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Chemical Compound Review

AC1NSKM9     2-[(2S)-5,5- dimethylmorpholin-2...

Synonyms: SureCN340881, AG-A-07905, CHEMBL1895916, KBioSS_002245, SCH-50911, ...
 
 
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Disease relevance of SCH 50911

 

Psychiatry related information on SCH 50911

 

High impact information on SCH 50911

 

Chemical compound and disease context of SCH 50911

 

Anatomical context of SCH 50911

  • In an effort to better understand the mechanisms underlying this inhibition, we examined the effect of the selective GABA(B) receptor antagonist SCH 50911 on the GVG-induced decrease in cocaine's elevation of extracellular DA concentrations in the nucleus accumbens (NACC) [8].
 

Associations of SCH 50911 with other chemical compounds

  • Experiments were conducted to characterize the pharmacology of SCH 50911 ((+)-5,5-dimethyl-2-morpholineacetic acid hydrochloride), a structurally novel GABA-B receptor antagonist [5].
  • This muscimol effect was not affected by bicuculline but occluded the presynaptic inhibitory effect of the GABAB receptor agonist baclofen and was abolished by the type B GABA (GABAB) receptor-specific antagonist (+)-5, 5-dimethyl-2-morpholineacetic acid (SCH 50911; 20 microM) [9].
  • However, application of phaclofen (100 microM GABAB receptor antagonist or SCH 50911, a more potent GABAB antagonist significantly inhibited the DAMGO effect (49+/-15%; 51+/-19% inhibition, P<0.05) [10].
 

Gene context of SCH 50911

  • SCH 50911 was equipotent with the GABAB antagonist CGP 46381 (ID50 = 20 mumol/kg) in the lh/lh mouse model [2].
  • Finally, the NMDA receptor antagonist (+)MK-801 and the GABA(B) receptor antagonist SCH-50911, but not the GABA(A) receptor antagonist (-)bicuculline, dampened the latter response [11].
 

Analytical, diagnostic and therapeutic context of SCH 50911

  • However, microinjection of antagonists with higher affinity for the GABA(B) receptor SCH 50911, CGP 56433 and CGP 55845 did not result in rotational behaviour, but did induce convulsions at higher doses [12].
  • When whole cell recordings were made from lateral superior olive neurons in a brain slice preparation, the long-lasting depression of medial nucleus of the trapezoid body-evoked inhibitory potentials was eliminated by the GABA(B) receptor antagonist, SCH-50911 [13].

References

  1. Presynaptic mechanisms underlying cannabinoid inhibition of excitatory synaptic transmission in rat striatal neurons. Huang, C.C., Lo, S.W., Hsu, K.S. J. Physiol. (Lond.) (2001) [Pubmed]
  2. Characterization of the antiabsence effects of SCH 50911, a GABA-B receptor antagonist, in the lethargic mouse, gamma-hydroxybutyrate, and pentylenetetrazole models. Hosford, D.A., Wang, Y., Liu, C.C., Snead, O.C. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  3. GABAA receptors modulate cannabinoid-evoked hypothermia. Rawls, S.M., Tallarida, R.J., Kon, D.A., Geller, E.B., Adler, M.W. Pharmacol. Biochem. Behav. (2004) [Pubmed]
  4. Modification of d-amphetamine-induced responses by baclofen in rats. Phillis, B.D., Ong, J., White, J.M., Bonnielle, C. Psychopharmacology (Berl.) (2001) [Pubmed]
  5. The pharmacology of SCH 50911: a novel, orally-active GABA-beta receptor antagonist. Bolser, D.C., Blythin, D.J., Chapman, R.W., Egan, R.W., Hey, J.A., Rizzo, C., Kuo, S.C., Kreutner, W. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  6. Protection by the GABAB receptor antagonist, SCH 50911, of gamma-hydroxybutyric acid-induced mortality in mice. Carai, M.A., Colombo, G., Gessa, G.L. Eur. J. Pharmacol. (2004) [Pubmed]
  7. Acupuncture-mediated inhibition of ethanol-induced dopamine release in the rat nucleus accumbens through the GABAB receptor. Yoon, S.S., Kwon, Y.K., Kim, M.R., Shim, I., Kim, K.J., Lee, M.H., Lee, Y.S., Golden, G.T., Yang, C.H. Neurosci. Lett. (2004) [Pubmed]
  8. Implication of the GABA(B) receptor in gamma vinyl-GABA's inhibition of cocaine-induced increases in nucleus accumbens dopamine. Ashby, C.R., Rohatgi, R., Ngosuwan, J., Borda, T., Gerasimov, M.R., Morgan, A.E., Kushner, S., Brodie, J.D., Dewey, S.L. Synapse (1999) [Pubmed]
  9. Presynaptic inhibition by muscimol through GABAB receptors. Yamauchi, T., Hori, T., Takahashi, T. Eur. J. Neurosci. (2000) [Pubmed]
  10. Mu opioids enhance mossy fiber synaptic transmission indirectly by reducing GABAB receptor activation. Jin, W., Chavkin, C. Brain Res. (1999) [Pubmed]
  11. Role of cholinergic and GABAergic systems in the feedback inhibition of dorsal raphe 5-HT neurons. Haddjeri, N., Lucas, G., Blier, P. Neuroreport (2000) [Pubmed]
  12. Functional characterization and expression of thalamic GABA(B) receptors in a rodent model of Parkinson's disease. de Groote, C., Wüllner, U., Löchmann, P.A., Luiten, P.G., Klockgether, T. Neuropharmacology (1999) [Pubmed]
  13. GABA(B) and Trk receptor signaling mediates long-lasting inhibitory synaptic depression. Kotak, V.C., DiMattina, C., Sanes, D.H. J. Neurophysiol. (2001) [Pubmed]
 
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