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AR-A000002

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
AR-A000002
Clinical data
Other namesAZD-8129; AZD8129
ATC code
  • none
Identifiers
  • (R)-N-[5-methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydro-2-naphthyl]-4-morpholinobenzamide
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC27H36N4O2
Molar mass448.611 g·mol−1
3D model (JSmol)
  • 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, also known asAZD-8129, is adrug which is one of the first compounds developed to act as aselectiveantagonist for theserotonin receptor5-HT1B,[1] with approximately 10x selectivity for 5-HT1B over the closely related5-HT1D receptor.[2][3] It has been shown to produce sustained increases in levels of serotonin in the brain, and hasanxiolytic effects in animal studies.[4][5]

See also

[edit]

References

[edit]
  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. ^"AZD 8129".AdisInsight. 18 August 2005. Retrieved11 December 2024.
  4. ^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.
  5. ^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.
5-HT1ARTooltip 5-HT1A receptoragonists
GABAARTooltip GABAA receptorPAMsTooltip positive allosteric modulators
Gabapentinoids
(α2δVDCCblockers)
Antidepressants
Sympatholytics
(Antiadrenergics)
Others
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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