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Volumn 21, Issue 8, 2011, Pages 2484-2488

Potential CRF1R PET imaging agents: N-Fluoroalkyl-8-(6-methoxy- 2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines

Author keywords

Anxiety; Corticotropin releasing factor; Depression; Imaging agents; Positron emission tomography

Indexed keywords

ALKYL GROUP; AMINE; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; FLUORENE DERIVATIVE; OCTANOL; PHOSPHATE; PYRAZOLE DERIVATIVE; PYRIDINE DERIVATIVE; TRIAZINE DERIVATIVE; CORTICOTROPIN RELEASING FACTOR RECEPTOR; CRF RECEPTOR TYPE 1; DIAGNOSTIC AGENT;

EID: 79953278002     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.050     Document Type: Article
Times cited : (14)

References (26)
  • 16
    • 79953279095 scopus 로고    scopus 로고
    • Gilligan, P. J. 4-(2-Butylamino)-2,7-dimethyl-8-(2-methyl-6-methoxypyrid- 3-yl)[1,5-a]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as a corticotropin releasing factor Receptor ligands, US 7157578 B2 (2007)
    • Gilligan, P. J. 4-(2-Butylamino)-2,7-dimethyl-8-(2-methyl-6-methoxypyrid- 3-yl)[1,5-a]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as a corticotropin releasing factor Receptor ligands, US 7157578 B2 (2007).
  • 17
    • 79953283762 scopus 로고    scopus 로고
    • 2O (10%)/TFA (0.1%); starting% B, 0; final% B, 100; flow rate 5 mL/min; gradient time, 2 min; end time, 3 min.
    • 2O (10%)/TFA (0.1%); starting% B, 0; final% B, 100; flow rate 5 mL/min; gradient time, 2 min; end time, 3 min.
  • 19
    • 79953268191 scopus 로고    scopus 로고
    • note
    • 125I-o-CRF (2200 Ci/mmol) was obtained from PerkinElmer Life Sciences, Inc. (Boston, MA).
  • 20
    • 79953274056 scopus 로고    scopus 로고
    • note
    • Shake-flask log D determination assay for lipophilicity: In a 250 mL separatory funnel were added 25 mM phosphate buffer (200 mL) and octanol (10 mL). The two-phase system was mixed well and let stand overnight to allow complete saturation and separation of both layers. A sample (1.0 mg) was dissolved in octanol (1 mL) and transferred to a volumetric flask, containing 50 mL of the phosphate buffer, saturated with octanol, as described above. The resulting mixture was shaken intensely for 30-40 min and was allowed to stand until two layers separated completely. A sample of each layer was analyzed by an HPLC method twice. The sample area counts were used to calculate the shake-flask log D.
  • 21
    • 79953280243 scopus 로고    scopus 로고
    • note
    • +).
  • 22
    • 79953292773 scopus 로고    scopus 로고
    • note
    • 2O (10%)/TFA (0.1%); starting% B, 30; final% B, 100; flow rate 25 mL/min; gradient time, 20 min; end time, 25 min.
  • 24
    • 79953286916 scopus 로고    scopus 로고
    • The X-ray crystal structure of 18 was deposited with Cambridge Crystallographic Data Centre (deposition number - CCDC 810575)
    • The X-ray crystal structure of 18 was deposited with Cambridge Crystallographic Data Centre (deposition number - CCDC 810575).
  • 26
    • 79953275376 scopus 로고    scopus 로고
    • The log D values of compounds 1-6 had not been reported and, therefore, were unavailable for comparison with the log D value of 7e
    • The log D values of compounds 1-6 had not been reported and, therefore, were unavailable for comparison with the log D value of 7e.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.