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FR260010

From Wikipedia, the free encyclopedia

Pharmaceutical compound
FR260010
Clinical data
Other namesFR-260010
Routes of
administration		Oral[1][2]
Drug classSerotonin5-HT2C receptorantagonist
ATC code
  • None
Identifiers
  • N-[3-(4-methylimidazol-1-yl)phenyl]-5,6-dihydrobenzo[h]quinazolin-4-amine
CAS Number
PubChemCID
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 aselectiveserotonin5-HT2C receptorantagonist which was under development for the treatment ofanxiety disorders but was never marketed.[1][3][2][4] It is takenorally.[1][2]

The drug shows highaffinity for the serotonin 5-HT2C receptor (Ki = 1.1 nM) and highselectivity over the serotonin5-HT2A receptor (Ki = 386 nM) and many othertargets.[2] Similarly, it shows little affinity for the serotonin5-HT2B receptor.[2] FR260010 is asilent antagonist of the serotonin 5-HT2C receptor.[2] It blocks thehypolocomotion andhypophagia induced by the serotonin 5-HT2C receptor agonistmeta-chlorophenylpiperazine (mCPP) in rodents.[2] Similarly todiazepam, the drug producesanxiolytic-like effects in multiple differentanimal models ofanxiety, whereasbuspirone was ineffective in the same models.[2][4] In contrast to diazepam but similarly to buspirone, FR260010 has modestadverse effect-like properties in rodents.[2]

FR260010 was under development byAstellas Pharma.[1][3] It was first described in thescientific 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

[edit]

References

[edit]
  1. ^abcde"Research programme: CNS disorders therapeutics (ASP5854; FR 194921; FR 260010)".AdisInsight. 16 July 2016. Retrieved18 January 2026.
  2. ^abcdefghijHarada 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. ^abc"Delving into the Latest Updates on FR-260010 with Synapse".Synapse. 17 January 2026. Retrieved18 January 2026.
  4. ^abcHarada 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.
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
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