118156-83-5Relevant articles and documents
EC18 as a Tool to Understand the Role of HCN4 Channels in Mediating Hyperpolarization-Activated Current in Tissues
Romanelli, Maria Novella,Del Lungo, Martina,Guandalini, Luca,Zobeiri, Mehrnoush,Gy?keres, András,árpádffy-Lovas, Tamás,Koncz, Istvan,Sartiani, Laura,Bartolucci, Gianluca,Dei, Silvia,Manetti, Dina,Teodori, Elisabetta,Budde, Thomas,Cerbai, Elisabetta
, p. 584 - 589 (2019/02/27)
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are membrane proteins encoded by four genes (HCN1-4) and widely distributed in the central and peripheral nervous system and in the heart. HCN channels are involved in several physiological functions, including the generation of rhythmic activity, and are considered important drug targets if compounds with isoform selectivity are developed. At present, however, few compounds are known, which are able to discriminate among HCN channel isoforms. The inclusion of the three-methylene chain of zatebradine into a cyclohexane ring gave a compound (3a) showing a 5-fold preference for HCN4 channels, and ability to selectively modulate Ih in different tissues. Compound 3a has been tested for its ability to reduce Ih and to interact with other ion channels in the heart and the central nervous system. Its preference for HCN4 channels makes this compound useful to elucidate the contribution of this isoform in the physiological and pathological processes involving hyperpolarization-activated current.
Hypervalent iodine(III)-induced intramolecular cyclization of α-(aryl)alkyl-β-dicarbonyl compounds: A convenient synthesis of benzannulated and spirobenzannulated compounds
Arisawa,Ramesh,Nakajima,Tohma,Kita
, p. 59 - 65 (2007/10/03)
A novel hypervalent iodine(III)-induced direct intramolecular cyclization of α-(aryl)alkyl-β-dicarbonyl compounds has been described. Both meta- and para-substituted phenol ether derivatives containing acyclic or cyclic 1,3-dicarbonyl moieties at the side chain undergo this reaction in a facile manner. The reactions afford benzannulated and spirobenzannulated compounds that are of biological importance. The reaction is found to be general, mild, and high yielding. The mechanism of the reaction has been shown to involve a cation radical intermediate.