The population of reserve alpha-2 adrenoceptors that mediate the inhibitory effect of clonidine on the activity of locus coeruleus neurons has been studied using extracellular recordings in anesthetized rats. Animals were pretreated with the irreversible receptor antagonist N-ethoxycarbonyl-2-ethoxy-1-2-dihydroquinoline (EEDQ). In rats pretreated with EEDQ (1, 2 and 6 mg/kg, i.p., 6 hr before e...

Cystic fibrosis transmembrane conductance regulator (CFTR) is unique among ion channels in that after its phosphorylation by protein kinase A (PKA), its ATP-dependent gating violates microscopic reversibility caused by the intimate involvement of ATP hydrolysis in controlling channel closure. Recent studies suggest a gating model featuring an energetic coupling between opening and closing of th...

A one-pot and efficient approach to the synthesis of dialkyl 2-[1-[(alkoxycarbonyl)anilino]-2(1H)(isoquinolin-2-yl) (or -quinolin-1-yl or -pyridin-1-yl)]-2-butenedioates is described. This method involves a three-component reaction between isoquinoline, quinoline or pyridine, dialkyl acetylenedicarboxylates and N-phenylcarbamates under solvent-free conditions, without using any catalyst and at ...

Yang, J. 2017. Development of Peptide Binders. Applied to Human CRP, Carbonic Anhydrase (II, IX) and Lysine Demethylase 1. Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology 1568. 60 pp. Uppsala: Acta Universitatis Upsaliensis. ISBN 978-91-513-0086-3. In this thesis, a polypeptide binder concept is illustrated. By conjugation to a set of sixteen ...