\n1,1-Dimethyl-4-phenylpiperazinium iodide\n

Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels comprising five subunits. The muscle-type receptor is made of two (A)1 (B), (G) and (D) subunits, while the neuronal nicotinic receptors are formed by different combination of 2 (A) and 3 (B) subunits. These receptors are expressed on neuronal and different types of non-neuronal cells like: lymphocytes, alveolar macrophages, airway smooth muscle cells, epithelial cells, and fibroblasts.\n\nnAChRs mediate numerous specific physiological functions depending on the type of cell involved. For example, nicotine induces the release of dopamine in the central nervous system and stimulates nitric oxide (NO) synthase gene expression in endothelial cells.\n\n1,1-Dimethyl-4-phenylpiperazinium iodide (DMPP) is a selective nAChR agonist. For a long time, DMPP was considered to be the prototype of ganglionic stimulating agents, since it was able to activate the nicotinic receptor in sympathetic ganglia with higher potency than the muscle-type. However, it has since been shown that DMPP binds with higher affinity to the nicotinic receptor in the brain. 1,1-Dimethyl-4-phenylpiperazinium iodide activates had IC₅₀ of 0.77 uM on (A)4 nicotinic channel expressed in xenopus oocytes.\n\nNicotinic agonists, such as DMPP, have anti-inflammatory effects in mouse models of hypersensitivity pneumonitis, asthma, airway inflammation, and Type I diabetes. DMPP reduces the release of IL-1 and TNF from isolated spleen cells, and the release of TNF and IL-6 from macrophages.

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