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Chemical Compound Review

Oxotremorine     1-(4-pyrrolidin-1-ylbut-2- ynyl)pyrrolidin...

Synonyms: Oxotremorin, Oxytremorine, Lopac-O-9126, Tocris-0843, CHEMBL7634, ...
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Disease relevance of Oxytremorine


Psychiatry related information on Oxytremorine


High impact information on Oxytremorine


Chemical compound and disease context of Oxytremorine


Biological context of Oxytremorine


Anatomical context of Oxytremorine

  • The lowest behaviorally effective dose, 0.5 microgram OXO, did not influence WM performance when infused into the lateral ventricles (intracerebroventricularly) of either 22MO or 4MO rats [24].
  • Systemic administration of the muscarinic agonist oxotremorine (OXO, 0.1 to 1.0 mg/kg, i.p.) increased LCGU in the neocortex, mesocortex, and paleocortex [25].
  • (2) Stimulation of muscarinic receptor with oxotremorine provokes translocation of m4R from the membrane to endosomes in perikarya and dendrites of medium spiny neurons but has no influence on the localization of m4R in the cytoplasm of cholinergic cell bodies [26].
  • Calcium current modulation by the muscarinic cholinergic agonist oxotremorine methiodide (oxo-M) was examined in sympathetic neurons from the superior cervical ganglion of the rat [27].
  • The muscarinic effects of analogs of oxotremorine were compared on strips of the guinea pig ileum and urinary bladder [28].

Associations of Oxytremorine with other chemical compounds


Gene context of Oxytremorine


Analytical, diagnostic and therapeutic context of Oxytremorine

  • Using whole-cell patch-clamp techniques, which isolate the slow pathway, we found that the muscarinic agonist oxotremorine methiodide not only inhibits currents at positive potentials but enhances N-type current at negative potentials [38].
  • After parasympathectomy, ventricular sarcolemma displayed significant increases in both basal and oxotremorine-stimulated GTPase activity [39].
  • Intracerebroventricular (i.c.v.) pretreatment with antisense oligonucleotides (aODNs) against the alpha subunit of G(q) and G(11) proteins prevented the analgesia induced by physostigmine and oxotremorine [40].
  • In control canines bilateral perfusion with oxotremorine (10(-5)-10(-3) M) did not produce any cataplectic attacks, but did produce muscle atonia after the highest concentration [8].
  • After treatment of embryos in vivo with carbachol to decrease the reserve of spare receptors in the atria, oxotremorine could no longer elicit a significant negative chronotropic response under conditions in which carbachol was still effective [41].


