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Volumn 19, Issue 8, 2009, Pages 2190-2194

In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists

Author keywords

Central nervous system; mgluR1; Nociceptive pain

Indexed keywords

AMINE; GLUTAMIC ACID; METABOTROPIC RECEPTOR ANTAGONIST; MORPHINE; PYRIDO[3,4 D]PYRAMID 4 YLAMINE; UNCLASSIFIED DRUG;

EID: 63349101749     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.02.106     Document Type: Article
Times cited : (14)

References (9)
  • 4
    • 34248580649 scopus 로고    scopus 로고
    • Procedures for the synthesis of or methods of preparation for all the compounds within this manuscript are contained within Harbottle, G. W, Feeder, N, Gibson, K. R, Glossop, M, Maw, G. N, Million, W. A, Morel, F. F, Osborne, S, Poinsard, C. Tetrahedron Lett. 2007, 48, 4293 or Edwards, P. J, Gibson, K. R, Mantell, S. J, Maw, G. N, Poinsard, C. US 2005038047
    • Procedures for the synthesis of or methods of preparation for all the compounds within this manuscript are contained within Harbottle, G. W.; Feeder, N.; Gibson, K. R.; Glossop, M.; Maw, G. N.; Million, W. A.; Morel, F. F.; Osborne, S.; Poinsard, C. Tetrahedron Lett. 2007, 48, 4293 or Edwards, P. J.; Gibson, K. R.; Mantell, S. J.; Maw, G. N.; Poinsard, C. US 2005038047.
  • 7
    • 63349090633 scopus 로고    scopus 로고
    • note
    • The EMG was recorded by a concentric electrode inserted into a flexor leg muscle and the reflex evoked by a 5 s application of an arterial clip. The clip exerts a constant force that was reported to be mildly noxious when the experimenters applied it to themselves. In this model iv administration of morphine at doses that have been reported to cause analgesia in awake rats inhibits the EMG reflex by approximately 40%. Drugs were administered iv; a loading bolus was given over 30 s and a maintenance infusion for the remainder of the experiment (1 h). The pinch stimulus was applied at 10 min intervals, when three consecutive pinch responses varied by less than 10% the drug or vehicle was applied. The data for each study was normalised with respect the mean of the three consistent baseline responses. At the end of the study plasma and CSF samples were taken to assess the drug level achieved peripherally and centrally for each study.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.