Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 6, 2009, Pages 1729-1732

  Malik, Leila ^a   Kelly, Nicholas M ^a   Ma, Jian Nong ^b   Currier, Erika A ^b   Burstein, Ethan S ^b   Olsson, Roger ^a  

^a ACADIA Pharmaceuticals AB   (Sweden)

^b ACADIA PHARMACEUTICALS INC   (United States)

Author keywords

Agonist; Mas related; MrgX1; MrgX2; Nociception; Non peptidergic; R SAT; Sensory neuron specific receptors; Small molecule; SNSR; Solid phase

Indexed keywords

BAM22 PEPTIDE; BENZIMIDAZOLE DERIVATIVE; CORTICOSTATIN; CORTICOSTATIN 14; MRGX1 RECEPTOR AGONIST; MRGX2 RECEPTOR AGONIST; PEPTIDE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; SOLID PHASE SYNTHESIS; STRUCTURE ACTIVITY RELATION;

ANIMALS; BENZIMIDAZOLES; CATTLE; CHEMISTRY, PHARMACEUTICAL; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG DESIGN; HUMANS; LIGANDS; MACACA MULATTA; MODELS, CHEMICAL; NERVE TISSUE PROTEINS; PEPTIDES; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NEUROPEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

MACACA MULATTA;

EID: 61349141397     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.085     Document Type: Article

References (12)

1. Dong X., Han S., Zylka M.J., Simon M.I., and Anderson D.J. Cell 106 (2001) 619
2. Lembo P.M., Grazzini E., Groblewski T., O'Donnell D., Roy M.O., Zhang J., Hoffert C., Cao J., Schmidt R., Pelletier M., Labarre M., Gosselin M., Fortin Y., Banville D., Shen S.H., Strom P., Payza K., Dray A., Walker P., and Ahmad S. Nat. Neurosci. 5 (2002) 201
3. Robas N., Mead E., and Fidock M. J. Biol. Chem. 278 (2003) 44400
4. Spier A.D., and De Lecea L. Brain Res. Rev. 33 (2000) 228
5. Kamohara M., Matsuo A., Takasaki J., Kohda M., Matsumoto M., Matsumoto S., Soga T., Hiyama H., Kobori M., and Katou M. Biochem. Biophys. Res. Commun. 20 (2005) 1146
6. Chen H., and Ikeda S.R. J. Neurosci. 26 (2004) 5044
7. Burstein E.S., Ott T.R., Feddock M., Ma J.N., Fuhs S., Wong S., Schiffer H.H., Brann M.R., and Nash N.R. Br. J. Pharmacol. 147 (2006) 73
8. Zhang L., Taylor N., Xie Y., Ford R., Johnson J., Paulsen J.E., and Bates B. Mol. Brain. Res. 133 (2005) 187
9. Kunapuli P., Lee S., Zheng W., Alberts M., Kornienko O., Mull R., Kreamer A., Hwang J.I., Simon M.I., and Strulovici B. Anal. Biochem. 351 (2006) 50
10. Burstein E.S., Piu F., Ma J.N., Weissman J.T., Currier E.A., Nash N.R., Weiner D.M., Spalding T.A., Schiffer H.H., Del Tredici A.L., and Brann M.R. Curr. Pharm. Des. 12 (2006) 1717
11. Lang, H.; Pei, Y. W.O. Patent 2001,023,392, 2001; Chem Abstr. 2001, 247, 341.
12. Result not shown.