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Chemical Compound Review

Mip-urea     1-(1-methylindol-5-yl)-3- pyridin-3-yl-urea

Synonyms: Tocris-1371, CHEMBL85194, SureCN173735, S0568_SIGMA, AC1L2QVR, ...
 
 
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Disease relevance of Mip-urea

  • ). Catalepsy induced by MDL 100,151 (3 mg/kg) was blocked by co-treatment with clozapine, but not by SB 200646A (both at 10 mg/kg, s.c [1].
  • A 5-HT2C receptor binding assay using [3H]-mesulergine and SB 200646A to define nonspecific binding was applied to postmortem tissue from patients with Parkinson's disease and from age-matched control patients [2].
 

Psychiatry related information on Mip-urea

 

High impact information on Mip-urea

  • Furthermore, we have demonstrated that systemic administration of selective 5-HT2C receptor antagonists SB 200646A (20 mg/kg) and SB 206553 (20 mg/kg) can potentiate the antiparkinsonian action of the dopamine D2 receptor agonist quinpirole in the 6-hydroxydopamine-lesioned rat [5].
  • The increase in social interaction was prevented by pretreatment with the 5-HT2C/2B receptor antagonist N-(1-methyl-5-indoyl)-N'-(3-pyridyl) urea hydrochloride (SB 200646A, at 2 but not 1 mg/kg p.o., 1 hr pretest), which did not alter behaviour when given alone [6].
  • SB 200646A is the first selective 5-HT2C/5-HT2B receptor antagonist and has previously been observed to have anxiolytic-like properties in the rat social interaction test [7].
  • The selective 5-HT2B/2C receptor antagonist, SB 200646A evoked a concentration-dependent, parallel and dextral displacement of the concentration-response curve to 5-HT, yielding a pA2 estimate of 7.17 [8].
  • However, although mianserin, methiothepin, ritanserin, mesulergine and N-(1-methyl-5'-indolyl)-N'-(3-pyridyl)urea hydrochloride (SB 200646) all antagonised the effect of 5-hydroxytryptamine (5-HT) on IP3 formation in the rat choroid plexus, they failed to antagonise the mCPP response in the drug discrimination studies [9].
 

Gene context of Mip-urea

  • Effect of SB 200646A, a 5-HT2C/5-HT2B receptor antagonist, in two conflict models of anxiety [7].

References

  1. Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat. Kalkman, H.O., Neumann, V., Nozulak, J., Tricklebank, M.D. Eur. J. Pharmacol. (1998) [Pubmed]
  2. 5-HT2C receptor binding is increased in the substantia nigra pars reticulata in Parkinson's disease. Fox, S.H., Brotchie, J.M. Mov. Disord. (2000) [Pubmed]
  3. In vivo properties of SB 200646A, a 5-HT2C/2B receptor antagonist. Kennett, G.A., Wood, M.D., Glen, A., Grewal, S., Forbes, I., Gadre, A., Blackburn, T.P. Br. J. Pharmacol. (1994) [Pubmed]
  4. Involvement of 5-HT(2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism? Meneses, A. Cell. Mol. Neurobiol. (2002) [Pubmed]
  5. Behavioral effects of 5-HT2C receptor antagonism in the substantia nigra zona reticulata of the 6-hydroxydopamine-lesioned rat model of Parkinson's disease. Fox, S.H., Moser, B., Brotchie, J.M. Exp. Neurol. (1998) [Pubmed]
  6. Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat. Duxon, M.S., Kennett, G.A., Lightowler, S., Blackburn, T.P., Fone, K.C. Neuropharmacology (1997) [Pubmed]
  7. Effect of SB 200646A, a 5-HT2C/5-HT2B receptor antagonist, in two conflict models of anxiety. Kennett, G.A., Bailey, F., Piper, D.C., Blackburn, T.P. Psychopharmacology (Berl.) (1995) [Pubmed]
  8. Functional evidence for a 5-HT2B receptor mediating contraction of longitudinal muscle in human small intestine. Borman, R.A., Burleigh, D.E. Br. J. Pharmacol. (1995) [Pubmed]
  9. Pharmacologic evaluation of the discriminative stimulus of metachlorophenylpiperazine. Bourson, A., Wanner, D., Wyler, R., Petit, N., Zwingelstein, C., Rudler, A., Sleight, A.J. Pharmacol. Biochem. Behav. (1996) [Pubmed]
 
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