The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Arecaine     1-methyl-5,6-dihydro-2H- pyridine-3...

Synonyms: Arecaidine, Methylguvacine, CHEMBL432561, SureCN336164, NSC-76017, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of C10128


Psychiatry related information on C10128

  • However, arecaidine, at the same i.c.v. doses, was able to reduce the pain threshold in the hot-plate and paw pressure tests.(ABSTRACT TRUNCATED AT 250 WORDS)[5]
  • As tertiary arecaidine and isoarecaidine esters easily penetrate the blood-brain barrier, they might also stimulate central M1 receptors and thus become lead compounds in the search for an effective drug treatment of Alzheimer's disease [6].

High impact information on C10128

  • Acetylcholine- and arecaidine propargyl ester-induced 6-keto-PGF1 alpha synthesis and cGMP formation in endothelial cells were attenuated by atropine, AF-DX 116 (M2 antagonist), and hexahydrosiladifenidol (M3 antagonist) but not by pirenzepine (M1 antagonist) [7].
  • Employing this technique, we found that the GABAA agonists, muscimol, isoguvacine, 4,5,6,7-tetrahydroisoxazolo(5,4-C)pyridine-3-ol, and 3-amino-1-propane sulfonate, all produced a concentration-dependent increase in 36Cl- influx, but baclofen, a GABAB agonist, failed to alter 36Cl- flux [8].
  • Either isoguvacine (a GABA(A) receptor agonist) or kynurenic acid (a non-selective ionotropic glutamate receptor antagonist) microinjected bilaterally into the paraventricular nucleus (PVN) attenuated the increase in LSNA induced by the hyperosmotic stimulus (control: 25 +/- 2%; after isoguvacine: 7 +/- 2%; after kynurenic: 8 +/- 3%) [9].
  • In the formalin model of orofacial nociception in rats, a peri-oral co-injection of the M2 agonist arecaidine dose-dependently inhibited phase 2 nocifensive behavior up to approximately 50% at 5 nmol [10].
  • Control experiments using a GABAA receptor agonist, isoguvacine, indicated that both components of the baroreflex (parasympathetic and sympathetic) could be blocked from the NTS injection site [11].

Biological context of C10128


Anatomical context of C10128

  • Acetylcholine and arecaidine propargyl ester, a selective M2 agonist, produced a dose-dependent increase in 6-keto-PGF1 alpha output and cGMP formation in confluent endothelial cells but not in confluent vascular smooth muscle cells [7].
  • Does uptake limit the actions of GABA agonists in vivo? Experiments with muscimol, isoguvacine and THIP in cat spinal cord [17].
  • 2. Interneurons and pyramidal cells from P2-5 slices loaded with fluo-3 AM responded by an increase in [Ca2+]i to isoguvacine and to glutamate, in contrast to cells from P12-13 slices which responded to glutamate but not to isoguvacine [18].
  • 2. The arecaidine 2-butynyl and 2-pentynyl esters were approximately equipotent with APE at M1 and M2 receptors, whereas the 2-hexynyl derivative was found to be less potent than APE in atria (-log EC50 = 6.80) and ileum (-log EC50 = 6.70) by about one order of magnitude [15].
  • Likewise, isoguvacine (10(-5) to 10(-4) M) reduced amplitudes (-26.7% to -37.5%) and increased latencies (+11.2% and +24.0%) of cuneate-gracilis fasciculi responses but had little or no effect on corticospinal tract response amplitudes (-6.2% to -3.8%) or latencies (-0.8% to +1.5%) [19].

Associations of C10128 with other chemical compounds


Gene context of C10128

  • GABA or GABA(A) agonist isoguvacine treatment resulted in increased or decreased levels of several mRNAs, including transcription factors (c-fos, hsf-1, egr-1) and cell cycle-associated genes (Cdk2, cyclin D1) [23].
  • Isoguvacine (EC50 approximately to 10 microM) induced biphasic relaxation for both alpha 1 beta 3 and alpha 1 beta 3 gamma 2 subunit receptors (tau 1 = 288.6 +/- 43.3 and 167 +/- 15 ms, and tau 2 = 8.0 +/- 1.9 and 4.4 +/- 0.4 S, respectively, for each subunit combination) [21].
  • In contrast, the GABA(A) receptor agonists 3APS and isoguvacine (10(-5) M each) did not modify endozepine release [24].
  • When neurointermediate lobes were treated for 3 days, inhibition of POMC biosynthesis by NPY was maintained, and inhibition by apomorphine was even stronger, whereas isoguvacine gave an inhibition of 52%, and baclofen produced 34% inhibition [25].
  • The GABAA agonist, isoguvacine (10-100 microM), did not reduce SP release but, if anything, tended to increase SP release [26].

