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Chemical Compound Review:

CHEMBL473186 4-(4-fluoronaphthalen-1-yl)- 6-propan-2-yl...

Synonyms: SureCN375979, CHEBI:559270, BCPP000085, RS-127445, MT 500, ...

Bonhaus, D.W. et al., Kimura, Y. et al., Knight, A.R. et al., Mucke, H.A.

Kimura, Hatanaka, Naitou, Maeno, Shimada, Koakutsu, Wanibuchi, Yamaguchi, Knight, Misra, Quirk, Benwell, Revell, Kennett, Bickerdike, Bonhaus, Flippin, Greenhouse, Jaime, Rocha, Dawson, Van Natta, Chang, Pulido-Rios, Webber, Leung, Eglen, Martin, Mucke,

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Disease relevance of MT 500

POZEN acquired MT-500 from Roche in November 1999, and assumed full responsibility for its development for migraine propylaxis [1].

High impact information on MT 500

In conclusion, RS-127445 is a selective, high affinity 5-HT2B receptor antagonist suitable for use is vivo [2].
These studies confirmed that there are a number of highly selective antagonists available to investigate 5-HT2 receptor subtype function (for example, MDL 100907, RS-127445 and RS-102221 for 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors respectively) [3].
A selective 5-HT(2A) receptor antagonist, MDL100907 (R(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenylethyl)]-4-piperidine-methanol), and a selective 5-HT(2B) receptor antagonist, RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine), had no effect on the decline in penile erection frequency at 2.03 mg/kg of YM348 [4].

Biological context of MT 500

RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites [2].

References

MT-500 (POZEN). Mucke, H.A. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Bonhaus, D.W., Flippin, L.A., Greenhouse, R.J., Jaime, S., Rocha, C., Dawson, M., Van Natta, K., Chang, L.K., Pulido-Rios, T., Webber, A., Leung, E., Eglen, R.M., Martin, G.R. Br. J. Pharmacol. (1999) [Pubmed]
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Knight, A.R., Misra, A., Quirk, K., Benwell, K., Revell, D., Kennett, G., Bickerdike, M. Naunyn Schmiedebergs Arch. Pharmacol. (2004) [Pubmed]
Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. Kimura, Y., Hatanaka, K., Naitou, Y., Maeno, K., Shimada, I., Koakutsu, A., Wanibuchi, F., Yamaguchi, T. Eur. J. Pharmacol. (2004) [Pubmed]

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