Chemistry:SDZ SER-082

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Short description: Chemical compound

SDZ SER-082
Clinical data
Other namesSDZ SER-082; SDZ SER082
Drug classSelective serotonin 5-HT2B and 5-HT2C receptor antagonist or weak partial agonist
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC15H20N2
Molar mass228.339 g·mol−1
3D model (JSmol)
  (verify)

SER-082, or SDZ SER-082, is a selective serotonin 5-HT2B and 5-HT2C receptor antagonist or weak partial agonist with an ergoline-like structure which is used in scientific research.[1][2][3] It shows similar affinity for the serotonin 5-HT2B and 5-HT2C receptors and has ~40-fold higher affinity for the serotonin 5-HT2C receptor over the closely related serotonin 5-HT2A receptor.[1][3]

Usages

It has been used in animal studies into the behavioural effects of the different 5-HT2 subtypes,[4][5][6] and how they influence the effects of other drugs such as cocaine.[7][8][9] The drug has been found to have no effect on anxiety in multiple paradigms in rodents.[10] In contrast to other serotonin 5-HT2C receptor antagonists, SER-082 does not produce hyperlocomotion in rodents, and instead can produce hypolocomotion at high doses that is independent of the serotonin 5-HT2C receptor.[11]

It fails to block the effects of serotonergic psychedelics in multiple behavioral paradigms, in contrast to serotonin 5-HT2A receptor antagonists.[12][13][14] However, the hypolocomotion induced by high doses of the phenethylamine psychedelic DOI can be attenuated by SER-082.[15] Conversely, the drug was ineffective against the hypolocomotion induced by the tryptamine psychedelic 5-MeO-DMT, whereas the serotonin 5-HT1A receptor antagonist WAY-100635 was effective.[16]

See also

  • Lysergine

References

  1. ↑ 1.0 1.1 "5-HT2A, 5-HT2B and 5-HT2C receptor ligands". Pharmacochemistry Library. 27. Elsevier. 1997. pp. 161–197. doi:10.1016/s0165-7208(97)80013-x. ISBN 978-0-444-82041-9. 
  2. ↑ "Serotonin receptor and transporter ligands - current status". Current Medicinal Chemistry 8 (9): 999–1034. July 2001. doi:10.2174/0929867013372599. PMID 11472239. 
  3. ↑ 3.0 3.1 "(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity". Journal of Medicinal Chemistry 38 (1): 28–33. January 1995. doi:10.1021/jm00001a007. PMID 7837236. 
  4. ↑ "Role of 5-HT2A and 5-HT2C receptor subtypes in the two types of fear generated by the elevated T-maze". Pharmacology, Biochemistry, and Behavior 58 (4): 1051–1057. December 1997. doi:10.1016/S0091-3057(97)00057-9. PMID 9408213. 
  5. ↑ "A novel behavioral model that discriminates between 5-HT2A and 5-HT2C receptor activation". Pharmacology, Biochemistry, and Behavior 72 (1–2): 371–378. May 2002. doi:10.1016/S0091-3057(01)00767-5. PMID 11900808. 
  6. ↑ "Effects of selective serotonin2 ligands on behaviors evoked by stress in the rat". Pharmacology, Biochemistry, and Behavior 90 (4): 632–639. October 2008. doi:10.1016/j.pbb.2008.05.006. PMID 18572227. 
  7. ↑ "Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses". The Journal of Pharmacology and Experimental Therapeutics 310 (3): 1246–1254. September 2004. doi:10.1124/jpet.104.068841. PMID 15131246. 
  8. ↑ "Role of serotonin (5-HT)2 receptors in cocaine self-administration and seeking behavior in rats". Pharmacological Reports 57 (1): 35–46. 2005. PMID 15849375. 
  9. ↑ "Contribution of serotonin (5-HT) 5-HT2 receptor subtypes to the discriminative stimulus effects of cocaine in rats". Psychopharmacology 183 (4): 482–489. January 2006. doi:10.1007/s00213-005-0197-y. PMID 16261316. 
  10. ↑ "5-HT 2 receptors and anxiety". Drug Development Research 65 (3): 133–140. 2005. doi:10.1002/ddr.20016. ISSN 0272-4391. 
  11. ↑ "Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice". Neuropharmacology 57 (3): 259–267. September 2009. doi:10.1016/j.neuropharm.2009.05.011. PMID 19501602. 
  12. ↑ "The Pharmacology of Psychedelics". Handbook of Medical Hallucinogens. Guilford Publications. 2021. pp. 3–28. ISBN 978-1-4625-4544-5. https://books.google.com/books?id=ebb2DwAAQBAJ&pg=PA3. Retrieved 17 January 2025. "M 100907, but not the 5-HT2C/2B antagonist SER-082, can block most of the behavioral effects of DOI in the BPM paradigm, which are therefore likely mediated by activation of 5-HT2A receptors (Krebs-Thomson, Paulus, & Geyer, 1998). [...] Furthermore, 5-HT2B antagonists (e.g., SB 200,646A, SB 206,553, and SER-082) and the selective 5-HT2C antagonist SB 242,084, consistently fail to block the effects of hallucinogens in a variety of behavioral paradigms (Halberstadt et al., 2016; Ouagazzal et al., 2001; Schreiber et al., 1994; Sipes & Geyer, 1995; Smith et al., 1999; Wettstein, Host, & Hitchcock, 1999; Winter, Rice, Amorosi, & Rabin, 2007)." 
  13. ↑ "Direct injection of 5-HT2A receptor agonists into the medial prefrontal cortex produces a head-twitch response in rats". The Journal of Pharmacology and Experimental Therapeutics 282 (2): 699–706. August 1997. doi:10.1016/S0022-3565(24)36840-5. PMID 9262333. 
  14. ↑ "Effects of hallucinogens on locomotor and investigatory activity and patterns: influence of 5-HT2A and 5-HT2C receptors". Neuropsychopharmacology 18 (5): 339–351. May 1998. doi:10.1016/S0893-133X(97)00164-4. PMID 9536447. 
  15. ↑ "5-HT(2A) and 5-HT(2C) receptors exert opposing effects on locomotor activity in mice". Neuropsychopharmacology 34 (8): 1958–1967. July 2009. doi:10.1038/npp.2009.29. PMID 19322172. 
  16. ↑ "The roles of 5-HT1A and 5-HT2 receptors in the effects of 5-MeO-DMT on locomotor activity and prepulse inhibition in rats". Psychopharmacology 189 (3): 319–329. December 2006. doi:10.1007/s00213-006-0566-1. PMID 17013638. 



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