PMID- 11120383
OWN - NLM
STAT- MEDLINE
DCOM- 20010125
LR  - 20191210
IS  - 0306-3623 (Print)
IS  - 0306-3623 (Linking)
VI  - 34
IP  - 3
DP  - 2000 Mar
TI  - Effects of three different Ca(2+) pump ATPase inhibitors on evoked contractions 
      in rabbit aorta and activities of Ca(2+) pump ATPases in porcine aorta.
PG  - 211-20
AB  - Using vascular smooth muscle, we describe the actions of three pharmacological 
      tools, cyclopiazonic acid (CPA), thapsigargin (TG) and 
      2,5-di-(tert-butyl)-1,4-benzohydroquinone (tBHQ), which are presumed to act as 
      selective inhibitors of the sarco-endoplasmic reticulum Ca(2+)-ATPases (SERCAs). 
      In porcine aortic smooth muscle microsomes two Ca(2+)-ATPase activities have been 
      described, one vanadate-sensitive and one vanadate-resistant, representing the 
      Ca(2+)-ATPase activities of the plasma membrane and SERCAs, respectively. In 
      agreement, CPA, TG and tBHQ, in the concentration range 0.1 microM to 0.1 mM, 
      dose-dependently inhibit the Ca(2+)-ATPase activity only in the 
      vanadate-resistant microsomes. However, 0.1 mM tBHQ also significantly inhibited 
      the Ca(2+)-ATPase activity of vanadate-sensitive microsomes. In rabbit aortic 
      rings, all three SERCA inhibitors produced a dose-dependant inhibition of 
      contractions evoked by 20 mM caffeine or 1 microM phenylephrine (PE) in a 
      Ca(2+)-free physiological solution. However, in PE-contracted rings, tBHQ (> or 
      =30 microM) also significantly inhibited the ability of cromakalim to induce 
      relaxation. In conclusion, the data suggest that CPA, TG and tBHQ can all act as 
      selective SERCA inhibitors in both porcine and rabbit aortic smooth muscle. 
      However, in contrast to CPA and TG, high concentrations of tBHQ can exhibit some 
      nonspecific effects, which include inhibition of the plasma membrane 
      Ca(2+)-ATPase and possibly K(+) channels regulated by cromakalim.
FAU - Luo, D
AU  - Luo D
AD  - Department of Pharmacology, Niigata University School of Medicine, 951, Niigata, 
      Japan. luodl@ems.hrbmu.edu.cn
FAU - Nakazawa, M
AU  - Nakazawa M
FAU - Yoshida, Y
AU  - Yoshida Y
FAU - Cai, J
AU  - Cai J
FAU - Imai, S
AU  - Imai S
LA  - eng
PT  - Journal Article
PL  - England
TA  - Gen Pharmacol
JT  - General pharmacology
JID - 7602417
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Hydroquinones)
RN  - 0 (Indoles)
RN  - 0 (Vasodilator Agents)
RN  - 0G4X367WA3 (Cromakalim)
RN  - 1WS297W6MV (Phenylephrine)
RN  - 3G6A5W338E (Caffeine)
RN  - 3WHH0066W5 (Vanadates)
RN  - 67526-95-8 (Thapsigargin)
RN  - C12674942B (2-tert-butylhydroquinone)
RN  - EC 7.2.2.10 (Calcium-Transporting ATPases)
RN  - RWP5GA015D (Potassium)
RN  - SY7Q814VUP (Calcium)
RN  - X9TLY4580Z (cyclopiazonic acid)
SB  - IM
MH  - Animals
MH  - Aorta
MH  - Caffeine/pharmacology
MH  - Calcium/metabolism
MH  - Calcium-Transporting ATPases/*antagonists & inhibitors/metabolism
MH  - Cromakalim/pharmacology
MH  - Drug Interactions
MH  - Enzyme Inhibitors/*pharmacology
MH  - Hydroquinones/pharmacology
MH  - In Vitro Techniques
MH  - Indoles/*pharmacology
MH  - Microsomes/drug effects/enzymology
MH  - Muscle, Smooth, Vascular/drug effects/enzymology
MH  - Phenylephrine/pharmacology
MH  - Potassium/pharmacology
MH  - Rabbits
MH  - Swine
MH  - Thapsigargin/pharmacology
MH  - Vanadates/pharmacology
MH  - Vasoconstriction/*drug effects
MH  - Vasodilator Agents/pharmacology
EDAT- 2000/12/20 11:00
MHDA- 2001/02/28 10:01
CRDT- 2000/12/20 11:00
PHST- 2000/12/20 11:00 [pubmed]
PHST- 2001/02/28 10:01 [medline]
PHST- 2000/12/20 11:00 [entrez]
AID - S0306362300000641 [pii]
AID - 10.1016/s0306-3623(00)00064-1 [doi]
PST - ppublish
SO  - Gen Pharmacol. 2000 Mar;34(3):211-20. doi: 10.1016/s0306-3623(00)00064-1.