FR260010

Last updated

FR260010
Clinical data
Other namesFR-260010
Routes of
administration 		Oral [1] [2]
Drug class Serotonin 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
Formula C22H19N5
Molar mass 353.429 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. [1] [3] [2] [4] It is taken orally. [1] [2]

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. [2] [4] 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. [1] [3] It was first described in the scientific literature by 2006. [2] [4] No recent development has been reported as of 2016. [1] It reached the discovery stage of development prior to its discontinuation. [3]

See also

References

  1. 1 2 3 4 5 "Research programme: CNS disorders therapeutics (ASP5854; FR 194921; FR 260010)". AdisInsight. 16 July 2016. Retrieved 18 January 2026.
  2. 1 2 3 4 5 6 7 8 9 10 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. 1 2 3 "Delving into the Latest Updates on FR-260010 with Synapse". Synapse. 17 January 2026. Retrieved 18 January 2026.
  4. 1 2 3 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.
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