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Chemical Compound Review:

CHEMBL34291 4-amino-5-chloro-N-[[(1S,8S)- 2,3,5,6,7,8...

Synonyms: SureCN678624, SC-53116, DNC012754, PDSP2_001604, SC53116, ...

McLean, P.G. et al., McLean, P.G. et al., Eglen, R.M. et al., Varanasi, S. et al., Matsumoto, M. et al.

Matsumoto, Togashi, Mori, Ueno , Ohashi, Kojima, Yoshioka,

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High impact information on SC-53116

SC 53116 (10 microg/rat i.c.v.) also augmented the tetanus-induced long-term potentiation (LTP) [1].
SC 53116 showed no agonist activity in the rat ileum and human colon, but at 1 microM it did antagonize the effect of 5-HT in the human colon with a dose-ratio of 11.3 +/- 0.3.(ABSTRACT TRUNCATED AT 400 WORDS)[2]
1. The pharmacological properties of 5-hydroxytryptamine (5-HT), the 5-HT4 receptor agonists, DAU 6236 and SC 53116 and the 5-HT4 receptor antagonist, GR 1130808, were studied in the rat oesophagus, rat ileum and human colon [2].
Affinity estimates (-log KB) at 5-HT4 receptors using either renzapride or SC-53116 as agonists yielded a -log KB value of 8.0 +/- 0.01 [3].

Anatomical context of SC-53116

Moreover, coinjection of SC-53116 (5-HT4 agonist) decreased the gastric acid output by 45% compared with the RX response itself [4].
The 5-HT4 agonist SC 53116 induced antiabsorptive effects in both regions of the small intestine, but DAU 6236 did not affect the rates of fluid transport [5].

Associations of SC-53116 with other chemical compounds

4. The compounds, DAU 6236 and SC 53116, showed a different pattern of potencies and efficacies in the rat oesophagus, rat ileum and human colon compared to 5-HT [2].

References

Evidence for involvement of central 5-HT(4) receptors in cholinergic function associated with cognitive processes: behavioral, electrophysiological, and neurochemical studies. Matsumoto, M., Togashi, H., Mori, K., Ueno , K., Ohashi, S., Kojima, T., Yoshioka, M. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
A comparative study of functional 5-HT4 receptors in human colon, rat oesophagus and rat ileum. McLean, P.G., Coupar, I.M., Molenaar, P. Br. J. Pharmacol. (1995) [Pubmed]
RS 23597-190: a potent and selective 5-HT4 receptor antagonist. Eglen, R.M., Bley, K., Bonhaus, D.W., Clark, R.D., Hegde, S.S., Johnson, L.G., Leung, E., Wong, E.H. Br. J. Pharmacol. (1993) [Pubmed]
5-CT or DOI augments TRH analog-induced gastric acid secretion at the dorsal vagal complex. Varanasi, S., Chi, J., Stephens, R.L. Am. J. Physiol. (1997) [Pubmed]
Investigation into the effect of 5-hydroxytryptamine on fluid transport in the rat small intestine. McLean, P.G., Coupar, I.M. Gen. Pharmacol. (1998) [Pubmed]

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