Article · Wikipedia archive · Last revised Jul 4, 2026

FR260010

FR260010 is a selective serotonin 5-HT2C receptor antagonist which was under development for the treatment of anxiety disorders but was never marketed. It is taken orally.

Last revised
Jul 4, 2026
Read time
≈ 1 min
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319 w
Citations
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Wikipedia ↗
FR260010
Clinical data
Other namesFR-260010
Routes of
administration		Oral12
Drug classSerotonin 5-HT2C receptor antagonist
ATC code
  • None
Identifiers
  • N-[3-(4-methylimidazol-1-yl)phenyl]-5,6-dihydrobenzo[h]quinazolin-4-amine
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC22H19N5
Molar mass353.429 g·mol−1
3D model (JSmol)
  • CC1=CN(C=N1)C2=CC=CC(=C2)NC3=NC=NC4=C3CCC5=CC=CC=C54
  • InChI=1S/C22H19N5/c1-15-12-27(14-25-15)18-7-4-6-17(11-18)26-22-20-10-9-16-5-2-3-8-19(16)21(20)23-13-24-22/h2-8,11-14H,9-10H2,1H3,(H,23,24,26)
  • Key:LFKNMCJSJZOQJF-UHFFFAOYSA-N

FR260010 is a selective serotonin 5-HT2C receptor antagonist which was under development for the treatment of anxiety disorders but was never marketed.1324 It is taken orally.12

The drug shows high affinity for the serotonin 5-HT2C receptor (Ki = 1.1 nM) and high selectivity over the serotonin 5-HT2A receptor (Ki = 386 nM) and many other targets.2 Similarly, it shows little affinity for the serotonin 5-HT2B receptor.2 FR260010 is a silent antagonist of the serotonin 5-HT2C receptor.2 It blocks the hypolocomotion and hypophagia induced by the serotonin 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) in rodents.2 Similarly to diazepam, the drug produces anxiolytic-like effects in multiple different animal models of anxiety, whereas buspirone was ineffective in the same models.24 In contrast to diazepam but similarly to buspirone, FR260010 has modest adverse effect-like properties in rodents.2

FR260010 was under development by Astellas Pharma.13 It was first described in the scientific literature by 2006.24 No recent development has been reported as of 2016.1 It reached the discovery stage of development prior to its discontinuation.3

See also

See also

References

References

  1. "Research programme: CNS disorders therapeutics (ASP5854; FR 194921; FR 260010)". AdisInsight. 16 July 2016. Retrieved 18 January 2026.
  2. Harada K, Aota M, Inoue T, Matsuda R, Mihara T, Yamaji T, et al. (December 2006). "Anxiolytic activity of a novel potent serotonin 5-HT2C receptor antagonist FR260010: a comparison with diazepam and buspirone". European Journal of Pharmacology. 553 (1–3): 171–184. doi:10.1016/j.ejphar.2006.09.042. PMID 17074317.
  3. "Delving into the Latest Updates on FR-260010 with Synapse". Synapse. 17 January 2026. Retrieved 18 January 2026.
  4. Harada K, Yamaji T, Matsuoka N (March 2008). "Activation of the serotonin 5-HT2C receptor is involved in the enhanced anxiety in rats after single-prolonged stress". Pharmacology, Biochemistry, and Behavior. 89 (1): 11–16. doi:10.1016/j.pbb.2007.10.016. PMID 18067955.