  1. Muscarinic supersensitivity and impaired receptor desensitization in G protein-coupled receptor kinase 5-deficient mice. Gainetdinov, R.R., Bohn, L.M., Walker, J.K., Laporte, S.A., Macrae, A.D., Caron, M.G., Lefkowitz, R.J., Premont, R.T. Neuron (1999) [Pubmed]
  2. Trans-synaptic modulation via muscarinic receptors of serotonin-containing small intensely fluorescent cells of superior cervical ganglion. Hadjiconstantinou, M., Potter, P.E., Neff, N.H. J. Neurosci. (1982) [Pubmed]
  3. Pharmacologic modulation of the autonomic nervous system in the prevention of sudden cardiac death. A study with propranolol, methacholine and oxotremorine in conscious dogs with a healed myocardial infarction. De Ferrari, G.M., Salvati, P., Grossoni, M., Ukmar, G., Vaga, L., Patrono, C., Schwartz, P.J. J. Am. Coll. Cardiol. (1993) [Pubmed]
  4. Regulation of GH3 pituitary tumour-cell adenylate cyclase activity by activators of protein kinase C. Quilliam, L.A., Dobson, P.R., Brown, B.L. Biochem. J. (1989) [Pubmed]
  5. Antidepressant-like effects of triiodothyroacetic acid in mice. Massol, J., Martin, P., Brochet, D., Puech, A., Simon, P. Psychopharmacology (Berl.) (1988) [Pubmed]
  6. Induction of depression with oxotremorine in patients with Alzheimer's disease. Davis, K.L., Hollander, E., Davidson, M., Davis, B.M., Mohs, R.C., Horvath, T.B. The American journal of psychiatry. (1987) [Pubmed]
  7. Cholinergic drug effects and brain muscarinic receptor binding in aged rats. Pedigo, N.W., Minor, L.D., Krumrei, T.N. Neurobiol. Aging (1984) [Pubmed]
  8. Cholinergic regulation of cataplexy in canine narcolepsy in the pontine reticular formation is mediated by M2 muscarinic receptors. Reid, M.S., Tafti, M., Nishino, S., Siegel, J.M., Dement, W.C., Mignot, E. Sleep. (1994) [Pubmed]
  9. 3,4-Methylenedioxyphenyl-, isopropylidenedioxyphenyl-, and benzyl-substituted chiral 2-aminosuccinimides and 3-aminopyrrolidines. Stereoselective investigations of potential anti-parkinsonian, antipsychotic, and anticonvulsant activities. Witiak, D.T., Vishnuvajjala, B.R., Cook, W.L., Minatelli, J.A., Gupta, T.K., Gerald, M.C. J. Med. Chem. (1977) [Pubmed]
  10. The effect of 6-hydroxydopamine on the antinociceptive action of oxotremorine. Slater, P. Psychopharmacology (Berl.) (1981) [Pubmed]
  11. Muscarinic receptors on rat isolated colonic epithelial cells. A correlation between inhibition of [3H]quinuclidinyl benzilate binding and alteration in ion transport. Zimmerman, T.W., Binder, H.J. Gastroenterology (1982) [Pubmed]
  12. Differential involvement of the hippocampus, anterior cingulate cortex, and basolateral amygdala in memory for context and footshock. Malin, E.L., McGaugh, J.L. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  13. Muscarinic cholinergic-receptor stimulation of specific GTP hydrolysis related to adenylate cyclase activity in canine cardiac sarcolemma. Fleming, J.W., Watanabe, A.M. Circ. Res. (1988) [Pubmed]
  14. Electrical responses of smooth muscle cells during cholinergic vasodilation in the rabbit saphenous artery. Komori, K., Suzuki, H. Circ. Res. (1987) [Pubmed]
  15. Centrally active antimuscarinic analogs of oxotremorine selectively block physostigmine-induced hypertension, but not peripheral muscarinic vasodepression. Vargas, H.M., Ringdahl, B. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  16. Neuropharmacological characterization of basal forebrain cholinergic stimulated cataplexy in narcoleptic canines. Reid, M.S., Nishino, S., Tafti, M., Siegel, J.M., Dement, W.C., Mignot, E. Exp. Neurol. (1998) [Pubmed]
  17. Effects of scopolamine, pilocarpine, and oxotremorine on the exploratory behavior of two psychogenetically selected lines of rats in a complex maze. Martin, J.R., Overstreet, D.H., Driscoll, P., Bättig, K. Psychopharmacology (Berl.) (1981) [Pubmed]
  18. Activation of central muscarinic receptors causes respiratory stimulation in conscious animals. Weinstock, M. Br. J. Pharmacol. (1981) [Pubmed]
  19. Cholinergic M2 muscarinic receptor-mediated inhibition of endogenous noradrenaline release from the isolated vascularly perfused rat stomach. Yokotani, K., Osumi, Y. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  20. Subcellular redistribution of m2 muscarinic acetylcholine receptors in striatal interneurons in vivo after acute cholinergic stimulation. Bernard, V., Laribi, O., Levey, A.I., Bloch, B. J. Neurosci. (1998) [Pubmed]
