Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism.

Xia, Lizi; de Vries, Henk; Yang, Xue; Lenselink, Eelke B; Kyrizaki, Athina; Barth, Francis; Louvel, Julien; Dreyer, Matthias K; van der Es, Daan; IJzerman, Adriaan P; Heitman, Laura H

Xia, Lizi; de Vries, Henk; Yang, Xue; Lenselink, Eelke B; Kyrizaki, Athina; Barth, Francis; Louvel, Julien; Dreyer, Matthias K; van der Es, Daan; IJzerman, Adriaan P; Heitman, Laura H.

Affiliation

Xia L; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
de Vries H; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Yang X; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Lenselink EB; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Kyrizaki A; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Barth F; Sanofi-Aventis Research and Development, 371, Rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
Louvel J; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Dreyer MK; Sanofi-Aventis Deutschland GmbH R&D, Integrated Drug Discovery, Industriepark Hoechst, 65926 Frankfurt, Germany.
van der Es D; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
IJzerman AP; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands.
Heitman LH; Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, The Netherlands. Electronic address: l.h.heitman@lacdr.leidenuniv.nl.

Biochem Pharmacol ; 151: 166-179, 2018 05.

Article de En | MEDLINE | ID: mdl-29102677

Sujet(s)
Mots clés

Antagonist 1 (CAS Registry Number: 1207203-10-8); Antagonist 2 (CAS Registry Number: 1207203-08-4); Antagonist 3 (CAS Registry Number: 1207203-09-5); Antagonist 4 (CAS Registry Number: 1207203-19-7); Antagonist 5 (CAS Registry Number: 1207203-16-4); Antagonist 6 (CAS Registry Number: 1207203-15-3); Antagonist 7 (CAS Registry Number: 1207202-94-5); Antagonist 8 (CAS Registry Number: 1207203-14-2); Antagonist 9 (CAS Registry Number: 1207203-18-6); CP55940 (PubChem CID: 104895); Cannabinoid 1 receptor; Insurmountable antagonism; Preincubation; Radioligand binding; Residence time; Rimonabant (PubChem CID: 104850); Structure-kinetics relationships

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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Récepteur cannabinoïde de type CB1 / Antagonistes des récepteurs de cannabinoïdes Limites: Animals Langue: En Journal: Biochem Pharmacol Année: 2018 Type de document: Article Pays d'affiliation: Pays-Bas Pays de publication: Royaume-Uni

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