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Volumn 21, Issue 11, 2011, Pages 3399-3403

2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity

(34)  Brown, Dean G a   Maier, Donna L a   Sylvester, Mark A a   Hoerter, Tiffany N a   Menhaji Klotz, Elnaz a   Lasota, Celina C a   Hirata, Lee T a   Wilkins, Deidre E a   Scott, Clay W a   Trivedi, Shephali a   Chen, Tongming a   McCarthy, Dennis J a   MacIag, Carla M a   Sutton, Evelynjeane J a   Cumberledge, Jerry a   Mathisen, Don a   Roberts, John a   Gupta, Anshul a   Liu, Frank a   Elmore, Charles S a   more..


Author keywords

Anti depressant; NMDA antagonist; NR2B

Indexed keywords

2,6 DISUBSTITUTED PYRAZINE; AMINE; DIZOCILPINE; IFENPRODIL; IMIPRAMINE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; PHENOL DERIVATIVE; POTASSIUM CHANNEL HERG; TRAXOPRODIL; UNCLASSIFIED DRUG;

EID: 79956116531     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.117     Document Type: Article
Times cited : (23)

References (19)
  • 13
    • 84888461499 scopus 로고    scopus 로고
    • note
    • 3H]CP101,606 binding to membranes from post-natal day 11 rat brain minus cerebellum. This was a filtration assay conducted in 96 well plate format. The assay was conducted in either single concentration or concentration effect mode. Compounds were solubilized in DMSO and tested in a final DMSO concentration of 1%.
  • 15
    • 84888455295 scopus 로고    scopus 로고
    • note
    • 6) δ ppm 1.35 (dt, J = 12.21, 6.41 Hz, 2 H) 1.45 (td, J = 7.17, 3.66 Hz, 2 H) 1.53-1.75 (m, 4 H) 3.00 (t, J = 6.26 Hz, 1 H) 3.28 (br s, 1 H) 3.73 (s, 2 H) 3.76-3.82 (m, 3 H) 6.89 (td, J = 8.39, 2.44 Hz, 1 H) 7.06 (dd, J = 11.29, 2.44 Hz, 1 H) 7.37 (dd, J = 8.39, 6.87 Hz, 1 H) 7.78 (t, J = 1.98 Hz, 1 H) 8.45 (d, J = 1.53 Hz, 1 H) 8.49 (d, J = 2.14 Hz, 1 H); m/z (TOF) (M+H) calcd = 301.1711 found = 301.1729.
  • 16
    • 84888450557 scopus 로고    scopus 로고
    • note
    • The NR2B functional assay utilized the ChanTest NR1/NR2B HEK293 cell line. The cells were treated with tetracycline in the presence of ketamine in order to induce stable expression. Activation of the NR2B receptor with glutamate and glycine resulted in changes in cellular calcium concentrations that were quantified using a calcium sensitive dye and fluorescent detection platform.
  • 18
    • 84888464987 scopus 로고    scopus 로고
    • The assay for NR2A activity employed stably transfected oocytes with NR1/NR2A receptors. Cells were stimulated with glutamate and glycine, and concentration response curves were determined by TEVC using OpusExpress 6000
    • The assay for NR2A activity employed stably transfected oocytes with NR1/NR2A receptors. Cells were stimulated with glutamate and glycine, and concentration response curves were determined by TEVC using OpusExpress 6000.
  • 19
    • 0017618768 scopus 로고
    • Mouse forced swim test is a widely accepted assay for anti-depressant effects. Mice are individually forced to swim in a container for a defined time interval. Immobility time is the amount of time the animal stops swimming and remains motionless in the water. A decrease in immobility time is a signature of an anti-depressant effect
    • Porsolt, R. D.; Bertin, A.; Jalfre, M. Nature 1977, 266, 730. Mouse forced swim test is a widely accepted assay for anti-depressant effects. Mice are individually forced to swim in a container for a defined time interval. Immobility time is the amount of time the animal stops swimming and remains motionless in the water. A decrease in immobility time is a signature of an anti-depressant effect.
    • (1977) Nature , vol.266 , pp. 730
    • Porsolt, R.D.1    Bertin, A.2    Jalfre, M.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.