110406-97-8Relevant 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)
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.
High hypolipidemic activity of saturated side-chain α-asarone analogs
Cruz, Adriana,Garduno, Leticia,Salazar, Maria,Martinez, Elizdath,Diaz, Francisco,Chamorro, German,Tamariz, Joaquin
, p. 587 - 595 (2007/10/03)
With the aim of evaluating the pharmacophore potential of the side chain of α-asarone (1) regarding its high hypolipidemic activity, the series of derivatives 7a-7e, and 11-13 were evaluated pharmacologically. For the hydrocarbon compounds 7a-7e, with a variable-size side chain, significant decreases in serum cholesterol, LDL-cholesterol, and triglyceride levels and significant increases in HDL-cholesterol levels were observed in mice. The small-size side-chain derivatives were even more active than 1 in reducing cholesterol. The results suggested that the length and saturated character of the side chain seem to be a key feature in improving hypolipidemic activity of α-asarone (1) analogs.