Bioorganic & Medicinal Chemistry 2004-03-01

Synthesis and pharmacological evaluation of N-acyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.

Hideki Kubota, Toshihiro Watanabe, Akio Kakefuda, Noriyuki Masuda, Kouichi Wada, Noe Ishii, Shuichi Sakamoto, Shinichi Tsukamoto

Index: Bioorg. Med. Chem. 12(5) , 871-82, (2004)

Full Text: HTML

Abstract

A series of N-acyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized and evaluated for their bradycardic activities in isolated guinea pig right atria and in urethane-anesthetized rats. These efforts resulted in identification of the compound 8a, which exhibits potent bradycardic activity with minimal influence on mean blood pressure in urethane-anesthetized rats. Oral administration of compound 8a to conscious rats revealed increased potency and prolonged duration of action when compared to Zatebradine.

Related Compounds

  • Zatebradine hydroc...

Related Articles:

Abnormal diastolic currents in ventricular myocytes from spontaneous hypertensive heart failure rats.

2006-11-01

[Am. J. Physiol. Heart Circ. Physiol. 291(5) , H2192-8, (2006)]

Effects of tachycardia on regional wall motion in acute ischemic canine heart.

2004-06-01

[Tohoku J. Exp. Med. 203(2) , 111-21, (2004)]

Validation of a high-sensitivity assay for zatebradine in dried blood spots of human blood at pg/ml concentrations using HILIC-MS/MS.

2010-11-01

[Bioanalysis 2(11) , 1863-71, (2010)]

Heart rate reduction by zatebradine reduces infarct size and mortality but promotes remodeling in rats with experimental myocardial infarction.

2004-04-01

[Am. J. Physiol. Heart Circ. Physiol. 286(4) , H1281-8, (2004)]

Blocking effects of acehytisine on pacemaker currents (I(f)) in sinoatrial node cells and human HCN4 channels expressed in Xenopus laevis oocytes.

2012-01-06

[J. Ethnopharmacol. 139(1) , 42-51, (2012)]

More Articles...