  21. Characterization of muscarinic cholinergic receptors on rat pancreatic acini by N-[3H]methylscopolamine binding. Their relationship with calcium 45 efflux and amylase secretion. Dehaye, J.P., Winand, J., Poloczek, P., Christophe, J. J. Biol. Chem. (1984) [Pubmed]
  22. Activation of M3 muscarinic acetylcholine receptors inhibits voltage-dependent calcium influx in small cell lung carcinoma. Williams, C.L., Lennon, V.A. J. Biol. Chem. (1990) [Pubmed]
  23. Cholinergic antagonism of beta-adrenergic stimulation of cardiac membrane protein phosphorylation in situ. Iwasa, Y., Hosey, M.M. J. Biol. Chem. (1983) [Pubmed]
  24. Cholinergic manipulations in the medial septal area: age-related effects on working memory and hippocampal electrophysiology. Markowska, A.L., Olton, D.S., Givens, B. J. Neurosci. (1995) [Pubmed]
  25. Effects of oxotremorine on local glucose utilization in the rat cerebral cortex. Dam, M., Wamsley, J.K., Rapoport, S.I., London, E.D. J. Neurosci. (1982) [Pubmed]
  26. Regulation of the subcellular distribution of m4 muscarinic acetylcholine receptors in striatal neurons in vivo by the cholinergic environment: evidence for regulation of cell surface receptors by endogenous and exogenous stimulation. Bernard, V., Levey, A.I., Bloch, B. J. Neurosci. (1999) [Pubmed]
  27. A voltage-independent calcium current inhibitory pathway activated by muscarinic agonists in rat sympathetic neurons requires both Galpha q/11 and Gbeta gamma. Kammermeier, P.J., Ruiz-Velasco, V., Ikeda, S.R. J. Neurosci. (2000) [Pubmed]
  28. Selectivity of partial agonists related to oxotremorine based on differences in muscarinic receptor reserve between the guinea pig ileum and urinary bladder. Ringdahl, B. Mol. Pharmacol. (1987) [Pubmed]
  29. Muscarinic control of histamine release from airways. Inhibitory M1-receptors in human bronchi but absence in rat trachea. Reinheimer, T., Möhlig, T., Zimmermann, S., Höhle, K.D., Wessler, I. Am. J. Respir. Crit. Care Med. (2000) [Pubmed]
  30. Interactions of agonists with M2 and M4 muscarinic receptor subtypes mediating cyclic AMP inhibition. McKinney, M., Miller, J.H., Gibson, V.A., Nickelson, L., Aksoy, S. Mol. Pharmacol. (1991) [Pubmed]
  31. The binding of a 2-chloroethylamine derivative of oxotremorine (BM 123) to muscarinic receptors in the rat cerebral cortex. Ehlert, F.J., Jenden, D.J. Mol. Pharmacol. (1985) [Pubmed]
  32. Muscarinic cholinergic receptors of two cell lines that regulate cyclic AMP metabolism by different molecular mechanisms. Evans, T., Smith, M.M., Tanner, L.I., Harden, T.K. Mol. Pharmacol. (1984) [Pubmed]
  33. Novel alkoxy-oxazolyl-tetrahydropyridine muscarinic cholinergic receptor antagonists. Shannon, H.E., Bymaster, F.P., Hendrix, J.C., Quimby, S.J., Mitch, C.H. Psychopharmacology (Berl.) (1995) [Pubmed]
  34. Role of specific muscarinic receptor subtypes in cholinergic parasympathomimetic responses, in vivo phosphoinositide hydrolysis, and pilocarpine-induced seizure activity. Bymaster, F.P., Carter, P.A., Yamada, M., Gomeza, J., Wess, J., Hamilton, S.E., Nathanson, N.M., McKinzie, D.L., Felder, C.C. Eur. J. Neurosci. (2003) [Pubmed]
  35. Regulation of muscarinic acetylcholine receptor function in acetylcholinesterase knockout mice. Li, B., Duysen, E.G., Volpicelli-Daley, L.A., Levey, A.I., Lockridge, O. Pharmacol. Biochem. Behav. (2003) [Pubmed]
  36. Differential in vivo induction of immediate early genes by oxotremorine in the central nervous system of long- and short-sleep mice. Tsiokas, L., Watson, M. Mol. Pharmacol. (1995) [Pubmed]
  37. Muscarinic receptors control glucagon-like peptide 1 secretion by human endocrine L cells. Anini, Y., Brubaker, P.L. Endocrinology (2003) [Pubmed]
  38. Arachidonic acid mediates muscarinic inhibition and enhancement of N-type Ca2+ current in sympathetic neurons. Liu, L., Rittenhouse, A.R. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  39. Selective parasympathectomy increases the quantity of inhibitory guanine nucleotide-binding proteins in canine cardiac ventricle. Hodges, T.D., Bailey, J.C., Fleming, J.W., Kovacs, R.J. Mol. Pharmacol. (1989) [Pubmed]
  40. The phospholipase C-IP3 pathway is involved in muscarinic antinociception. Galeotti, N., Bartolini, A., Ghelardini, C. Neuropsychopharmacology (2003) [Pubmed]
  41. Partial agonist activity of oxotremorine at muscarinic acetylcholine receptors in the embryonic chick heart. Nathanson, N.M., Holttum, J., Hunter, D.D., Halvorsen, S.W. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
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