dimethylphenylpiperazinium iodide


Summary: A selective nicotinic cholinergic agonist used as a research tool. DMPP activates nicotinic receptors in autonomic ganglia but has little effect at the neuromuscular junction.

Top Publications

  1. Park T, Seo H, Kang B, Kim K. Noncompetitive inhibition by camphor of nicotinic acetylcholine receptors. Biochem Pharmacol. 2001;61:787-93 pubmed
    ..Ca2+]i increases induced by high K+, veratridine, and bradykinin were not affected by camphor. The data suggest that camphor specifically inhibits catecholamine secretion by blocking nAChRs without affecting agonist binding. ..
  2. Roe D, Craviso G, Waymire J. Nicotinic stimulation modulates tyrosine hydroxylase mRNA half-life and protein binding to the 3'UTR in a manner that requires transcription. Brain Res Mol Brain Res. 2004;120:91-102 pubmed
    ..Thus, nicotinic stimulation produces a transcription-dependent increase in TH mRNA half-life that is mediated by previously unrecognized TH mRNA binding proteins. ..
  3. Jimenez Gonzalez A, Ros Moreno R, Moreno Guzmán M, Rodriguez Caabeiro F. Characterization of levamisole binding sites in Trichinella spiralis. Parasitol Res. 1998;84:757-9 pubmed
    ..76 microM and a receptor density (Bmax) of 2.14 pmol/mg of protein. In inhibition studies, only dimethylphenylpiperazinium iodide (DMPP) and hexamethonium were found to be competitive inhibitors of the [3H]LEV binding with an ..
  4. Briggs C, McKenna D, Monteggia L, Touma E, Roch J, Arneric S, et al. Gain of function mutation of the alpha7 nicotinic receptor: distinct pharmacology of the human alpha7V274T variant. Eur J Pharmacol. 1999;366:301-8 pubmed
    ..These results support and extend the concept that human nicotinic receptor pharmacology can be profoundly altered by single amino acid changes in the pore-lining segment. ..
  5. Kim O, Lim G, Lim D. Influence of naloxone on catecholamine release evoked by nicotinic receptor stimulation in the isolated rat adrenal gland. Arch Pharm Res. 2005;28:699-708 pubmed
  6. Ruaud A, Bessereau J. The P-type ATPase CATP-1 is a novel regulator of C. elegans developmental timing that acts independently of its predicted pump function. Development. 2007;134:867-79 pubmed
    ..These results obtained in vivo provide further evidence for the recently proposed pump-independent scaffolding functions of P-type ATPases in the modulation of intracellular signaling. ..
  7. Park Y, Ha Choi Y, Park C, Kim K. Nongenomic glucocorticoid effects on activity-dependent potentiation of catecholamine release in chromaffin cells. Endocrinology. 2008;149:4921-7 pubmed publisher
    ..Altogether, we suggest that glucocorticoids inhibit ADP of catecholamine release by decreasing myristoylated alanine-rich C kinase substrate phosphorylation, which inhibits F-actin disassembly and vesicle translocation. ..
  8. Hao M, Boesmans W, Van den Abbeel V, Jennings E, Bornstein J, Young H, et al. Early emergence of neural activity in the developing mouse enteric nervous system. J Neurosci. 2011;31:15352-61 pubmed publisher
    ..Along with the spinal cord and hindbrain, the ENS appears to be one of the earliest parts of the nervous system to exhibit electrical activity. ..
  9. Cirillo C, Tack J, Vanden Berghe P. Nerve activity recordings in routine human intestinal biopsies. Gut. 2013;62:227-35 pubmed publisher
    ..This novel approach is of key importance to study living neurons in both health and disease and to test newly developed compounds in an in-vitro human tissue model. ..

More Information


  1. Douglas H, Kitchen I. Non-opioid effects of N-methyl levallorphan in the anaesthetised rat. Gen Pharmacol. 1990;21:67-70 pubmed
    ..3. The narrow selectivity of N-methyl levallorphan makes this compound inappropriate for opioid antagonist studies where nicotinic receptors may be involved. ..
  2. Villarroya M, Lopez M, Cano Abad M, Garcia A. Measurement of Ca2+ entry using 45Ca2+. Methods Mol Biol. 2006;312:135-45 pubmed
  3. Rehn M, Hübschle T, Diener M. TNF-alpha hyperpolarizes membrane potential and potentiates the response to nicotinic receptor stimulation in cultured rat myenteric neurones. Acta Physiol Scand. 2004;181:13-22 pubmed
  4. Lim D, Kim I. Arecoline inhibits catecholamine release from perfused rat adrenal gland. Acta Pharmacol Sin. 2006;27:71-9 pubmed
    ..There seems to be a difference in the mode of action of nicotine and arecoline in rat adrenomedullary CA secretion. ..
