induced responses (IC50s = >1 µM for all). Additionally, it decreases mean arterial blood pressure in normotensive rats at doses ranging from 10 to 50 nmol/kg.

MB327, a bipyridine nonoxime compound, enhances neuromuscular function by restoring the activity of nicotinamide acetylcholine receptors (nAChRs) against carbachol desensitization through a typical type II PAM approach. Additionally, MB327 is effective in neutralizing nerve agent poisoning [1] [2].

Xenin 8 acetate is a biologically active fragment of Xenin in the neurotensin xenopsin family. Xenin 8 acetate augments Arginine-induced insulin release (by 40%) and potentiates the glucagon responses to both Arginine (by 60%), Carbachol (by 50%).