AR-A000002

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]

AR-A000002
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • (R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC27H36N4O2
Molar mass448.611 g·mol−1
3D model (JSmol)
SMILES
  • C5COCCN5c(cc4)ccc4C(=O)NC2CCc1c(C2)c(ccc1C)N3CCN(C)CC3
InChI
  • 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)

References
  1. Hudzik TJ, Yanek M, Porrey T, Evenden J, Paronis C, Mastrangelo M, et al. (March 2003). "Behavioral pharmacology of AR-A000002, a novel, selective 5-hydroxytryptamine(1B) antagonist". The Journal of Pharmacology and Experimental Therapeutics. 304 (3): 1072–84. doi:10.1124/jpet.102.045468. PMID 12604684. S2CID 20463714.
  2. Ahlgren C, Eriksson A, Tellefors P, Ross SB, Stenfors C, Malmberg A (September 2004). "In vitro characterization of AR-A000002, a novel 5-hydroxytryptamine(1B) autoreceptor antagonist". European Journal of Pharmacology. 499 (1–2): 67–75. doi:10.1016/j.ejphar.2004.07.067. PMID 15363952.
  3. Stenfors C, Ahlgren C, Yu H, Wedén M, Larsson LG, Ross SB (March 2004). "Effects of long-term administration of the 5-hydroxytryptamine1B receptor antagonist AR-A000002 to guinea pigs". Psychopharmacology. 172 (3): 333–40. doi:10.1007/s00213-003-1667-8. PMID 14652708. S2CID 25130658.
  4. Stenfors C, Hallerbäck T, Larsson LG, Wallsten C, Ross SB (March 2004). "Pharmacology of a novel selective 5-hydroxytryptamine1B receptor antagonist, AR-A000002". Naunyn-Schmiedeberg's Archives of Pharmacology. 369 (3): 330–7. doi:10.1007/s00210-004-0866-0. PMID 14758468. S2CID 21075322.
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