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Chemical Compound Review

Prozerin     [3- (dimethylcarbamoyloxy)phenyl]- trimethyl...

Synonyms: Eustigmin, Eustigmine, Neostigmin, Prostigmin, Synstigmin, ...
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Disease relevance of Prostigmin


Psychiatry related information on Prostigmin


High impact information on Prostigmin

  • In the in vitro study, HSR-803 inhibited cholinesterase dose-dependently, and IC50 was 2.9 x 10(-6) mol/L, while those of neostigmine and domperidone were 2.3 x 10(-8) mol/L and 1.7 x 10(-5) mol/L, respectively [11].
  • In 85% of experiments with guanethidine, neostigmine, glucose, and castor oil, giant migrating contractions occurred before defecation [12].
  • In order to investigate the pathophysiology of this symptom, we studied colonic compliance, as well as motor and myoelectrical activity, in the fasting and postprandial states and after neostigmine stimulation in 9 patients with clinically and electrophysiologically documented complete thoracic spinal cord injury [13].
  • Intraluminally administered neostigmine or atropine did not influence transport in either jejunum or ileum [14].
  • A considerable portal/femoral vein gradient ranging from twofold in the basal state to sevenfold during stimulation with neostigmine indicated that the gut was the main source of circulating VIP [15].

Chemical compound and disease context of Prostigmin


Biological context of Prostigmin


Anatomical context of Prostigmin


Associations of Prostigmin with other chemical compounds


Gene context of Prostigmin

  • In conclusion, cholinergic agonists such as neostigmine are able to increase both basal and GHRH-induced GH secretion in short children even when given intranasally [30].
  • Responses to neurally released ACh were revealed in Sl/Sl(d) mice by inhibiting ACh breakdown with the acetylcholinesterase inhibitor neostigmine [31].
  • In conclusion, these results indicate that IT neostigmine facilitates the activation of spinal M2 receptors and this activation ultimately leads to release of adrenal catecholamines which contribute to the anti-inflammatory effect observed at the site of tissue inflammation [32].
  • This possibility was supported by the finding that atropine and pirenzepine which are known to have comparable affinities for M1 but not M2 receptors, had comparable potencies in antagonizing the action of oxotremorine or neostigmine [33].
  • We asked if administration of neostigmine (an acetylcholinesterase inhibitor) and/or succinylcholine (an agent which competes for and inhibits butyrylcholinesterase) altered ACh responsiveness in hyporesponsive C3H/HeJ and hyperresponsive A/J mouse strains [34].

Analytical, diagnostic and therapeutic context of Prostigmin

  • Two patients who had an initial response to neostigmine required colonoscopic decompression for recurrence of colonic distention; one eventually underwent subtotal colectomy [2].
  • Thymopoietin and myasthenia gravis: neostigmine-responsive neuromuscular block produced in mice by a synthetic peptide fragment of thymopoietin [35].
  • They failed to demonstrate the postprandial increase in colonic motor and myoelectrical activity observed in a control group (p less than 0.01), but did respond to neostigmine with an increase in both motor and myoelectrical activity (p less than 0.02), suggesting an intact myogenic component [13].
  • A transection and reanastomosis in the mid-small intestine blocked the reflex inhibition by close intraarterial injection of neostigmine beyond the transection site [36].
  • These stimulatory effects of neostigmine on DA efflux in the striatum were confirmed using in vivo microdialysis [37].


