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Chemical Compound Review:

CI988 3-[[(1S)-2-[[(2R)-2-(2...

Synonyms: LS-71358, AC1L33I2, PD 134308, 130404-91-0

This record was replaced with 108187.

Meltzer, L.T. et al., Stepan, V.M. et al., DelValle, J. et al., Powell, K.R. et al., Dasgupta, S. et al.

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High impact information on 3-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propanoyl]amino]-1-phenyl-ethyl]carbamoyl]propanoic acid

Glycine-extended gastrin induced a dose-dependent increase in [3H]thymidine uptake in LoVo (143 +/- 8% versus control at 10(-10) M) and HT 29 (151 +/- 11% versus control at 10(-10) M) cells that was not inhibited by PD 134308 or by a mitogen-activated protein (MAP) or ERK kinase (MEK) inhibitor (PD 98509) [1].
This change was blocked by the CCKB receptor antagonist PD 134308 (50 nM) [2].
Comparison of the effects of the cholecystokinin-B receptor antagonist, PD 134308, and the cholecystokinin-A receptor antagonist, L-364,718, on dopamine neuronal activity in the substantia nigra and ventral tegmental area [3].
The ability of PD 134308 and L-364,718 to alter the apomorphine-induced inhibition of substantia nigra DA neurons was assessed [3].
Neither L-364,718 (0.1-1.6 mg/kg i.v.) nor PD 134308 (0.1-6.4 mg/kg) altered the basal firing rate of substantia nigra or ventral tegmental area DA neurons [3].

Anatomical context of 3-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propanoyl]amino]-1-phenyl-ethyl]carbamoyl]propanoic acid

In D-cells pretreated with high concentrations of gastrin, L-364,718 was able to inhibit the gastrin-resistant fraction of 125I-CCK-8 binding, but the CCK-B/gastrin receptor selective antagonist (PD 134308) was unable to influence this fraction of binding in doses as high as 10(-6) M [4].

Gene context of 3-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propanoyl]amino]-1-phenyl-ethyl]carbamoyl]propanoic acid

PD 134308 produces anxiolytic-like effects in this animal model of anxiety that would suggest potential clinical efficacy in humans of a novel class of compounds with actions at or modulated by cholecystokinin receptors [5].

References

Glycine-extended gastrin exerts growth-promoting effects on human colon cancer cells. Stepan, V.M., Sawada, M., Todisco, A., Dickinson, C.J. Mol. Med. (1999) [Pubmed]
Regulation of dopamine D2 receptor affinity by cholecystokinin octapeptide in fibroblast cells cotransfected with human CCKB and D2L receptor cDNAs. Dasgupta, S., Li, X.M., Jansson, A., Finnman, U.B., Matsui, T., Rinken, A., Arenas, E., Agnati, L.F., Fuxe, K. Brain Res. Mol. Brain Res. (1996) [Pubmed]
Comparison of the effects of the cholecystokinin-B receptor antagonist, PD 134308, and the cholecystokinin-A receptor antagonist, L-364,718, on dopamine neuronal activity in the substantia nigra and ventral tegmental area. Meltzer, L.T., Christoffersen, C.L., Serpa, K.A., Razmpour, A. Synapse (1993) [Pubmed]
Distinct receptors for cholecystokinin and gastrin on canine fundic D-cells. DelValle, J., Chiba, T., Park, J., Yamada, T. Am. J. Physiol. (1993) [Pubmed]
Evaluation of the effects of PD 134308 (CI-988), a CCK-B antagonist, on the punished responding of squirrel monkeys. Powell, K.R., Barrett, J.E. Neuropeptides (1991) [Pubmed]

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