  5. Cahill A, Perlman R. Phorbol esters cause preferential secretion of norepinephrine from bovine chromaffin cells. J Neurochem. 1992;58:768-71 pubmed
    ..These results suggest that protein kinase C plays a specific role in the regulation of catecholamine secretion from norepinephrine-containing cells. ..
  6. Scholze P, Orr Urtreger A, Changeux J, McIntosh J, Huck S. Catecholamine outflow from mouse and rat brain slice preparations evoked by nicotinic acetylcholine receptor activation and electrical field stimulation. Br J Pharmacol. 2007;151:414-22 pubmed
    ..The impact of nAChRs in catecholaminergic projection areas differs between species and has thus to be considered when extrapolating results from animal models to human conditions. ..
  7. Ruaud A, Bessereau J. Activation of nicotinic receptors uncouples a developmental timer from the molting timer in C. elegans. Development. 2006;133:2211-22 pubmed
    ..elegans. Activation of DMPP-sensitive nAChRs during the second larval stage uncouples a molting timer and a developmental timer, thus causing a heterochronic phenotype that is lethal at the subsequent molt. ..
  8. Ruaud A, Katic I, Bessereau J. Insulin/Insulin-like growth factor signaling controls non-Dauer developmental speed in the nematode Caenorhabditis elegans. Genetics. 2011;187:337-43 pubmed publisher
    ..Our studies provide further evidence for broad conservation of insulin/insulin-like growth factor (IGF) functions in developmental speed control. ..
  9. Fu X, Nurse C, Farragher S, Cutz E. Expression of functional nicotinic acetylcholine receptors in neuroepithelial bodies of neonatal hamster lung. Am J Physiol Lung Cell Mol Physiol. 2003;285:L1203-12 pubmed
  10. Moura E, Afonso J, Hein L, Vieira Coelho M. Alpha2-adrenoceptor subtypes involved in the regulation of catecholamine release from the adrenal medulla of mice. Br J Pharmacol. 2006;149:1049-58 pubmed
    ..This study was carried out to elucidate which alpha(2)-adrenoceptor subtypes mediated the inhibition of noradrenaline and adrenaline release from the adrenal medulla of mice...
  11. Anderson D, Puttfarcken P, Jacobs I, Faltynek C. Assessment of nicotinic acetylcholine receptor-mediated release of [(3)H]-norepinephrine from rat brain slices using a new 96-well format assay. Neuropharmacology. 2000;39:2663-72 pubmed
    ..In contrast, DHbetaE antagonism of [(3)H]-dopamine release from striatal slices using a similar methodology was competitive. ..
  12. Puttfarcken P, Jacobs I, Faltynek C. Characterization of nicotinic acetylcholine receptor-mediated [(3)H]-dopamine release from rat cortex and striatum. Neuropharmacology. 2000;39:2673-80 pubmed
    ..In addition, the data suggest that the subtypes of nAChRs involved in regulating [(3)H]-DA release may be somewhat different in the two tissues. ..
  13. Bazzani C, Bertolini A, Ricigliano G, Cainazzo M, Balugani A, Guarini S. The reversal of experimental hemorrhagic shock induced by nicotine and dimethylphenylpiperazinium is adrenal-dependent. Resuscitation. 1996;31:145-50 pubmed
    ..It is concluded that stimulation of adrenaline release plays a fundamental role in the mechanism of action of nicotine- and DMPP-induced shock reversal. ..
  14. Finnegan J, Borges R, Wightman R. Comparison of cytosolic Ca2+ and exocytosis responses from single rat and bovine chromaffin cells. Neuroscience. 1996;71:833-43 pubmed
    ..This can be advantageous to minimize biological variability which occurs with organs obtained from slaughter houses and enables the investigation of genetically-altered animals. ..
  15. Woo K, Park Y, Jun D, Lim J, Baek W, Suh B, et al. Phytoestrogen cimicifugoside-mediated inhibition of catecholamine secretion by blocking nicotinic acetylcholine receptor in bovine adrenal chromaffin cells. J Pharmacol Exp Ther. 2004;309:641-9 pubmed
    ..The results suggest that cimicifugoside selectively inhibits nAChR-mediated response in bovine chromaffin cells. ..
  16. Sotirov E, Papasova M. Nitric oxide modulates release of noradrenaline in guinea-pig gastric fundus. Brain Res Bull. 2000;51:401-5 pubmed
    ..The data suggests that endogenous NO increases the release of [(3)H]NA, evoked either by activation of the nicotinic receptors or by electrical stimulation in guinea-pig gastric fundus...
  17. Egea J, Hernandez Guijo J, Olivares R, Lopez M, Garcia A. Desensitized nicotinic receptors that, however, afford cytoprotection in bovine chromaffin cells. J Mol Neurosci. 2006;30:59-60 pubmed
    ..We have also investigated cytoprotection elicited by DMPP and EPB against the cytotoxic effects of veratridine in bovine chromaffin cells. ..
  18. Hong S. Inhibition of autonomic nerve-mediated inotropic responses in guinea pig atrium by bafilomycin A. Synapse. 2002;45:200-5 pubmed
    ..Furthermore, bafilomycin A preferentially inhibited neurotransmitter release emanating from the immediately releasable pool. ..
  19. Craviso G, Poss J, Lanctot C, Lundback S, Chatterjee I, Publicover N. Intracellular calcium activity in isolated bovine adrenal chromaffin cells in the presence and absence of 60 Hz magnetic fields. Bioelectromagnetics. 2002;23:557-67 pubmed
    ..On the other hand, plasma membrane nicotinic receptors may be affected in a manner that is important for ligand-receptor interactions. ..
  20. Klinge E, Alaranta S, Sjostrand N. Pharmacological analysis of nicotinic relaxation of bovine retractor penis muscle. J Pharmacol Exp Ther. 1988;245:280-6 pubmed
    ..Moreover, nicotinic activation of these nerves of the bovine retractor penis muscle can be used as a model for further characterization of mammalian erectile nerves. ..
  21. Chern Y, Bott M, Chu P, Lin Y, Kao L, Westhead E. The adenosine analogue N6-L-phenylisopropyladenosine inhibits catecholamine secretion from bovine adrenal medulla cells by inhibiting calcium influx. J Neurochem. 1992;59:1399-404 pubmed
    ..These data suggest that inhibition by PIA occurs at the level of the voltage-sensitive calcium channel. ..
  22. Ito S, Ohta T, Kasai Y, Yonekubo K, Nakazato Y. Heterogeneity of neuronal nicotinic acetylcholine receptors in 5-HT-containing chemoreceptor cells of the chicken aorta. Br J Pharmacol. 2001;132:1934-40 pubmed
    ..It is suggested that neuronal nicotinic ACh receptors, sensitive and insensitive to alpha - BTX, are present on the chemoreceptor cells of the chicken aorta, the activation of which causes the release of 5-HT. ..
  23. Tan H, Collewijn H. Muscarinic nature of cholinergic receptors in the cerebellar flocculus involved in the enhancement of the rabbit's optokinetic response. Brain Res. 1992;591:337-40 pubmed
    ..We conclude that muscarinic receptors are involved in the positive modulatory action of the cholinergic system in the cerebellar flocculus...
  24. Ma Z, Strecker R, McKenna J, Thakkar M, McCarley R, Tao R. Effects on serotonin of (-)nicotine and dimethylphenylpiperazinium in the dorsal raphe and nucleus accumbens of freely behaving rats. Neuroscience. 2005;135:949-58 pubmed
    ..In conclusion, there are different mechanisms involved in nicotine- and DMPP-evoked increases in 5-HT. This is consistent with prior work suggesting DMPP may primarily act on 5-HT carriers. ..
  25. Bradaia A, Trouslard J. Nicotinic receptors regulate the release of glycine onto lamina X neurones of the rat spinal cord. Neuropharmacology. 2002;43:1044-54 pubmed
    ..These data demonstrate that neurones surrounding the central canal of the spinal cord present a glycinergic synaptic transmission which is modulated by terminal nAChRs. ..
  26. Böhmer G, Schmid K, Schmidt P, Stehle J. Cholinergic effects on spike-density and burst-duration of medullary respiration-related neurones in the rabbit: an iontophoretic study. Neuropharmacology. 1987;26:1561-72 pubmed
    ..The functional significance of cholinergic effects on respiration-related neurones is discussed with special emphasis of effects on burst duration...
  27. Fonteriz R, Garcia Sancho J, Gandia L, Lopez M, Garcia A. Permeation and inactivation by calcium and manganese of bovine adrenal chromaffin cell calcium channels. Am J Physiol. 1992;263:C818-24 pubmed
    ..Inactivation of Ca2+ entry was achieved at estimated mean intracellular Mn2+ concentrations as low as 10(-9) M. ..
  28. Zhou Z, Zhao D. Coordinated transitions in neurotransmitter systems for the initiation and propagation of spontaneous retinal waves. J Neurosci. 2000;20:6570-7 pubmed
  29. Gioanni Y, Rougeot C, Clarke P, Lepouse C, Thierry A, Vidal C. Nicotinic receptors in the rat prefrontal cortex: increase in glutamate release and facilitation of mediodorsal thalamo-cortical transmission. Eur J Neurosci. 1999;11:18-30 pubmed
    ..Such a mechanism may be relevant to the cognitive effects of nicotine and nicotinic antagonists. ..
  30. Eberhard D, Holz R. Cholinergic stimulation of inositol phosphate formation in bovine adrenal chromaffin cells: distinct nicotinic and muscarinic mechanisms. J Neurochem. 1987;49:1634-43 pubmed
  31. Vernino S, Rogers M, Radcliffe K, Dani J. Quantitative measurement of calcium flux through muscle and neuronal nicotinic acetylcholine receptors. J Neurosci. 1994;14:5514-24 pubmed
    ..At both muscle and neuronal cholinergic synapses, activity-dependent Ca2+ influx through nicotinic receptors produces intracellular signals that may have important roles in synaptic development, maintenance, and plasticity. ..
  32. Gandia L, Casado L, Lopez M, Garcia A. Separation of two pathways for calcium entry into chromaffin cells. Br J Pharmacol. 1991;103:1073-8 pubmed
  33. Wang Y, Neuman R, Bieger D. Nicotinic cholinoceptor-mediated excitation in ambigual motoneurons of the rat. Neuroscience. 1991;40:759-67 pubmed
    ..5-2 pmol), hexamethonium (0.2 mM) and D-tubocurarine (10 microM) and persisted in the presence of tetrodotoxin (10(-6) M) or Mn2+ (5 mM) in the bathing medium.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  34. Terbush D, Bittner M, Holz R. Ca2+ influx causes rapid translocation of protein kinase C to membranes. Studies of the effects of secretagogues in adrenal chromaffin cells. J Biol Chem. 1988;263:18873-9 pubmed
    ..In addition, the muscarinic receptor-mediated enhancement of nicotinic receptor-stimulated secretion may be due to newly activated protein kinase C. ..
  35. Grider J, Jin J. Vasoactive intestinal peptide release and L-citrulline production from isolated ganglia of the myenteric plexus: evidence for regulation of vasoactive intestinal peptide release by nitric oxide. Neuroscience. 1993;54:521-6 pubmed
    ..The study provides the first direct evidence of nitric oxide production from enteric ganglia. ..
  36. Baccari M, Bani D, Calamai F. Evidence for a modulatory role of orexin A on the nitrergic neurotransmission in the mouse gastric fundus. Regul Pept. 2009;154:54-9 pubmed publisher
    ..These results indicate that, in mouse gastric fundus, OXA exerts a modulatory action at the postganglionic level on the nitrergic neurotransmission...
  37. Blanchet M, Israël Assayag E, Cormier Y. Modulation of airway inflammation and resistance in mice by a nicotinic receptor agonist. Eur Respir J. 2005;26:21-7 pubmed
    ..In conclusion, these results show that 1,1-dimethyl-4-phenylpiperazinium reduces lung inflammation and prevents airway hyperresponsiveness in the mouse model of asthma. ..
  38. Hanna S, Cao K, Wang R. Interaction of acetylcholine with Kir6.1 channels heterologously expressed in human embryonic kidney cells. Eur J Pharmacol. 2005;515:34-42 pubmed
    ..8 pA/pF, n=8, p<0.05). In conclusion, we have demonstrated an excitatory effect of acetylcholine on Kir6.1 channels, which is mediated neither by an acetylcholine receptor-dependent mechanism, nor by alteration in ATP metabolism. ..
  39. Jonsson Fagerlund M, Dabrowski M, Eriksson L. Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009;110:1244-52 pubmed publisher
  40. Schneider D, Perrone M, Galligan J. Nicotinic acetylcholine receptors at sites of neurotransmitter release to the guinea pig intestinal circular muscle. J Pharmacol Exp Ther. 2000;294:363-9 pubmed
    ..Although the prejunctional nAChRs are not targets for endogenously released acetylcholine under the conditions tested here, these receptors may be targets for the development of new prokinetic agents. ..
  41. Wardle K, Ellis E, Baxter G, Kennett G, Gaster L, Sanger G. The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon. Br J Pharmacol. 1994;112:789-94 pubmed
    ..6. SB 204070 is a highly potent, highly selective 5-HT4 receptor antagonist and as such is an important new tool in evaluating the functional role of the 5-HT4 receptor. ..
  42. Xu J, Yang W, Zhang G, Gu Q, Lee L. Calcium transient evoked by nicotine in isolated rat vagal pulmonary sensory neurons. Am J Physiol Lung Cell Mol Physiol. 2007;292:L54-61 pubmed
    ..6% of the RARs tested. In conclusion, nicotine exerts a direct stimulatory effect on vagal pulmonary sensory nerves, and the effect is probably mediated through an activation of the NnAChRs expressed on the membrane of these neurons. ..
  43. Fernandez E, Craviso G. Protein synthesis blockade differentially affects the degradation of constitutive and nicotinic receptor-induced tyrosine hydroxylase protein level in isolated bovine chromaffin cells. J Neurochem. 1999;73:169-78 pubmed
  44. Barnes R, Ward L, Frank K, Tyce G, Hunter L, Rorie D. Nitric oxide modulates evoked catecholamine release from canine adrenal medulla. Neuroscience. 2001;104:1165-73 pubmed
  45. Smith T, Oliver G, Hennig G, O Shea D, Vanden Berghe P, Kang S, et al. A smooth muscle tone-dependent stretch-activated migrating motor pattern in isolated guinea-pig distal colon. J Physiol. 2003;551:955-69 pubmed
    ..These peristaltic waves usually originate just oral to the pellet, and their apparent conduction velocity is generated by activation of descending inhibitory nerve pathways...
  46. Sotirov E, Itzev D, Papasova M. Modulation of electrically evoked responses in rat duodenum by activation of nicotinic cholinoceptors. Clin Exp Pharmacol Physiol. 1998;25:331-5 pubmed
    ..8. The data suggest that activation of nicotinic cholinoceptors modulates EFS-evoked responses in the rat duodenum as a result of the potentiation of nitrergic and adrenergic neurotransmission. ..
  47. Chamberlin N, Bocchiaro C, Greene R, Feldman J. Nicotinic excitation of rat hypoglossal motoneurons. Neuroscience. 2002;115:861-70 pubmed
  48. Guth P, Dunn A, Kronomer K, Norris C. The cholinergic pharmacology of the frog saccule. Hear Res. 1994;75:225-32 pubmed
    ..The difference in distribution of ACH receptors may be important for understanding the physiology of vestibular efferents. ..
  49. Krstić M. Pressor response mediated via histamine H1-receptors of the guinea-pig sympathetic ganglia. Neuropharmacology. 1988;27:1215-9 pubmed
  50. Kuwashima H, Matsumura C, Kimura T. Inhibition and facilitation by pimobendan, a calcium sensitizer, of catecholamine secretion from bovine adrenal chromaffin cells. J Pharmacol Sci. 2003;91:211-8 pubmed
    ..Neither Ca(2+) sensitizing nor PDE-III inhibiting actions seem to be related to these effects. ..
  51. Nieves Cintrón M, Caballero Rivera D, SILVA W, Navedo M, Lasalde Dominicci J. Functional contribution of alpha3L8' to the neuronal nicotinic alpha3 receptor. J Neurosci Res. 2008;86:2884-94 pubmed publisher
    ..These data demonstrate that structural alterations at position alpha3L8' could propagate to the agonist-binding site. ..
  52. Torocsik A, Oberfrank F, Sershen H, Lajtha A, Nemesy K, Vizi E. Characterization of somatodendritic neuronal nicotinic receptors located on the myenteric plexus. Eur J Pharmacol. 1991;202:297-302 pubmed
  53. Hibberd T, Zagorodnyuk V, Spencer N, Brookes S. Identification and mechanosensitivity of viscerofugal neurons. Neuroscience. 2012;225:118-29 pubmed publisher
    ..All viscerofugal neurons are directly mechanosensitive, although they have been reported to receive synaptic inputs. In short, viscerofugal neurons combine interneuronal function with length-sensitive mechanosensitivity. ..