Analytical, diagnostic and therapeutic context of C10128


  1. Betel nuts, arecaidine, and oral cancer. Ashby, J., Styles, J.A., Boyland, E. Lancet (1979) [Pubmed]
  2. Hippocampal CA1 lacunosum-moleculare interneurons: comparison of effects of anoxia on excitatory and inhibitory postsynaptic currents. Khazipov, R., Congar, P., Ben-Ari, Y. J. Neurophysiol. (1995) [Pubmed]
  3. Involvement of dihydropyridine-sensitive calcium channels in the GABAA potentiation of TRH-induced TSH release. Roussel, J.P., Astier, H. Eur. J. Pharmacol. (1990) [Pubmed]
  4. An in-vitro comparison of human fibroblasts from normal and oral submucous fibrosis tissue. Meghji, S., Scutt, A., Harvey, W., Canniff, J.P. Arch. Oral Biol. (1987) [Pubmed]
  5. Role of muscarinic receptor subtypes in central antinociception. Bartolini, A., Ghelardini, C., Fantetti, L., Malcangio, M., Malmberg-Aiello, P., Giotti, A. Br. J. Pharmacol. (1992) [Pubmed]
  6. Stimulation of ganglionic muscarinic M1 receptors by a series of tertiary arecaidine and isoarecaidine esters in the pithed rat. Wess, J., Lambrecht, G., Moser, U., Mutschler, E. Eur. J. Pharmacol. (1987) [Pubmed]
  7. Muscarinic receptor-mediated prostacyclin and cGMP synthesis in cultured vascular cells. Jaiswal, N., Jaiswal, R.K., Malik, K.U. Mol. Pharmacol. (1991) [Pubmed]
  8. gamma-Aminobutyric acid agonists and antagonists alter chloride flux across brain membranes. Allan, A.M., Harris, R.A. Mol. Pharmacol. (1986) [Pubmed]
  9. A spinal vasopressinergic mechanism mediates hyperosmolality-induced sympathoexcitation. Antunes, V.R., Yao, S.T., Pickering, A.E., Murphy, D., Paton, J.F. J. Physiol. (Lond.) (2006) [Pubmed]
  10. Cholinergic modulation of nociceptive responses in vivo and neuropeptide release in vitro at the level of the primary sensory neuron. Dussor, G.O., Helesic, G., Hargreaves, K.M., Flores, C.M. Pain (2004) [Pubmed]
  11. Nociception attenuates parasympathetic but not sympathetic baroreflex via NK1 receptors in the rat nucleus tractus solitarii. Pickering, A.E., Boscan, P., Paton, J.F. J. Physiol. (Lond.) (2003) [Pubmed]
  12. Age-related decrease in GABAB receptor binding in the Fischer 344 rat inferior colliculus. Milbrandt, J.C., Albin, R.L., Caspary, D.M. Neurobiol. Aging (1994) [Pubmed]
  13. GABA-induced facilitation of the periodic bursting activity of oxytocin neurones in suckled rats. Moos, F.C. J. Physiol. (Lond.) (1995) [Pubmed]
  14. Coexistence of GABAA and GABAB receptors on A delta and C primary afferents. Désarmenien, M., Feltz, P., Occhipinti, G., Santangelo, F., Schlichter, R. Br. J. Pharmacol. (1984) [Pubmed]
  15. Structure-activity relationships of new analogues of arecaidine propargyl ester at muscarinic M1 and M2 receptor subtypes. Moser, U., Lambrecht, G., Wagner, M., Wess, J., Mutschler, E. Br. J. Pharmacol. (1989) [Pubmed]
  16. A metabolomic approach to the metabolism of the areca nut alkaloids arecoline and arecaidine in the mouse. Giri, S., Idle, J.R., Chen, C., Zabriskie, T.M., Krausz, K.W., Gonzalez, F.J. Chem. Res. Toxicol. (2006) [Pubmed]
