New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists

Autor:	Page Daniel, Christopher Walpole, François Gaudreault, Meredith Fyfe, Hua Yang, Manon Fleurent, Stephane St-Onge, William Brown
Rok vydání:	2007
Předmět:	Agonist Cannabinoid receptor Indoles medicine.drug_class Stereochemistry Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Biochemistry Chemical synthesis Binding Competitive Receptor Cannabinoid CB2 Drug Discovery Cannabinoid receptor type 2 medicine Moiety Pyrroles Molecular Biology Indole test Molecular Structure Chemistry Organic Chemistry In vitro Molecular Medicine lipids (amino acids peptides and proteins) Selectivity
Zdroj:	Bioorganicmedicinal chemistry letters. 17(22)
ISSN:	0960-894X
Popis:	The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC50 values. They also showed moderate to good (>350-fold) selectivity over the CB1 receptor.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13002dd9d03208d0da7bfdc7ac12b204 https://pubmed.ncbi.nlm.nih.gov/17884494 Zobrazit plný text záznamu Full Text from ScienceDirect