Aminoquinazolines as TRPV1 antagonists : Modulation of drug-like properties through the exploration of 2-position substitution
- Author
- BLUM, Charles A1 ; XIAOZHANG ZHENG1 ; NGO, Chu K1 ; FUNG, Lawrence1 ; DAY, Marta1 ; KERSHAW, Mark1 ; DE LOMBAERT, Stéphane1 ; CHENARD, Bertrand L1 ; BRIELMANN, Harry1 ; HODGETTS, Kevin J1 ; BAKTHAVATCHALAM, Rajagopal1 ; CHANDRASEKHAR, Jayaraman1 ; KRAUSE, James E1 ; CORTRIGHT, Daniel1 ; MATSON, David1 ; CRANDALL, Marci1
[1] Neurogen Corporation, 35 N. E. Industrial Road, Branford, CT 06405, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2008, Vol 18, Num 16, pp 4573-4577, 5 p ; ref : 15 ref
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Oxford
- Publication country
- United Kingdom
- Document type
- Article
- Language
- English
- Author keyword
- Aminoquinazolines Antagonists TRPV1 VR1
- Keyword (fr)
- Affinité Analgésique Animal Antagoniste Chimiothérapie Composé aromatique Composé bicyclique Dérivé de la pyridine Dérivé du benzène Hyperalgésie Hétérocycle azote In vitro In vivo Pharmacocinétique Rat Relation structure activité Récepteur vanilloïde VR1 Synthèse chimique Voie intraveineuse Voie orale Canal ionique TRP Quinazoline(2-méthoxyméthyl-4-[4-(trifluorométhyl)anilino]-7-[3-trifluorométhyl-2-pyridyl]) Récepteur vanilloïde TRPV1 Fluor Composé organique Mammalia Rodentia Traitement Vertebrata
- Keyword (en)
- Affinity Analgesic Animal Antagonist Chemotherapy Aromatic compound Bicyclic compound Pyridine derivatives Benzene derivatives Hyperalgesia Nitrogen heterocycle In vitro In vivo Pharmacokinetics Rat Structure activity relation VR1 vanilloid receptor Chemical synthesis Intravenous administration Oral administration TRP ion channel TRPV1 vanilloid receptor Fluorine Organic compounds Mammalia Rodentia Treatment Vertebrata
- Keyword (es)
- Afinidad Analgésico Animal Antagonista Quimioterapia Compuesto aromático Compuesto bicíclico Piridina derivado Benceno derivado Hiperalgesia Heterociclo nitrógeno In vitro In vivo Farmacocinética Rata Relación estructura actividad Receptor vaniloide VR1 Síntesis química Vía intravenosa Vía oral Fluor Compuesto orgánico Mammalia Rodentia Tratamiento Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02B Neuropharmacology / 002B02B05 Analgesics
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 20608600
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmcl.2008.07.036 
https://dx.doi.org/10.1016/j.bmcl.2008.07.036
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