  17. Does uptake limit the actions of GABA agonists in vivo? Experiments with muscimol, isoguvacine and THIP in cat spinal cord. Lodge, D., Curtis, D.R., Johnston, G.A. J. Neurochem. (1978) [Pubmed]
  18. Synaptic GABAA activation induces Ca2+ rise in pyramidal cells and interneurons from rat neonatal hippocampal slices. Leinekugel, X., Tseeb, V., Ben-Ari, Y., Bregestovski, P. J. Physiol. (Lond.) (1995) [Pubmed]
  19. GABA and potassium effects on corticospinal and primary afferent tracts of neonatal rat spinal dorsal columns. Honmou, O., Sakatani, K., Young, W. Neuroscience (1993) [Pubmed]
  20. gamma-Aminobutyric acidB receptor activation modifies agonist binding to beta-adrenergic receptors in rat brain cerebral cortex. Scherer, R.W., Ferkany, J.W., Karbon, E.W., Enna, S.J. J. Neurochem. (1989) [Pubmed]
  21. Recombinant GABAA receptor desensitization: the role of the gamma 2 subunit and its physiological significance. Dominguez-Perrot, C., Feltz, P., Poulter, M.O. J. Physiol. (Lond.) (1996) [Pubmed]
  22. Alternative splicing of a Drosophila GABA receptor subunit gene identifies determinants of agonist potency. Hosie, A.M., Buckingham, S.D., Presnail, J.K., Sattelle, D.B. Neuroscience (2001) [Pubmed]
  23. Insights into GABA receptor signalling in TM3 Leydig cells. Doepner, R.F., Geigerseder, C., Frungieri, M.B., Gonzalez-Calvar, S.I., Calandra, R.S., Raemsch, R., Fohr, K., Kunz, L., Mayerhofer, A. Neuroendocrinology (2005) [Pubmed]
  24. GABA inhibits endozepine release from cultured rat astrocytes. Patte, C., Gandolfo, P., Leprince, J., Thoumas, J.L., Fontaine, M., Vaudry, H., Tonon, M.C. Glia (1999) [Pubmed]
  25. Differential action of secreto-inhibitors on proopiomelanocortin biosynthesis in the intermediate pituitary of Xenopus laevis. Dotman, C.H., Cruijsen, P.M., Jenks, B.G., Roubos, E.W. Endocrinology (1996) [Pubmed]
  26. Gamma-aminobutyric acidB, but not gamma-aminobutyric acidA receptor activation, inhibits electrically evoked substance P-like immunoreactivity release from the rat spinal cord in vitro. Malcangio, M., Bowery, N.G. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  27. Modulation of GABA-gated chloride currents by intracellular Ca2+ in cultured porcine melanotrophs. Mouginot, D., Feltz, P., Schlichter, R. J. Physiol. (Lond.) (1991) [Pubmed]
  28. GABA(B) receptor autoradiography in hippocampal sclerosis associated with human temporal lobe epilepsy. Billinton, A., Baird, V.H., Thom, M., Duncan, J.S., Upton, N., Bowery, N.G. Br. J. Pharmacol. (2001) [Pubmed]
  29. The Kölliker-Fuse nucleus gates the postinspiratory phase of the respiratory cycle to control inspiratory off-switch and upper airway resistance in rat. Dutschmann, M., Herbert, H. Eur. J. Neurosci. (2006) [Pubmed]
  30. Agonist administration in ovo down-regulates cerebellar GABAA receptors in the chick embryo. Calkin, P.A., Baumgartner, B.J., Barnes, E.M. Brain Res. Mol. Brain Res. (1994) [Pubmed]
  31. High-performance liquid chromatographic determination of arecoline in human saliva. Cox, S., Piatkov, I., Vickers, E.R., Ma, G. Journal of chromatography. A. (2004) [Pubmed]
WikiGenes - Universities