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Chemical Compound Review

CHEMBL71950     4-bromo-N-(2-methyl-3-oxo-6- phenyl-2,5...

Synonyms: AGN-PC-000PNP, SureCN8977570, CHEBI:214223, AC1L522V, L-365,031, ...
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High impact information on L 365031

  • Two potent and highly selective nonpeptide antagonists, L-365,031 [1-methyl-3-(4-bromobenzoyl)amino-5-phenyl-3H-1,4 benzodiazepin-2-one] and 3H-L-364,718 [1-methyl-3-(2-indoloyl)amino-5-phenyl-3H-1,4 benzodiazepin-2-one] were used to localize "peripheral" CCK receptors in rat brain [1].
  • In autoradiographic experiments, L-365,031 displaced 125I-Bolton Hunter CCK-8 binding from the interpeduncular nucleus (IPN) (IC50 = 7 X 10(-8) M), the area postrema (AP), and the nucleus tractus solitarius (NTS) without influencing specific binding to other areas, such as the cerebral cortex or the spinal tract of the trigeminal nerve [1].
  • The effects of the selective CCK-A antagonist L-365,031 and the selective CCK-B antagonist L-365,260 on morphine analgesia and opiate tolerance and dependence in rats were examined [2].
  • In both rat and mouse, 125I-Bolton Hunter CCK binding in the region of the interpeduncular nucleus (IPN) was inhibited by L-365,031 indicating that these receptors resemble CCK receptors found in peripheral tissues [3].
  • Similarly, L-365,031, a specific, but less potent, CCKA antagonist, also produced a profile consistent with weak anxiolysis but only at 5 micrograms/kg [4].


  1. Autoradiographic localization and biochemical characterization of peripheral type CCK receptors in rat CNS using highly selective nonpeptide CCK antagonists. Hill, D.R., Campbell, N.J., Shaw, T.M., Woodruff, G.N. J. Neurosci. (1987) [Pubmed]
  2. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Dourish, C.T., O'Neill, M.F., Coughlan, J., Kitchener, S.J., Hawley, D., Iversen, S.D. Eur. J. Pharmacol. (1990) [Pubmed]
  3. Species differences in the localization of 'peripheral' type cholecystokinin receptors in rodent brain. Hill, D.R., Shaw, T.M., Woodruff, G.N. Neurosci. Lett. (1987) [Pubmed]
  4. The effects of CCKA and CCKB antagonists on activity in the black/white exploration model of anxiety in mice. Hendrie, C.A., Neill, J.C., Shepherd, J.K., Dourish, C.T. Physiol. Behav. (1993) [Pubmed]
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