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CGS-12066

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
CGS-12066
Clinical data
Other namesCGS12066; CGS-12066A; CGS12066A; CGS-12066B; CGS12066B
Routes of
administration		Unknown[1]
Drug classSerotonin5-HT1B receptoragonist
ATC code
  • None
Identifiers
  • 4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC17H17F3N4
Molar mass334.346 g·mol−1
3D model (JSmol)
  • CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4
  • InChI=1S/C17H17F3N4/c1-22-7-9-23(10-8-22)16-15-3-2-6-24(15)14-5-4-12(17(18,19)20)11-13(14)21-16/h2-6,11H,7-10H2,1H3
  • Key:LXFHSCDLMBZYKY-UHFFFAOYSA-N

CGS-12066, also known asCGS-12066A andCGS-12066B, is a predominantserotonin5-HT1B receptoragonist which was under development for the treatment ofanxiety disorders but was never marketed.[1][2][3][4] Itsroute of administration is unknown.[1]

In terms ofaffinity, it is moderately (17-fold)selective for the serotonin 5-HT1B receptor over the serotonin5-HT1A receptor, where it is also an agonist.[3][4][5] Although reported to be a selective serotonin 5-HT1B receptor agonist, it was subsequently found to beequipotent as an agonist of the serotonin 5-HT1B and5-HT1D receptors.[6] The drug showed weak affinity for the serotonin5-HT2A,5-HT2B, and5-HT2C receptors (Ki = 871–4,270 nM).[7] It had minimal affinity for variousadrenergic anddopamine receptors.[4][8]

CGS-12066 producesanxiolytic-like,[9][10]prosocial,[11] andantiaggressive effects in rodents.[12][13] There is rapidtolerance to its prosocial effects, thought to be due todesensitization of serotonin 5-HT1B receptors.[11] The drug also produceshyperlocomotion in rodents, although to a much lesser extent thanRU-24969, perhaps due to its lower-efficacypartial agonism of the serotonin 5-HT1B receptor.[14] It produceswakefulness and reducesslow wave sleep (SWS) andrapid eye movement (REM)sleep in rodents.[15][16][17] Some of the effects of CGS-12066 in animals, such ashypothermia andserotonin behavioral syndrome, are not mediated by the serotonin 5-HT1B receptor.[18]

CGS-12066 was first described in thescientific literature by 1987.[4] It reached thepreclinical research stage of development for anxiety disorders prior to the discontinuation of its development in 1995.[1][2]

See also

[edit]

References

[edit]
  1. ^abcd"CGS 12066B".AdisInsight. 24 January 1996. Retrieved19 January 2026.
  2. ^ab"Delving into the Latest Updates on CGS-12066B with Synapse".Synapse. 15 May 2025. Retrieved19 January 2026.
  3. ^abMiddlemiss DN, Hutson PH (1990). "The 5-HT1B receptors".Annals of the New York Academy of Sciences.600:132–47, discussion 347–48.doi:10.1111/j.1749-6632.1990.tb16878.x.PMID 2252306.
  4. ^abcdNeale RF, Fallon SL, Boyar WC, Wasley JW, Martin LL, Stone GA, et al. (April 1987). "Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist".European Journal of Pharmacology.136 (1):1–9.doi:10.1016/0014-2999(87)90772-2.PMID 3496228.
  5. ^Berendsen HH, Broekkamp CL (November 1990)."Behavioural evidence for functional interactions between 5-HT-receptor subtypes in rats and mice".British Journal of Pharmacology.101 (3):667–673.doi:10.1111/j.1476-5381.1990.tb14138.x.PMC 1917735.PMID 2150180.
  6. ^Schoeffter P, Hoyer D (June 1989). "Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist?".Naunyn-Schmiedeberg's Archives of Pharmacology.339 (6):675–683.doi:10.1007/BF00168661.PMID 2770889.
  7. ^Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, et al. (August 2004). "Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors".Naunyn-Schmiedeberg's Archives of Pharmacology.370 (2):114–123.doi:10.1007/s00210-004-0951-4.PMID 15322733.S2CID 8938111.
  8. ^Riva MA, Creese I (July 1989). "Comparison of two putatively selective radioligands for labeling central nervous system beta-adrenergic receptors: inadequacy of [3H]dihydroalprenolol".Molecular Pharmacology.36 (1):201–210.doi:10.1016/S0026-895X(25)09098-4.PMID 2546050.
  9. ^Benjamin D, Lal H, Meyerson LR (1990). "The effects of 5-HT1B characterizing agents in the mouse elevated plus-maze".Life Sciences.47 (3):195–203.doi:10.1016/0024-3205(90)90320-q.PMID 1975081.
  10. ^Rodgers RJ, Cole JC, Cobain MR, Daly P, Doran PJ, Eells JR, et al. (December 1992). "Anxiogenic-like effects of fluprazine and eltoprazine in the mouse elevated plus-maze: profile comparisons with 8-OH-DPAT, CGS 12066B, TFMPP and mCPP".Behavioural Pharmacology.3 (6):621–634.doi:10.1097/00008877-199212000-00009.PMID 11224163.
  11. ^abFrances H, Monier C (June 1991). "Tolerance to the behavioural effect of serotonergic (5-HT1B) agonists in the isolation-induced social behavioural deficit test".Neuropharmacology.30 (6):623–627.doi:10.1016/0028-3908(91)90082-m.PMID 1833660.
  12. ^de Boer SF, Koolhaas JM (December 2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis".European Journal of Pharmacology.526 (1–3):125–139.doi:10.1016/j.ejphar.2005.09.065.PMID 16310183.
  13. ^Bell R, Donaldson C, Gracey D (September 1995). "Differential effects of CGS 12066B and CP-94,253 on murine social and agonistic behaviour".Pharmacology, Biochemistry, and Behavior.52 (1):7–16.doi:10.1016/0091-3057(95)00077-a.PMID 7501681.
  14. ^Cheetham SC, Heal DJ (December 1993)."Evidence that RU 24969-induced locomotor activity in C57/B1/6 mice is specifically mediated by the 5-HT1B receptor".British Journal of Pharmacology.110 (4):1621–1629.doi:10.1111/j.1476-5381.1993.tb14010.x.PMC 2175846.PMID 8306109.
  15. ^Monti JM (August 2011). "Serotonin control of sleep-wake behavior".Sleep Medicine Reviews.15 (4):269–281.doi:10.1016/j.smrv.2010.11.003.PMID 21459634.
  16. ^Monti JM, Jantos H (2008). "The roles of dopamine and serotonin, and of their receptors, in regulating sleep and waking".Serotonin–Dopamine Interaction: Experimental Evidence and Therapeutic Relevance. Progress in Brain Research. Vol. 172. pp. 625–646.doi:10.1016/S0079-6123(08)00929-1.ISBN 978-0-444-53235-0.PMID 18772053.
  17. ^Bjorvatn B, Ursin R (June 1994). "Effects of the selective 5-HT1B agonist, CGS 12066B, on sleep/waking stages and EEG power spectrum in rats".Journal of Sleep Research.3 (2):97–105.doi:10.1111/j.1365-2869.1994.tb00112.x.PMID 10607113.
  18. ^Bjorvatn B, Neckelmann D, Bjørkum AA, Ursin R (October 1996). "Hypothermia and the 5-HT syndrome induced by CGS 12066B independently of 5-HT(1B) receptor activation".Behavioural Pharmacology.7 (5):462–469.PMID 11224442.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Phenylpiperazines
Benzylpiperazines
Naphthylpiperazines
Quinolinylpiperazines
Diphenylalkylpiperazines
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclic-linked piperazines
Others/uncategorized
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