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Volumn 18, Issue 12, 2008, Pages 3611-3615

Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor: In vitro and in vivo activity

Author keywords

7; Azabicyclic; nAChR; Nicotinic; PHA 543613; PHA 709829; Schizophrenia

Indexed keywords

AMPHETAMINE; BENZOTHIAZOLE; BUNGAROTOXIN RECEPTOR; CHLOROBENZAMIDE; FUROPYRIDINE; N [1 AZABICYCLO[3.2.1]OCT 3 YL]FURO[2,3 C]PYRIDINE 5 CARBOXAMIDE; NICOTINIC AGENT; PHA 543613; PHA 709829; PNU 282987; PYRIDINE DERIVATIVE; PYRROLOPYRIMIDINE; THIENOPYRIDINE;

EID: 44649098133     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.04.070     Document Type: Article
Times cited : (65)

References (31)
  • 1
  • 13
    • 44649185267 scopus 로고    scopus 로고
    • Rogers, B. N., Society for Neuroscience Annual Meeting, Satellite Meeting on Nicotinic Acetylcholine Receptors as Therapeutic Targets: Emerging Frontiers in Basic Research & Clinical Science, San Diego, CA, 2007.
    • Rogers, B. N., Society for Neuroscience Annual Meeting, Satellite Meeting on Nicotinic Acetylcholine Receptors as Therapeutic Targets: Emerging Frontiers in Basic Research & Clinical Science, San Diego, CA, 2007.
  • 18
    • 44649158617 scopus 로고    scopus 로고
    • note
    • 2O: C, 55.50; H, 6.02; N, 12.95. Found: C, 55.76; H, 5.80; N, 12.85.
  • 21
    • 44649129727 scopus 로고    scopus 로고
    • note
    • Doses are reported in free base equivalents.
  • 23
    • 44649110529 scopus 로고    scopus 로고
    • note
    • Compound 3a was screened against a panel of 90 receptors, channels and enzymes at CEREP and found to have no additional activities.
  • 25
    • 44649138919 scopus 로고    scopus 로고
    • note
    • Compounds screened in Chan Test, hERG Block Comparitor Screen.
  • 26
    • 44649131008 scopus 로고    scopus 로고
    • note
    • The aqueous solubility of compounds 3a and PHA-543613 is greater than 100 mg/mL (HPLC method in pH 7 buffer); thus, solubility should not complicate the results of the hERG assay, which were determined at a concentration of 20 μM.
  • 29
    • 44649101076 scopus 로고    scopus 로고
    • Hajos, M.; Krause, M.; Hoffmann, W. E.; Hajos-Korcsok, E.; Yu, J. H.; Robinson, D. D.; Wall, T. M.; Higdon, N. R.; Svensson, K. A.; Nichols, N. F.; Walters, R. R.; Groppi, V. E.; Arneric, S. P.; Hurst, R. S. Abstract of Papers, 37th Society for Neuroscience, San Diego, CA, 2007; Abstract 60.9/V17.2007.
    • Hajos, M.; Krause, M.; Hoffmann, W. E.; Hajos-Korcsok, E.; Yu, J. H.; Robinson, D. D.; Wall, T. M.; Higdon, N. R.; Svensson, K. A.; Nichols, N. F.; Walters, R. R.; Groppi, V. E.; Arneric, S. P.; Hurst, R. S. Abstract of Papers, 37th Society for Neuroscience, San Diego, CA, 2007; Abstract 60.9/V17.2007.
  • 30
    • 44649125727 scopus 로고    scopus 로고
    • note
    • It is worth noting that since PHA-543613 and PHA-709829 possess essentially equal affinity for the human α7 nAChR (7 nM vs. 9 nM), it is not known whether the improved efficacy of PHA-709829 in the rat auditory gating assay will translate to humans.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.