An article Discovery of Novel pERK1/2-or beta-Arrestin-Preferring 5-HT1A Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile WOS:000580558700018 published article about FUNCTIONAL SELECTIVITY; DRUG DISCOVERY; SEROTONIN; ANTAGONIST; METABOLISM; AGENTS; POTENT; RATS; HIPPOCAMPUS; ANXIOLYTICS in [Sniecikowska, Joanna; Gluch-Lutwin, Monika; Bucki, Adam; Wieckowska, Anna; Siwek, Agata; Jastrzebska-Wiesek, Magdalena; Partyka, Anna; Wilczynska, Daria; Pytka, Karolina; Latacz, Gniewomir; Przejczowska-Pomierny, Katarzyna; Wyska, Elzbieta; Wesolowska, Anna; Pawlowski, Maciej; Kolaczkowski, Marcin] Jagiellonian Univ, Med Coll, Fac Pharm, PL-30688 Krakow, Poland; [Newman-Tancredi, Adrian] Neurolixis, Castres, France in 2020, Cited 67. SDS of cas: 150-19-6. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6
Novel 1-(1-benzoylpiperidin-4-yl)methanamine derivatives with high affinity and selectivity for serotonin 5-HT1A receptors were obtained and tested in four functional assays: ERK1/2 phosphorylation, adenylyl cyclase inhibition, calcium mobilization, and beta-arrestin recruitment. Compounds 44 and 56 (2-methylaminophenoxyethyl and 2-(1H-indol-4-yloxy)ethyl derivatives, respectively) were selected as biased agonists with highly differential signaling fingerprints that translated into distinct in vivo profiles. In vitro, 44 showed biased agonism for ERK1/2 phosphorylation and, in vivo, it preferentially exerted an antidepressant-like effect in the Porsolt forced swimming test in rats. In contrast, compound 56 exhibited a first-in-class profile: it preferentially and potently activated beta-arrestin recruitment in vitro and potently elicited lower lip retraction in vivo, a component of serotonergic syndrome. Both compounds showed promising developability properties. The presented 5-HT1A receptor-biased agonists, preferentially targeting various signaling pathways, have the potential to become drug candidates for distinct central nervous system pathologies and possessing accentuated therapeutic activity and reduced side effects.
SDS of cas: 150-19-6. Welcome to talk about 150-19-6, If you have any questions, you can contact Sniecikowska, J; Gluch-Lutwin, M; Bucki, A; Wieckowska, A; Siwek, A; Jastrzebska-Wiesek, M; Partyka, A; Wilczynska, D; Pytka, K; Latacz, G; Przejczowska-Pomierny, K; Wyska, E; Wesolowska, A; Pawlowski, M; Newman-Tancredi, A; Kolaczkowski, M or send Email.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles