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Chemical Compound Review

mecamylamine     N,5,6,6-tetramethylbicyclo[2. 2.1]heptan-5...

Synonyms: Mecamine, Mekamine, Mevasine, Revertina, Versamine, ...
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Disease relevance of mecamylamine


Psychiatry related information on mecamylamine


High impact information on mecamylamine


Chemical compound and disease context of mecamylamine


Biological context of mecamylamine


Anatomical context of mecamylamine

  • A direct interaction of the drug with the alpha-BGT recognition site was not required for the increase in receptor number to occur; mecamylamine did not affect binding of alpha-BGT to chromaffin cells in culture in competition binding experiments, although d-tubocurarine did compete with alpha-BGT for binding to its recognition site [24].
  • These results suggested that, at the nicotinic receptors of the neuromuscular junction, mecamylamine acted as a noncompetitive blocker, binding primarily to the receptor's open channel conformation [23].
  • Behavioral and biochemical manifestations of mecamylamine-precipitated nicotine withdrawal in the rat: role of nicotinic receptors in the ventral tegmental area [25].
  • However, the maximal inhibition of responses achieved by alpha-conotoxin-MII (112 nM) was 44.9 +/- 5.4% for synaptosomes and 25.0 +/- 4.1% for slices, compared with an inhibition by 10 microM mecamylamine of 77.9 +/- 3.7 and 88.0 +/- 2.1%, respectively [26].
  • We have previously shown that fourth ventricular administration of Nic rapidly elevated plasma ACTH levels, that a nicotinic cholinergic antagonist, mecamylamine, instilled into the fourth ventricle inhibited the ACTH response to iv Nic, and that Nic stimulated norepinephrine secretion in the hypothalamic paraventricular nucleus [27].

Associations of mecamylamine with other chemical compounds


Gene context of mecamylamine

  • Mecamylamine (non-selective nicotinic receptor inhibitor), alpha-bungarotoxin (alpha7 nicotinic receptor inhibitor) could block Ca2+ accumulation, and then, prevented the phosphorylation on ERK1/2 and p38 [32].
  • These (+/-)-epibatidine effects on FGF-2 expression were antagonized by the non-competitive nAChR antagonist mecamylamine, indicating an involvement of nicotinic receptors [33].
  • Acetylcholine-induced AVP release is antagonized by atropine or mecamylamine, indicating that both muscarinic and nicotinic receptors are mediating the cholinergic effect in these brain regions [34].
  • The P2X purinoceptor blocker, suramin (50 microM) or a nicotinic ACh receptor (nAChR) blocker (hexamethonium, 100 microM; mecamylamine, 1 microM) only partially inhibited these responses, but together, blocked almost all activity [35].
  • In animals treated with mecamylamine the regional haemodynamic effects of the higher dose endothelin-1 were not different from those in animals with intact baroreflexes [36].

Analytical, diagnostic and therapeutic context of mecamylamine


  1. The vagus nerve and nicotinic receptors modulate experimental pancreatitis severity in mice. van Westerloo, D.J., Giebelen, I.A., Florquin, S., Bruno, M.J., Larosa, G.J., Ulloa, L., Tracey, K.J., van der Poll, T. Gastroenterology (2006) [Pubmed]
  2. Rat amylin mediates a pressor response in the anaesthetised rat: implications for the association between hypertension and diabetes mellitus. Haynes, J.M., Hodgson, W.C., Cooper, M.E. Diabetologia (1997) [Pubmed]
  3. Nicotine-sensitive paresis. Yokota, T., Kagamihara, Y., Hayashi, H., Tsukagoshi, H., Tanabe, H. Neurology (1992) [Pubmed]
  4. Prostaglandins and hypothalamic neurotransmitter receptors involved in hyperthermia: a critical evaluation. Simpson, C.W., Ruwe, W.D., Myers, R.D. Neuroscience and biobehavioral reviews. (1994) [Pubmed]
  5. Treatment of Tourette's syndrome with mecamylamine. Sanberg, P.R., Shytle, R.D., Silver, A.A. Lancet (1998) [Pubmed]
  6. Nicotinic acetylcholine receptors as targets for antidepressants. Shytle, R.D., Silver, A.A., Lukas, R.J., Newman, M.B., Sheehan, D.V., Sanberg, P.R. Mol. Psychiatry (2002) [Pubmed]
  7. The role of the dorsal raphe-serotonergic system and cholinergic receptors in the modulation of working memory. Ruotsalainen, S., Miettinen, R., MacDonald, E., Riekkinen, M., Sirviö, J. Neuroscience and biobehavioral reviews. (1998) [Pubmed]
  8. Mecamylamine combined with nicotine skin patch facilitates smoking cessation beyond nicotine patch treatment alone. Rose, J.E., Behm, F.M., Westman, E.C., Levin, E.D., Stein, R.M., Ripka, G.V. Clin. Pharmacol. Ther. (1994) [Pubmed]
  9. Evidence that the antinociceptive tail-flick response is produced independently from changes in either tail-skin temperature or core temperature. Lichtman, A.H., Smith, F.L., Martin, B.R. Pain (1993) [Pubmed]
  10. Cholinergic stimulation blocks endothelial cell activation and leukocyte recruitment during inflammation. Saeed, R.W., Varma, S., Peng-Nemeroff, T., Sherry, B., Balakhaneh, D., Huston, J., Tracey, K.J., Al-Abed, Y., Metz, C.N. J. Exp. Med. (2005) [Pubmed]
  11. Acetylcholine is synthesized by and acts as an autocrine growth factor for small cell lung carcinoma. Song, P., Sekhon, H.S., Jia, Y., Keller, J.A., Blusztajn, J.K., Mark, G.P., Spindel, E.R. Cancer Res. (2003) [Pubmed]
  12. Caenorhabditis elegans levamisole resistance genes lev-1, unc-29, and unc-38 encode functional nicotinic acetylcholine receptor subunits. Fleming, J.T., Squire, M.D., Barnes, T.M., Tornoe, C., Matsuda, K., Ahnn, J., Fire, A., Sulston, J.E., Barnard, E.A., Sattelle, D.B., Lewis, J.A. J. Neurosci. (1997) [Pubmed]
  13. Nicotine addiction and treatment. Rose, J.E. Annu. Rev. Med. (1996) [Pubmed]
  14. The pharmacology of mesolimbic dopamine neurons: a dual-probe microdialysis study in the ventral tegmental area and nucleus accumbens of the rat brain. Westerink, B.H., Kwint, H.F., deVries, J.B. J. Neurosci. (1996) [Pubmed]
  15. Comorbid bipolar disorder in Tourette's syndrome responds to the nicotinic receptor antagonist mecamylamine (Inversine). Shytle, R.D., Silver, A.A., Sanberg, P.R. Biol. Psychiatry (2000) [Pubmed]
  16. Postural hypotension following N-type Ca2+ channel blockade is amplified in experimental hypertension. Wright, C.E., Hawkes, A.L., Angus, J.A. J. Hypertens. (2000) [Pubmed]
  17. Methyllycaconitine, alpha-bungarotoxin and (+)-tubocurarine block fast ATP-gated currents in rat dorsal root ganglion cells. Lalo, U., Pankratov, Y., Krishtal, O., North, R.A. Br. J. Pharmacol. (2004) [Pubmed]
  18. Nicotine-induced decreases in VTA electrical self-stimulation thresholds: blockade by haloperidol and mecamylamine but not scopolamine or ondansetron. Ivanová, S., Greenshaw, A.J. Psychopharmacology (Berl.) (1997) [Pubmed]
  19. Nicotine stimulates a serotonergic autocrine loop in human small-cell lung carcinoma. Cattaneo, M.G., Codignola, A., Vicentini, L.M., Clementi, F., Sher, E. Cancer Res. (1993) [Pubmed]
  20. Regulation of human alpha4beta2 neuronal nicotinic acetylcholine receptors by cholinergic channel ligands and second messenger pathways. Gopalakrishnan, M., Molinari, E.J., Sullivan, J.P. Mol. Pharmacol. (1997) [Pubmed]
