《Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors》 was written by Jorgensen, William T.; Gulliver, Damien W.; Katte, Timothy A.; Werry, Eryn L.; Reekie, Tristan A.; Connor, Mark; Kassiou, Michael. Safety of 3,5-DihydroxybenzaldehydeThis research focused onWAY 267464 conformationally rigid derivative preparation oxytocin vasopressin receptor; Arginine vasopressin 1(a) receptor; Diazepine; Oxytocin receptor; WAY-267,464. The article conveys some information:
WAY-267,464 (I) and twelve conformationally rigid analogs were synthesized, characterized and evaluated in cellular assays with the aim of systematically exploring interactions with the oxytocin receptor (OTR). Each analog was evaluated in radioligand binding displacement assays at both human OTR and arginine vasopressin 1a receptors (V1aR). Physiol. characterization was determined by whole cell IP1 accumulation assays on stably transfected human embryonic kidney (HEK) cells. Incorporation of the rigid, optionally substituted benzene ring abolished OTR activity and diminished V1aR pharmacol. when compared to I. A general trend was observed in V1aR affinity for the Pr analogs which identified the ortho-substituted analog II as the best in series (Ki = 251 nM) followed by a decrease in affinity through the meta and para-derivatives ( Ki = 874 nM, 1756 nM resp.). This study confirms the importance of the central pharmacophoric motifs of WAY-267,464 and illuminates the differences in the binding pocket of the highly conserved OTR and V1aR. The experimental process involved the reaction of 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Safety of 3,5-Dihydroxybenzaldehyde)
3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.Safety of 3,5-Dihydroxybenzaldehyde
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts