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Seganserin

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Seganserin
Clinical data
Other namesR-56413; R56413
Drug classSerotonin 5-HT2 receptor antagonist; Serotonin 5-HT2A receptor antagonist
ATC code
  • None
Pharmacokinetic data
Onset of actionTmaxTooltip Time to peak levels: 1 hour[1]
Elimination half-life26 hours[1]
Identifiers
  • 3-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC29H27F2N3O
Molar mass471.552 g·mol−1
3D model (JSmol)
  • CC1=C(C(=O)N2C=CC=CC2=N1)CCN3CCC(=C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)CC3
  • InChI=1S/C29H27F2N3O/c1-20-26(29(35)34-16-3-2-4-27(34)32-20)15-19-33-17-13-23(14-18-33)28(21-5-9-24(30)10-6-21)22-7-11-25(31)12-8-22/h2-12,16H,13-15,17-19H2,1H3
  • Key:ZGUPMFYFHHSNFK-UHFFFAOYSA-N

Seganserin (INNTooltip International Nonproprietary Name, BANTooltip British Approved Name; developmental code name R-56413) is a selective serotonin 5-HT2 receptor antagonist which was studied for the treatment of insomnia and anxiety but was never marketed.[2][3][1][4][5][6] It acts as a dual serotonin 5-HT2A and 5-HT2C receptor antagonist.[3][4] The drug blocks the head-twitch response induced by serotonin precursor 5-hydroxytryptophan (5-HTP) and the psychedelic drug mescaline in rodents.[7] It has been found to enhance slow wave sleep (SWS) in clinical studies.[3][4][5][8][1] The drug's time to peak levels is 1 hour and its elimination half-life is 26 hours.[1] Seganserin reached phase 2 clinical trials prior to the discontinuation of its development.[2] It was first described in the scientific literature by 1985.[9][10]

See also

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References

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  1. ^ a b c d e Dijk DJ, Beersma DG, Daan S, van den Hoofdakker RH (November 1989). "Effects of seganserin, a 5-HT2 antagonist, and temazepam on human sleep stages and EEG power spectra". Eur J Pharmacol. 171 (2–3): 207–218. doi:10.1016/0014-2999(89)90109-x. PMID 2576000. Seganserin (R56413, Janssen Pharmaceutica, N.V.) is a highly specific 5HT 2 antagonist devoid of dopaminergic activity (Kennis et al., 1986). The plasma half-life is 26.1 ± 12.9 (S.D.) h. After oral administration maximal plasma levels are reached after 1.0 + 0.5 h (Van de Velde et al., 1986).
  2. ^ a b Baxter G, Kennett G, Blaney F, Blackburn T (March 1995). "5-HT2 receptor subtypes: a family re-united?". Trends Pharmacol Sci. 16 (3): 105–110. doi:10.1016/s0165-6147(00)88991-9. PMID 7792930.
  3. ^ a b c Monti, J.M. (2010). "Serotonin 5-HT2A receptor antagonists in the treatment of insomnia: present status and future prospects". Drugs of Today. 46 (3): 183. doi:10.1358/dot.2010.46.3.1437247. Retrieved 16 January 2026.
  4. ^ a b c Landolt HP, Wehrle R (May 2009). "Antagonism of serotonergic 5-HT2A/2C receptors: mutual improvement of sleep, cognition and mood?". Eur J Neurosci. 29 (9): 1795–1809. doi:10.1111/j.1460-9568.2009.06718.x. PMID 19473234.
  5. ^ a b Monti, Jaime M.; Torterolo, Pablo; Spence, David Warren; Pandi-Perumal, Seithikurippu R. (6 November 2017). "Selective Serotonin 5-HT2A Receptor Antagonists and Inverse Agonists Specifically Promote Slow Wave Sleep (Stage N3) in Man". Sleep and Vigilance. 2 (1): 23–31. doi:10.1007/s41782-017-0024-7. ISSN 2510-2265. Retrieved 16 January 2026.
  6. ^ Kennis, Ludo E. J.; Vandenberk, Jan; Boey, Jozef M.; Mertens, Jos C.; van Heertum, Albert H. M.; Janssen, Marcel; Awouters, Frans (1986). "The chemical development of selective and specific serotonin S 2 ‐antagonists". Drug Development Research. 8 (1–4): 133–140. doi:10.1002/ddr.430080116. ISSN 0272-4391. Retrieved 16 January 2026.
  7. ^ Meert, Theo F.; Niemegeers, Carlos J. E.; Awouters, Frans; Janssen, Paul A. J. (1988). "Partial and complete blockade of 5‐hydroxytrytophan (5‐HTP)‐induced head twitches in the rat: A study of ritanserin (R 55 667), risperidone (R 64 766), and related compounds". Drug Development Research. 13 (4): 237–244. doi:10.1002/ddr.430130406. ISSN 0272-4391. Retrieved 16 January 2026.
  8. ^ Dijk DJ (June 2010). "Slow-wave sleep deficiency and enhancement: implications for insomnia and its management". World J Biol Psychiatry. 11 Suppl 1: 22–28. doi:10.3109/15622971003637645. PMID 20509829.
  9. ^ Janssen PA (1985). "Pharmacology of potent and selective S2-serotonergic antagonists". J Cardiovasc Pharmacol. 7 Suppl 7: S2–11. doi:10.1097/00005344-198500077-00002. PMID 2412048.
  10. ^ Critchley MA, Handley SL (1987). "Effects in the X-maze anxiety model of agents acting at 5-HT1 and 5-HT2 receptors". Psychopharmacology (Berl). 93 (4): 502–506. doi:10.1007/BF00207243. PMID 3124184.
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