  1. Neostigmine for acute colonic pseudo-obstruction. Nicholson, D. N. Engl. J. Med. (1999) [Pubmed]
  2. Neostigmine for the treatment of acute colonic pseudo-obstruction. Ponec, R.J., Saunders, M.D., Kimmey, M.B. N. Engl. J. Med. (1999) [Pubmed]
  3. Blockade of acetylcholine receptors: a model of myasthenia gravis. Satyamurti, S., Drachman, D.B., Slone, F. Science (1975) [Pubmed]
  4. Doxepin overdose. Success with physostigmine and failure with neostigmine in reversing toxicity. Janson, P.A., Watt, J.B., Hermos, J.A. JAMA (1977) [Pubmed]
  5. Letter: Experimental myopathy induced by neostigmine methylsulphate. Kawabuchi, M., Kanaseki, T., Osame, M., Watanabe, S., Igata, A. Lancet (1975) [Pubmed]
  6. Gastrointestinal myoelectrical activity in idiopathic intestinal pseudo-obstruction. Sullivan, M.A., Snape, W.J., Matarazzo, S.A., Petrokubi, R.J., Jeffries, G., Cohen, S. N. Engl. J. Med. (1977) [Pubmed]
  7. Pontine nitric oxide modulates acetylcholine release, rapid eye movement sleep generation, and respiratory rate. Leonard, T.O., Lydic, R. J. Neurosci. (1997) [Pubmed]
  8. Coexisting childhood schizophrenia and myasthenia gravis treated successfully with neostigmine bromide. Schnackenberg, R.C., Holmes, G. The American journal of psychiatry. (1977) [Pubmed]
  9. Memory modulation with peripherally acting cholinergic drugs. Rush, D.K., Streit, K. Psychopharmacology (Berl.) (1992) [Pubmed]
  10. M2 muscarinic receptors in pontine reticular formation of C57BL/6J mouse contribute to rapid eye movement sleep generation. Coleman, C.G., Lydic, R., Baghdoyan, H.A. Neuroscience (2004) [Pubmed]
  11. A novel water-soluble dopamine-2 antagonist with anticholinesterase activity in gastrointestinal motor activity. Comparison with domperidone and neostigmine. Iwanaga, Y., Miyashita, N., Morikawa, K., Mizumoto, A., Kondo, Y., Itoh, Z. Gastroenterology (1990) [Pubmed]
  12. Giant migrating contractions during defecation in the dog colon. Karaus, M., Sarna, S.K. Gastroenterology (1987) [Pubmed]
  13. Colonic dysfunction in patients with thoracic spinal cord injury. Glick, M.E., Meshkinpour, H., Haldeman, S., Hoehler, F., Downey, N., Bradley, W.E. Gastroenterology (1984) [Pubmed]
  14. The influence of a parasympathetic agonist and antagonist on human intestinal transport in vivo. Morris, A.I., Turnberg, L.A. Gastroenterology (1980) [Pubmed]
  15. Neural release of vasoactive intestinal peptide from the gut. Bitar, K.N., Said, S.I., Weir, G.C., Saffouri, B., Makhlouf, G.M. Gastroenterology (1980) [Pubmed]
  16. Effect of intrahypothalamic injection of neostigmine on the secretion of epinephrine and norepinephrine and on plasma glucose level. Honmura, A., Yanase, M., Saito, H., Iguchi, A. Endocrinology (1992) [Pubmed]
  17. Involvement of the hippocampus in central nervous system-mediated glucoregulation in rats. Uemura, K., Iguchi, A., Yatomi, A., Miura, H., Honmura, A., Yanase, M., Sakamoto, N. Endocrinology (1989) [Pubmed]
  18. Role of increased cholinergic activity in reperfusion induced ventricular arrhythmias. Ferrara, N., Bonaduce, D., Abete, P., Leosco, D., Longobardi, G., Canonico, V., Rengo, F. Cardiovasc. Res. (1987) [Pubmed]
  19. Hyperglycemia induced by hippocampal administration of neostigmine is suppressed by intrahypothalamic atropine. Iguchi, A., Uemura, K., Kunoh, Y., Miura, H., Ishiguro, T., Nonogaki, K., Tamagawa, T., Gotoh, M., Sakamoto, N. Neuropharmacology (1991) [Pubmed]
  20. Edrophonium: duration of action and atropine requirement in humans during halothane anesthesia. Cronnelly, R., Morris, R.B., Miller, R.D. Anesthesiology (1982) [Pubmed]
