Di-aryl guanidinium derivatives: Towards improved α2-Adrenergic affinity and antagonist activity

Autor: Patricia Miranda-Azpiazu, Iria Brocos-Mosquera, Luis F. Callado, Brendan Kelly, Aaron P. Keogh, Helene B. Mihigo, Michela McMullan, Aintzane García-Bea, Fernando Rodriguez, Isabel Rozas

Publikováno v: Addi. Archivo Digital para la Docencia y la Investigación
instname
Addi: Archivo Digital para la Docencia y la Investigación
Universidad del País Vasco

Compounds with excellent receptor engagement displaying alpha(2)-AR antagonist activity are useful not only for therapeutic purposes (e.g. antidepressants), but also to help in the crystallization of this particular GPCR. Therefore, based on our broa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00098d673f7bf3bff0e2233d76891f00
http://hdl.handle.net/10810/50321

α2-adrenoceptor antagonists: synthesis, pharmacological evaluation, and molecular modeling investigation of pyridinoguanidine, pyridino-2-aminoimidazoline and their derivatives

Autor: Jorge E. Ortega, J. Javier Meana, Luis F. Callado, Brendan D. Kelly, Michela McMullan, Carolina Muguruza, Isabel Rozas

Publikováno v: Journal of medicinal chemistry. 58(2)

We have previously identified phenylguanidine and phenyl-2-aminoimidazoline compounds as high affinity ligands with conflicting functional activity at the α2-adrenoceptor, a G-protein-coupled receptor with relevance in several neuropsychiatric condi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af39a406658480e67195e964b6d64773
https://pubmed.ncbi.nlm.nih.gov/25868391