  21. Rapid relief of block by mecamylamine of neuronal nicotinic acetylcholine receptors of rat chromaffin cells in vitro: an electrophysiological and modeling study. Giniatullin, R.A., Sokolova, E.M., Di Angelantonio, S., Skorinkin, A., Talantova, M.V., Nistri, A. Mol. Pharmacol. (2000) [Pubmed]
  22. Untranslated region-dependent exclusive expression of high-sensitivity subforms of alpha4beta2 and alpha3beta2 nicotinic acetylcholine receptors. Briggs, C.A., Gubbins, E.J., Marks, M.J., Putman, C.B., Thimmapaya, R., Meyer, M.D., Surowy, C.S. Mol. Pharmacol. (2006) [Pubmed]
  23. The acetylcholine receptor of the neuromuscular junction recognizes mecamylamine as a noncompetitive antagonist. Varanda, W.A., Aracava, Y., Sherby, S.M., VanMeter, W.G., Eldefrawi, M.E., Albuquerque, E.X. Mol. Pharmacol. (1985) [Pubmed]
  24. Marked up-regulation of the beta-bungarotoxin site in adrenal chromaffin cells by specific nicotinic antagonists. Quik, M., Geertsen, S., Trifaró, J.M. Mol. Pharmacol. (1987) [Pubmed]
  25. Behavioral and biochemical manifestations of mecamylamine-precipitated nicotine withdrawal in the rat: role of nicotinic receptors in the ventral tegmental area. Hildebrand, B.E., Panagis, G., Svensson, T.H., Nomikos, G.G. Neuropsychopharmacology (1999) [Pubmed]
  26. Differential inhibition by alpha-conotoxin-MII of the nicotinic stimulation of [3H]dopamine release from rat striatal synaptosomes and slices. Kaiser, S.A., Soliakov, L., Harvey, S.C., Luetje, C.W., Wonnacott, S. J. Neurochem. (1998) [Pubmed]
  27. Selective administration of nicotine into catecholaminergic regions of rat brainstem stimulates adrenocorticotropin secretion. Matta, S.G., Foster, C.A., Sharp, B.M. Endocrinology (1993) [Pubmed]
  28. Augmented responses to intrathecal nicotinic agonists in spontaneous hypertension. Khan, I.M., Printz, M.P., Yaksh, T.L., Taylor, P. Hypertension (1994) [Pubmed]
  29. Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function. Xiao, Y., Meyer, E.L., Thompson, J.M., Surin, A., Wroblewski, J., Kellar, K.J. Mol. Pharmacol. (1998) [Pubmed]
  30. Mechanisms underlying cerebrovascular effects of cigarette smoking in rats in vivo. Iida, M., Iida, H., Dohi, S., Takenaka, M., Fujiwara, H. Stroke (1998) [Pubmed]
  31. A nicotine antagonist, mecamylamine, reduces cue-induced cocaine craving in cocaine-dependent subjects. Reid, M.S., Mickalian, J.D., Delucchi, K.L., Berger, S.P. Neuropsychopharmacology (1999) [Pubmed]
  32. Nicotine stimulates adhesion molecular expression via calcium influx and mitogen-activated protein kinases in human endothelial cells. Wang, Y., Wang, Z., Zhou, Y., Liu, L., Zhao, Y., Yao, C., Wang, L., Qiao, Z. Int. J. Biochem. Cell Biol. (2006) [Pubmed]
  33. The nicotinic acetylcholine receptor agonist (+/-)-epibatidine increases FGF-2 mRNA and protein levels in the rat brain. Belluardo, N., Mudò, G., Blum, M., Cheng, Q., Caniglia, G., Dell'Albani, P., Fuxe, K. Brain Res. Mol. Brain Res. (1999) [Pubmed]
  34. IL-1 beta potentiates the acetylcholine-induced release of vasopressin from the hypothalamus in vitro, but not from the amygdala. Raber, J., Pich, E.M., Koob, G.F., Bloom, F.E. Neuroendocrinology (1994) [Pubmed]
  35. Co-release of ATP and ACh mediates hypoxic signalling at rat carotid body chemoreceptors. Zhang, M., Zhong, H., Vollmer, C., Nurse, C.A. J. Physiol. (Lond.) (2000) [Pubmed]
  36. Coeliac haemodynamic effects of endothelin-1, endothelin-3, proendothelin-1 [1-38] and proendothelin-3 [1-41] in conscious rats. Gardiner, S.M., Kemp, P.A., Compton, A.M., Bennett, T. Br. J. Pharmacol. (1992) [Pubmed]
  37. Muscarinic and nicotinic contributions to cognitive function and cortical blood flow. Gitelman, D.R., Prohovnik, I. Neurobiol. Aging (1992) [Pubmed]
  38. Age-related effects of the nicotinic antagonist mecamylamine on cognition and behavior. Newhouse, P.A., Potter, A., Corwin, J., Lenox, R. Neuropsychopharmacology (1994) [Pubmed]
  39. Peripheral and central sites of action for A-85380 in the spinal nerve ligation model of neuropathic pain. Rueter, L.E., Kohlhaas, K.L., Curzon, P., Surowy, C.S., Meyer, M.D. Pain (2003) [Pubmed]
  40. Effects of the competitive nicotinic antagonist erysodine on behavior occasioned or maintained by nicotine: comparison with mecamylamine. Mansbach, R.S., Chambers, L.K., Rovetti, C.C. Psychopharmacology (Berl.) (2000) [Pubmed]
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