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Volumn 22, Issue 20, 2012, Pages 6469-6474

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators

Author keywords

Azetidinyl N cyclohexyl carboxamides and carbamates; Azetidinyl N sulfonamides; Azetidinyl oxadiazoles; mGluR5 positive allosteric modulators; PAM to NAM switching

Indexed keywords

1,2,4 OXADIAZOLE DERIVATIVE; ALKYL GROUP; AMIDE; AZETIDINE DERIVATIVE; AZETIDINYL OXADIAZOLE DERIVATIVE; CARBAMIC ACID DERIVATIVE; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR AGONIST; METABOTROPIC RECEPTOR ANTAGONIST; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; SULFONAMIDE; UNCLASSIFIED DRUG;

EID: 84866738528     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.044     Document Type: Article
Times cited : (14)

References (52)
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    • 80 response to l-glutamate in the presence of test compound.
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    • The solubility (μM) was measured from DMSO stock solution of the test compound (300 μL) diluted with 2 × 200μL, 25 mM potassium phosphate buffer in a titer plate shaker at a speed of 1.8 for 4 h. The supernatant was analyzed by waters acquity UPLC system (column: acquity UPLC BEH C-18, 1.7 μm 2.1 × 50 mm column and PDA detector at 254 nm for quantification) with a gradient (mobile phase A: 2% (w/v) ammonium formate and 20% acetonitrile in water, mobile phase B: 100% acetonitrile) for 2 min.
  • 52
    • 84875004741 scopus 로고    scopus 로고
    • note
    • A single dose brain and plasma PK of compounds 13n and 17c were assessed at 10 mg/kg, po dose in two animals at 1 h. The plasma concentrations were determined using a tandem Agilent 1100 HPLC (Agilent Technologies, Palo Alto, CA) and a TSQ Quantum MS (Thermo Finnigan, San Jose, CA) with Xcalibur software and averaged values are shown. Compound limit of quantification (LOQ) in the brain homogenate and plasma was 2 and 10 ng/mL respectively.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.