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.
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 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.
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been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.
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.
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been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.