A-349,821

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A-349,821
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Systematic (IUPAC) name
(4'-[3-(2R,5R-dimethylpyrrolidin-1-yl)propoxy]biphenyl-4-yl)morpholin-4-ylmethanone
Identifiers
PubChem CID 9954017
IUPHAR/BPS 1217
Chemical data
Formula C26H34N2O3
Molar mass 422.558[[Script error: No such module "String".]]
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A-349,821 is a potent and selective histamine H3 receptor antagonist[1] (or possibly an inverse agonist).[2] It has nootropic effects in animal studies,[3] although there do not appear to be any plans for clinical development at present and it is currently only used in laboratory research.

References

  1. Faghih R, Dwight W, Pan JB, Fox GB, Krueger KM, Esbenshade TA, McVey JM, Marsh K, Bennani YL, Hancock AA. Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters. 2003 Apr 7;13(7):1325-8. PMID 12657274
  2. Witte DG, Yao BB, Miller TR, Carr TL, Cassar S, Sharma R, Faghih R, Surber BW, Esbenshade TA, Hancock AA, Krueger KM. Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand. British Journal of Pharmacology. 2006 Jul;148(5):657-70. PMID 16715122
  3. Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA. Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochemical Pharmacology. 2004 Sep 1;68(5):933-45. PMID 15294456