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Query: UMLS:C0002962 (
angina
)
21,142
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The pharmacokinetic profile of a single dose of 100 mg of (+/-)-N-[2-[[3-(o-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]- 2-(p-hydroxyphenyl)
acetamide
(epanolol, Visacor), has been determined in an open study of 15 elderly patients with stable
angina pectoris
. Haematological, biochemical and physiological measurements demonstrated that epanolol was well tolerated in this group of patients. A mean peak epanolol concentration of 18.4 ng/ml was observed at a mean time of 1.08 h. In about one third of patients, an analytically significant secondary peak was observed. Peak concentrations showed an interindividual variability of 16-fold. Following the peak, plasma concentrations declined biphasically. Epanolol was eliminated from plasma with a mean terminal half-life of 22 h. There was some evidence of a linear relationship between heart rate and logarithmic plasma concentration but this was not statistically significant. These data are consistent with the results of pharmacokinetic studies in healthy young volunteers.
...
PMID:Pharmacokinetics of epanolol in elderly patients with stable angina pectoris. 197 Jul 34
Atrial fibrillation is the most common arrhythmia seen in clinical practice, and novel pharmacological approaches for treatment are sought. Ranolazine (Ranexa; N-(2,6-dimethylphenyl)-2-[4-(2-hydroxy-3-[2-methoxyphenoxy]propyl)piperazin-1-yl]
acetamide
) is used clinically for the treatment of
angina pectoris
. Evidence is reviewed from both pre-clinical and clinical studies, which suggests that ranolazine also exhibits antiarrhythmic activity with growing evidence for atrio-selectivity. Further work is required in order to explore more fully the potential of ranolazine in the treatment of atrial fibrillation. In particular, investigation of ranolazine actions against atrial fibrillation in animal models that incorporate atrial fibrillation-related remodeling and data from carefully controlled trials in human atrial fibrillation would be of value.
...
PMID:Perspective: does ranolazine have potential for the treatment of atrial fibrillation? 2110 55
The adenosine A
2B
receptor (A
2B
AR) has been identified as an important therapeutic target in cardiovascular disease, however in vitro and in vivo targeting has been limited by the paucity of pharmacological tools, particularly potent agonists. Interestingly, 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)-2-pyridinyl)thio)
acetamide
(BAY60-6583), a potent and subtype-selective A
2B
AR agonist, has the same core structure as 2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitril (capadenoson). Capadenoson, currently classified as an adenosine A
1
receptor (A
1
AR) partial agonist, has undergone two Phase IIa clinical trials, initially in patients with atrial fibrillation and subsequently in patients with stable
angina
. Capadenoson has also been shown to decrease cardiac remodeling in an animal model of advanced heart failure and a capadenoson derivative, neladenoson bialanate, recently entered clinical development for the treatment of chronic heart failure. The therapeutic effects of capadenoson are currently thought to be mediated through the A
1
AR. However, the ability of capadenoson to stimulate additional adenosine receptor subtypes, in particular the A
2B
AR, has not been rigorously assessed. In this study, we demonstrate that capadenoson does indeed have significant A
2B
AR activity in physiologically relevant cells, cardiac fibroblasts and cardiomyocytes, which endogenously express the A
2B
AR. Relative to the non-selective adenosine receptor agonist NECA, capadenoson was a biased A
2B
AR agonist with a preference for cAMP signal transduction over other downstream mediators in cells with recombinant and endogenous A
2B
AR expression. These findings suggest the reclassification of capadenoson as a dual A
1
AR/A
2B
AR agonist. Furthermore, a potential A
2B
AR contribution should be an important consideration for the future clinical development of capadenoson-like therapeutics, as the A
2B
AR can promote cardioprotection and modulate cardiac fibrosis in heart disease.
...
PMID:Capadenoson, a clinically trialed partial adenosine A
1
receptor agonist, can stimulate adenosine A
2B
receptor biased agonism. 2834 25
