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 ascocaine.[7][8][9] The drug has been found to have no effect onanxiety in multiple paradigms in rodents.[10] In contrast to other serotonin 5-HT2C receptor antagonists, SER-082 does not producehyperlocomotion in rodents, and instead can producehypolocomotion at high doses that is independent of the serotonin 5-HT2C receptor.[11]
It fails to block the effects ofserotonergic psychedelics in multiple behavioral paradigms, in contrast to serotonin 5-HT2A receptor antagonists.[12][13][14] However, the hypolocomotion induced by high doses of thephenethylamine psychedelicDOI can be attenuated by SER-082.[15] Conversely, the drug was ineffective against the hypolocomotion induced by thetryptamine psychedelic5-MeO-DMT, whereas the serotonin5-HT1A receptor antagonistWAY-100635 was effective.[16]
^Oh SJ, Ha HJ, Chi DY, Lee HK (July 2001). "Serotonin receptor and transporter ligands - current status".Current Medicinal Chemistry.8 (9):999–1034.doi:10.2174/0929867013372599.PMID11472239.
^abNozulak J, Kalkman HO, Floersheim P, Hoyer D, Schoeffter P, Buerki HR (January 1995). "(+)-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.doi:10.1021/jm00001a007.PMID7837236.
^Mora PO, Netto CF, Graeff FG (December 1997). "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.doi:10.1016/S0091-3057(97)00057-9.PMID9408213.S2CID11115355.
^Dave KD, Harvey JA, Aloyo VJ (May 2002). "A novel behavioral model that discriminates between 5-HT2A and 5-HT2C receptor activation".Pharmacology, Biochemistry, and Behavior.72 (1–2):371–378.doi:10.1016/S0091-3057(01)00767-5.PMID11900808.S2CID36921090.
^Hawkins MF, Uzelac SM, Hearn JK, Baumeister AA (October 2008). "Effects of selective serotonin2 ligands on behaviors evoked by stress in the rat".Pharmacology, Biochemistry, and Behavior.90 (4):632–639.doi:10.1016/j.pbb.2008.05.006.PMID18572227.S2CID25959070.
^Filip M, Bubar MJ, Cunningham KA (September 2004). "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.doi:10.1124/jpet.104.068841.PMID15131246.S2CID25809734.
^Filip M (2005). "Role of serotonin (5-HT)2 receptors in cocaine self-administration and seeking behavior in rats".Pharmacological Reports.57 (1):35–46.PMID15849375.
^Filip M, Bubar MJ, Cunningham KA (January 2006). "Contribution of serotonin (5-HT) 5-HT2 receptor subtypes to the discriminative stimulus effects of cocaine in rats".Psychopharmacology.183 (4):482–489.doi:10.1007/s00213-005-0197-y.PMID16261316.S2CID23148827.
^Bourin M, Nic Dhonnchadha BA (2005). "5-HT 2 receptors and anxiety".Drug Development Research.65 (3):133–140.doi:10.1002/ddr.20016.ISSN0272-4391.
^Fletcher PJ, Tampakeras M, Sinyard J, Slassi A, Isaac M, Higgins GA (September 2009). "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.doi:10.1016/j.neuropharm.2009.05.011.PMID19501602.
^Nichols D, Nichols CD (2021)."The Pharmacology of Psychedelics". In Grob C, Grigsby J (eds.).Handbook of Medical Hallucinogens. Guilford Publications. pp. 3–28.ISBN978-1-4625-4544-5. Retrieved17 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).
^Willins DL, Meltzer HY (August 1997). "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.doi:10.1016/S0022-3565(24)36840-5.PMID9262333.
^Krebs-Thomson K, Paulus MP, Geyer MA (May 1998). "Effects of hallucinogens on locomotor and investigatory activity and patterns: influence of 5-HT2A and 5-HT2C receptors".Neuropsychopharmacology.18 (5):339–351.doi:10.1016/S0893-133X(97)00164-4.PMID9536447.
^Krebs-Thomson K, Ruiz EM, Masten V, Buell M, Geyer MA (December 2006). "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.doi:10.1007/s00213-006-0566-1.PMID17013638.
