ganglionic

Pempidine (1,2,2,6,6-Pentamethylpiperidine) is a nicotinic antagonist and has been used as a ganglionic blocker for treating hypertension.

Gastrin-Releasing Peptide, human(TFA) is a regulatory human peptide that elicits gastrin release and regulates gastric acid secretion and enteric motor function. The post-ganglionic fibers of the vagus nerve that innervate the G cells of the stomach release GRP, which stimulates the G cells to release gastrin.

SM-2470 is an α1-adrenoceptor antagonist with antihypertensive activity that decreases anterior ganglionic adrenal nerve activity and aortic descending nerve activity.SM-2470 has hypocholesterolemic activity and inhibits cholesterol absorption.

Hexamethonium Free Base is a nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

13-Hydroxylupanine, a characteristic alkaloid of sweet lupins, inhibits ganglionic transmission, reduces cardiac contractility, and induces contraction of uterine smooth muscle [1].

Pentolinium Tartrate (Pendine) is a nicotinic antagonist that has been used as a ganglionic blocking agent in hypertension.

Arpenal HCl is a ganglionic blocking agent which may be useful in the treatment of bronchial asthma.

Guanethidine sulphate, synthesized in 1959, is thought to lowing blood pressure by interfering with the metabolism of chemical transmitter substances in post-ganglionic sympathetic nerve fibres.

Mecamylamine hydrochloride (Mevasin) is a nicotinic antagonist, used as a ganglionic blocker in hypertension.

Gardneramine has a mild central depressive effect. Gardneramine and hirsutine show a local anesthetic action, they also can inhibit the ganglionic transmission of the dog urinary bladder and that the blockade of the nicotinic receptor plays a main role.

TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration of 50 μM and inhibiting calcium influx and efflux in isolated guinea pig ileum when used at a concentration of 65 μM. It has been used in the study of intracellular calcium dynamics, particularly in smooth muscle. TMB 8 also inhibits protein kinase C (PKC) activity in a dose-dependent manner.

Arpenal is a ganglionic blocking agent which may be useful in the treatment of bronchial asthma.

Mecamylamine, an orally active, nonselective, noncompetitive antagonist of nAChR (nicotinic acetylcholine receptors), exhibits ganglionic blockade capabilities and can cross the blood-brain barrier. Its applications span research areas including neuropsychiatric disorders, hypertension, and antidepressant efficacy.

Gastrin-Releasing Peptide, human is a regulatory human peptide that elicits gastrin release and regulates gastric acid secretion and enteric motor function. The post-ganglionic fibers of the vagus nerve that innervate the G cells of the stomach release GRP, which stimulates the G cells to release gastrin.

Hexamethonium tartrate is a nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.

Chlorisondamine chloride is a nicotinic antagonist used primarily as a ganglionic blocker in animal research. It has been used as an antihypertensive agent but has been supplanted by more specific drugs in most clinical applications.

Pempidine tartrate is a nicotinic antagonist most commonly used as an experimental tool. It has been used as a ganglionic blocker in the treatment of hypertension but has largely been supplanted for that purpose by more specific drugs.

Pempidine HCl is a nicotinic antagonist most commonly used as an experimental tool. It has been used as a ganglionic blocker in the treatment of hypertension but has largely been supplanted for that purpose by more specific drugs.

Trimethaphan camsylate is a nicotinic antagonist that has been used as a ganglionic blocker in hypertension.