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]
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| Other names | R102444; R-102,444; R-96544 prodrug |
| Routes of administration | Unspecified[1] |
| Drug class | Serotonin 5-HT2 receptor antagonist; Serotonin 5-HT2A receptor antagonist |
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| Formula | C34H51NO4 |
| Molar mass | 537.785 g·mol−1 |
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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
editReferences
edit- 1 2 3 4 "R 102444". AdisInsight. 13 May 2008. Retrieved 22 April 2026.
- 1 2 3 "Delving into the Latest Updates on R-102444 with Synapse". Synapse. 10 January 2026. Retrieved 22 April 2026.
- 1 2 3 4 Tanaka N, Goto R, Ito R, Hayakawa M, Sugidachi A, Ogawa T, et al. (November 2000). "[2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2)". Chemical & Pharmaceutical Bulletin. 48 (11). Tokyo: 1729–1739. doi:10.1248/cpb.48.1729. PMID 11086903.
- 1 2 3 4 Ogawa T, Sugidachi A, Tanaka N, Fujimoto K, Asai F (December 2002). "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. doi:10.1016/s0014-2999(02)02654-7. PMID 12464356.
- 1 2 3 Ogawa T, Sugidachi A, Tanaka N, Fujimoto K, Asai F (February 2004). "Effects of R-102444, an orally active 5-HT2A receptor antagonist, in rat models of peripheral vascular disease". Vascular Pharmacology. 41 (1): 7–13. doi:10.1016/j.vph.2004.03.001. PMID 15135326.
- ↑ Ogawa T, Sugidachi A, Tanaka N, Fujimoto K, Fukushige J, Tani Y, et al. (October 2005). "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. doi:10.1016/j.ejphar.2005.08.033. PMID 16183055.