Chemistry:R-102444

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R-102444 is a serotonin 5-HT2 receptor antagonist which was under development for the treatment of peripheral arterial occlusive disorders and pancreatitis.[1][2][3][4][5][6] It is a laurate (dodecanoate) ester prodrug of R-96544.[3][4][5]

The drug has been found to inhibit serotonin-induced platelet aggregation and to have antithrombotic effects in preclinical research.[3][5] The active form, R-96544, shows selectivity for the serotonin 5-HT2A receptor over other targets, including the serotonin 5-HT1, 5-HT2B, and 5-HT3 receptors as well as the dopamine D2 receptor and adrenergic receptors, among others.[4] However, it also showed high affinity for the serotonin 5-HT2C receptor, which was about 4-fold less than for the serotonin 5-HT2A receptor.[4]

R-102444 was developed by Daiichi Sankyo Company.[1][2] It reached the preclinical research stage of development prior to its discontinuation.[1][2] R-102444 was first described in the scientific literature by Naoki Tanaka and colleagues by 2000.[3]

See also

References

  1. ↑ 1.0 1.1 1.2 "R 102444". 13 May 2008. https://adisinsight.springer.com/drugs/800015510. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on R-102444 with Synapse". 10 January 2026. https://synapse.patsnap.com/drug/b0b12ecbf94e4711bb4b28870820dc9c. 
  3. ↑ 3.0 3.1 3.2 3.3 "[2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2)". Chemical & Pharmaceutical Bulletin (Tokyo) 48 (11): 1729–1739. November 2000. doi:10.1248/cpb.48.1729. PMID 11086903. 
  4. ↑ 4.0 4.1 4.2 4.3 "Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444". European Journal of Pharmacology 457 (2–3): 107–114. December 2002. doi:10.1016/s0014-2999(02)02654-7. PMID 12464356. 
  5. ↑ 5.0 5.1 5.2 "Effects of R-102444, an orally active 5-HT2A receptor antagonist, in rat models of peripheral vascular disease". Vascular Pharmacology 41 (1): 7–13. February 2004. doi:10.1016/j.vph.2004.03.001. PMID 15135326. 
  6. ↑ "Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: Additional evidence for possible involvement of 5-HT2A receptors in the development of experimental pancreatitis". European Journal of Pharmacology 521 (1–3): 156–163. October 2005. doi:10.1016/j.ejphar.2005.08.033. PMID 16183055. 



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