最近の記事

2024/08/06
Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline.
2024/05/21
In vivo assessment of individual and total proteinuria in zebrafish larvae using the solvatochromic compound ZMB741
2021/10/31
Generation of a Transgenic Zebrafish Line for In Vivo Assessment of Hepatic Apoptosis
2021/08/19
Patient-Derived Cancer Xenograft Zebrafish Model (PDXZ) for Drug Discovery Screening and Personalized Medicine
2021/07/09
Establishment of a Quality Control Protocol for Zebrafish Developmental Toxicity Studies
2020/10/13
Gap junction protein beta 4 plays an important role in cardiac function in humans, rodents, and zebrafish
2020/05/28
A novel orexin antagonist from a natural plant was discovered using zebrafish behavioural analysis
2019/10/15
C3orf70 Is Involved in Neural and Neurobehavioral Development
2019/09/22
Generation of a Triple-Transgenic Zebrafish Line for Assessment of Developmental Neurotoxicity during Neuronal Differentiation
2019/07/17
Aging-associated microstructural deterioration of vertebra in zebrafish

一覧に戻る

1990/02/15
  • CiteULike
  • reddit
  • StumbleUpon
  • linkedin
  • Delicious
  • Mendeley
  • はてなブックマーク
  • Youtube
  • Google+
  • Twitter
  • Facebook

Effects of amrinone and enoximone on the subclasses of cyclic AMP phosphodiesterase from human heart and kideny.

Masuoka H, Ito M, Nakano T, Naka M, Tanaka T.
J Cardiovasc Pharmacol. 1990 Feb;15(2):302-7.

Abstract

We observed the intracellular localization of low-Km cyclic adenosine monophosphate (cAMP) phosphodiesterase (PDEIII) subclasses in human heart in comparison to that in human kidney by using comparable potencies of specific inhibitors. PDEIII was observed in not only soluble fraction but particulate fraction in human heart and kidney. Both soluble and particulate PDEIII from human heart selectively hydrolyzed cAMP with similar Km values of 0.36 and 0.40 microM, respectively. They were potently inhibited by amrinone, enoximone, and cyclic guanosine monophosphate (cGMP), but were weakly inhibited by rolipram with much the same IC50 values. Although several animals having soluble and particulate PDEIII possess two pharmacologically distinct subclasses of PDEIII, human heart has only one form, cGMP-sensitive PDEIII. In contrast to cardiac PDEIII, both soluble and particulate PDEIII from human kidney were not readily inhibited by amrinone, enoximone, and cGMP, but rather strongly inhibited by rolipram. Human kidney contains only cGMP-less sensitive form of PDEIII in soluble and particulate fractions. These results suggest that the intracellular distribution of PDEIII subclasses in human hearts are significantly different from those in the hearts of other animal species, and subclasses of PDEIII in humans hearts could not be distinguished by intracellular localization but by organ specificity.

関連リンク