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Page 1
Endothelin.
Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, Pollock DM, Webb DJ, Maguire JJ. Davenport AP, et al. Pharmacol Rev. 2016 Apr;68(2):357-418. doi: 10.1124/pr.115.011833. Pharmacol Rev. 2016. PMID: 26956245 Free PMC article. Review.
Highly selective peptide ETA and ETB antagonists and ETB agonists together with radiolabeled analogs have accurately delineated endothelin pharmacology in humans and animal models, although surprisingly no ETA agonist has been discovered. ET antagonists (bosentan, ambrisentan
Highly selective peptide ETA and ETB antagonists and ETB agonists together with radiolabeled analogs have accurately delineated endothelin p …
Pharmacokinetic and Pharmacodynamic Comparison of Sildenafil-Bosentan and Sildenafil-Ambrisentan Combination Therapies for Pulmonary Hypertension.
Hakamata A, Odagiri K, Miyakawa S, Irisawa H, Takeuchi K, Inui N, Tanaka S, Uchida S, Watanabe H. Hakamata A, et al. Clin Transl Sci. 2016 Feb;9(1):29-35. doi: 10.1111/cts.12382. Epub 2016 Jan 12. Clin Transl Sci. 2016. PMID: 26756977 Free PMC article. Clinical Trial.
To elucidate whether the pharmacokinetics (PK) and pharmacodynamics (PD) of sildenafil are influenced differently when it is coadministered with bosentan (S+B) or with ambrisentan (S+A), we evaluated the PK and PD profiles of sildenafil before and after 4-5 w …
To elucidate whether the pharmacokinetics (PK) and pharmacodynamics (PD) of sildenafil are influenced differently when it is coadmini …
Pharmacokinetic and pharmacodynamic evaluation of macitentan , a novel endothelin receptor antagonist for the treatment of pulmonary arterial hypertension.
Sidharta PN, Krähenbühl S, Dingemanse J. Sidharta PN, et al. Expert Opin Drug Metab Toxicol. 2015 Mar;11(3):437-49. doi: 10.1517/17425255.2015.1000859. Epub 2015 Jan 21. Expert Opin Drug Metab Toxicol. 2015. PMID: 25604973 Review.
AREAS COVERED: This review discusses the pharmacokinetics (PK) and pharmacodynamics (PD) of macitentan and its drug interaction potential based on preclinical and clinical data. ...The safety profile of macitentan is favorable with respect to hepatic safety and edema/fluid …
AREAS COVERED: This review discusses the pharmacokinetics (PK) and pharmacodynamics (PD) of macitentan and its drug interaction poten …
Gateways to clinical trials.
Bayés M, Rabasseda X, Prous JR. Bayés M, et al. Methods Find Exp Clin Pharmacol. 2004 Oct;26(8):639-63. Methods Find Exp Clin Pharmacol. 2004. PMID: 15605126
This issue focuses on the following selection of drugs: Abiraterone acetate, Ad5CMV-p53, adefovir dipivoxil, AE-941, ambrisentan, aripiprazole, atomoxetine hydrochloride, atrasentan; BCH-10618, bimatoprost, BMS-184476, BMS-275183, BMS-387032, botulinum toxin type B, BR-1, …
This issue focuses on the following selection of drugs: Abiraterone acetate, Ad5CMV-p53, adefovir dipivoxil, AE-941, ambrisentan, ari …
Endothelin-1 receptors in rat tissues: characterization by bosentan, ambrisentan and CI-1020.
Yokoyama Y, Osano A, Hayashi H, Itoh K, Okura T, Deguchi Y, Ito Y, Yamada S. Yokoyama Y, et al. Biol Pharm Bull. 2014;37(3):461-5. doi: 10.1248/bpb.b13-00881. Biol Pharm Bull. 2014. PMID: 24583865 Free article.
Significant amount of specific [(125)I]ET-1 binding was detected in the lung, heart, kidney, bladder and cerebral cortex of rats. ET-1, bosentan, ambrisentan, and CI-1020 inhibited specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. The Hill …
Significant amount of specific [(125)I]ET-1 binding was detected in the lung, heart, kidney, bladder and cerebral cortex of rats. ET-1, bose …
Effect of the novel endothelin(A) receptor antagonist LU 208075 on contraction and relaxation of isolated rat basilar artery.
Vatter H, Zimmermann M, Jung C, Weyrauch E, Lang J, Seifert V. Vatter H, et al. Clin Sci (Lond). 2002 Aug;103 Suppl 48:408S-413S. doi: 10.1042/CS103S408S. Clin Sci (Lond). 2002. PMID: 12193134
Relaxation was investigated on precontracted segments, calculated in percentage decrease of precontraction and compared by the pD(2) and E(max). ET-1 and bigET-1 induced contraction was dose dependently inhibited by LU 208075. ...
Relaxation was investigated on precontracted segments, calculated in percentage decrease of precontraction and compared by the pD(2) …