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Volumn 18, Issue 20, 2008, Pages 5493-5496

3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators

Author keywords

Anxiety; mGluR2; Positive allosteric modulators; Potentiators; Schizophrenia

Indexed keywords

3 (IMIDAZOLYLMETHYL) 3 AZABICYCLO[3.1.0]HEXAN 6 YLMETHYL ETHER DERIVATIVE; BICYCLO COMPOUND; IMIDAZOLE DERIVATIVE; METABOTROPIC RECEPTOR 2; METABOTROPIC RECEPTOR AGONIST; UNCLASSIFIED DRUG;

EID: 53349165547     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.09.026     Document Type: Article
Times cited : (22)

References (19)
  • 13
    • 53349167074 scopus 로고    scopus 로고
    • 20 glutamate challenge. Data is analyzed as a ratio of the peak fluorescence to the baseline after compound addition. Assay to assay variability in PAM potency required multiple experiments to determine potency, typically n > 3.
    • 20 glutamate challenge. Data is analyzed as a ratio of the peak fluorescence to the baseline after compound addition. Assay to assay variability in PAM potency required multiple experiments to determine potency, typically n > 3.
  • 14
    • 53349102865 scopus 로고    scopus 로고
    • Whole brain and blood samples were collected from Sprague-Dawley rats at various times following administration of a single 10 mg/kg subcutaneous dose. Plasma and brain homogenate samples were quantitated using an LC/MS method and the brain to plasma ratio reported.
    • Whole brain and blood samples were collected from Sprague-Dawley rats at various times following administration of a single 10 mg/kg subcutaneous dose. Plasma and brain homogenate samples were quantitated using an LC/MS method and the brain to plasma ratio reported.
  • 15
    • 53349161881 scopus 로고    scopus 로고
    • Compound 1 (1 μM) was incubated in rat or human liver microsome and monitored for substrate depletion using an LC/MS method. Hepatic clearance was determined by scaling of the observed half-life using the well stirred model.
    • Compound 1 (1 μM) was incubated in rat or human liver microsome and monitored for substrate depletion using an LC/MS method. Hepatic clearance was determined by scaling of the observed half-life using the well stirred model.
  • 16
    • 53349096368 scopus 로고    scopus 로고
    • Pharmacokinetic parameters were determined in rats following a 1 mg/kg intravenous or 5 mg/kg oral administration to male Sprague-Dawley rats. Whole blood was collected from a jugular (iv and oral) or portal vein (oral only) catheter and plasma samples analyzed using an LC/MS method. Pharmacokinetic parameters were calculated using a non-compartmental analysis of the plasma concentration versus time data.
    • Pharmacokinetic parameters were determined in rats following a 1 mg/kg intravenous or 5 mg/kg oral administration to male Sprague-Dawley rats. Whole blood was collected from a jugular (iv and oral) or portal vein (oral only) catheter and plasma samples analyzed using an LC/MS method. Pharmacokinetic parameters were calculated using a non-compartmental analysis of the plasma concentration versus time data.
  • 19
    • 53349098593 scopus 로고    scopus 로고
    • In vitro rat microsomal stability r-CLh of 14c is 41 ml/min/kg, consistent with the in vivo measurement (within two folds).
    • In vitro rat microsomal stability r-CLh of 14c is 41 ml/min/kg, consistent with the in vivo measurement (within two folds).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.