AR-A000002

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AR-A000002
AR-A000002 structure.png
Systematic (IUPAC) name
(R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide
Identifiers
ATC code none
PubChem CID: 9846516
ChemSpider 8022230
Chemical data
Formula C27H36N4O2
Molecular mass 448.599 g/mol
  • C5COCCN5c(cc4)ccc4C(=O)NC2CCc1c(C2)c(ccc1C)N3CCN(C)CC3
  • InChI=1S/C27H36N4O2/c1-20-3-10-26(31-13-11-29(2)12-14-31)25-19-22(6-9-24(20)25)28-27(32)21-4-7-23(8-5-21)30-15-17-33-18-16-30/h3-5,7-8,10,22H,6,9,11-19H2,1-2H3,(H,28,32)/t22-/m1/s1
  • Key:IHDRUIHIJWCTIY-JOCHJYFZSA-N
  (verify)

AR-A000002 is a drug which is one of the first compounds developed to act as a selective antagonist for the serotonin receptor 5-HT1B,[1] with approximately 10x selectivity for 5-HT1B over the closely related 5-HT1D receptor.[2] It has been shown to produce sustained increases in levels of serotonin in the brain, and has anxiolytic effects in animal studies.[3][4]

References

  1. ↑ Hudzik TJ, Yanek M, Porrey T, Evenden J, Paronis C, Mastrangelo M, Ryan C, Ross S, Stenfors C. Behavioral pharmacology of AR-A000002, a novel, selective 5-hydroxytryptamine(1B) antagonist. Journal of Pharmacology and Experimental Therapeutics. 2003 Mar;304(3):1072-84. PMID 12604684
  2. ↑ Ahlgren C, Eriksson A, Tellefors P, Ross SB, Stenfors C, Malmberg A. In vitro characterization of AR-A000002, a novel 5-hydroxytryptamine(1B) autoreceptor antagonist. European Journal of Pharmacology. 2004 Sep 19;499(1-2):67-75. PMID 15363952
  3. ↑ Stenfors C, Ahlgren C, Yu H, Wedén M, Larsson LG, Ross SB. Effects of long-term administration of the 5-hydroxytryptamine1B receptor antagonist AR-A000002 to guinea pigs. Psychopharmacology (Berlin). 2004 Mar;172(3):333-40. PMID 14652708
  4. ↑ Stenfors C, Hallerbäck T, Larsson LG, Wallsten C, Ross SB. Pharmacology of a novel selective 5-hydroxytryptamine1B receptor antagonist, AR-A000002. Naunyn Schmiedebergs Archives of Pharmacology. 2004 Mar;369(3):330-7. PMID 14758468


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