  21. Influence of neostigmine treatment on embryonic development of acetylcholine receptors and neuromuscular junctions. Sohal, G.S., Boydston, W.R. J. Cell Biol. (1982) [Pubmed]
  22. Concentration-dependent effects of neostigmine on the endplate acetylcholine receptor channel complex. Fiekers, J.F. J. Neurosci. (1985) [Pubmed]
  23. Functional decortication lowers ventromedial hypothalamic activation induced by hippocampal neostigmine injection. Monda, M., Viggiano, A., De Luca, V. Cereb. Cortex (2000) [Pubmed]
  24. Regional differences in cerebrovascular cholinergic innervation in goats. Triguero, D., López de Pablo, A.L., Gómez, B., Estrada, C. Stroke (1988) [Pubmed]
  25. Modulation of dopamine efflux in the nucleus accumbens after cholinergic stimulation of the ventral tegmental area in intact, pedunculopontine tegmental nucleus-lesioned, and laterodorsal tegmental nucleus-lesioned rats. Blaha, C.D., Allen, L.F., Das, S., Inglis, W.L., Latimer, M.P., Vincent, S.R., Winn, P. J. Neurosci. (1996) [Pubmed]
  26. Abnormal colonic motility in progressive systemic sclerosis. Battle, W.M., Snape, W.J., Wright, S., Sullivan, M.A., Cohen, S., Meyers, A., Tuthill, R. Ann. Intern. Med. (1981) [Pubmed]
  27. Differential cholinergic regulation of dopamine release in the dorsal and ventral neostriatum of the rat: an in vivo microdialysis study. O'Connor, W.T., Drew, K.L., Ungerstedt, U. J. Neurosci. (1995) [Pubmed]
  28. Molecular characterization of maize acetylcholinesterase: a novel enzyme family in the plant kingdom. Sagane, Y., Nakagawa, T., Yamamoto, K., Michikawa, S., Oguri, S., Momonoki, Y.S. Plant Physiol. (2005) [Pubmed]
  29. Inhibitory effects of cholinergic agents on the release of transmitter at the frog neuromuscular junction. Duncan, C.J., Publicover, S.J. J. Physiol. (Lond.) (1979) [Pubmed]
  30. Intranasal administration of neostigmine potentiates both intravenous and intranasal growth hormone (GH)-releasing hormone-induced GH release in short children. Ghigo, E., Procopio, M., Bellone, J., Mazza, E., Mucci, M., Boghen, M.F., Müller, E.E., Camanni, F. J. Clin. Endocrinol. Metab. (1991) [Pubmed]
  31. Loss of enteric motor neurotransmission in the gastric fundus of Sl/Sl(d) mice. Beckett, E.A., Horiguchi, K., Khoyi, M., Sanders, K.M., Ward, S.M. J. Physiol. (Lond.) (2002) [Pubmed]
  32. Intrathecal neostigmine reduces the zymosan-induced inflammatory response in a mouse air pouch model via adrenomedullary activity: involvement of spinal muscarinic type 2 receptors. Yoon, S.Y., Kwon, Y.B., Kim, H.W., Roh, D.H., Kang, S.Y., Kim, C.Y., Han, H.J., Kim, K.W., Yang, I.S., Beitz, A.J., Lee, J.H. Neuropharmacology (2005) [Pubmed]
  33. Central muscarinic cholinergic influences on ethanol sensitivity in long-sleep and short-sleep mice. Erwin, V.G., Korte, A., Jones, B.C. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  34. Cholinesterase activity is similar in C3H/HeJ and A/J mice and does not account for their different bronchoconstrictor responsiveness. Bulut, Y., Kleeberger, S.R., Hirshman, C.A. Exp. Lung Res. (1999) [Pubmed]
  35. Thymopoietin and myasthenia gravis: neostigmine-responsive neuromuscular block produced in mice by a synthetic peptide fragment of thymopoietin. Goldstein, G., Schlesinger, D.H. Lancet (1975) [Pubmed]
  36. An intrinsic neural pathway for long intestino-intestinal inhibitory reflexes. Frantzides, C.T., Sarna, S.K., Matsumoto, T., Lang, I.M., Condon, R.E. Gastroenterology (1987) [Pubmed]
  37. Modulation of dopamine efflux in the striatum following cholinergic stimulation of the substantia nigra in intact and pedunculopontine tegmental nucleus-lesioned rats. Blaha, C.D., Winn, P. J. Neurosci. (1993) [Pubmed]
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