PMID- 8632724
OWN - NLM
STAT- MEDLINE
DCOM- 19960628
LR  - 20190701
IS  - 0024-3205 (Print)
IS  - 0024-3205 (Linking)
VI  - 58
IP  - 9
DP  - 1996
TI  - Adaptive changes in adenosine receptors following long-term treatment with the 
      adenosine receptor agonist R-phenylisopropyl adenosine.
PG  - 769-76
AB  - Changes in brain A1 and A2A receptors and in the corresponding mRNA were studied 
      using quantitative receptor autoradiography and in situ hybridisation. [3H]-DPCPX 
      was used as an antagonist ligand at A1 receptors and [3H]-CGS 21680 as an agonist 
      ligand at A2A receptors. Treatment of rats with the relatively A1 receptor 
      selective adenosine analogue R-PIA (0.3 mg/kg) for 7 days in the presence of the 
      peripherally acting antagonist 8-p-sulfophenyltheophylline (8-PST; 10 mg/kg) 
      caused a decrease in the binding of the A1 receptor ligand, but not in that of 
      the A2A receptor ligand. The effect on A1 receptors was also seen in the presence 
      of 100 microM GTP that decreases agonist binding to insignificant levels. There 
      was no change in either A1 or A2A receptor mRNA. No significant changes were 
      detected following administration of either R-PIA or 8-PST alone. These results 
      thus demonstrate an effect on brain A1 receptors after systemic administration of 
      R-PIA in the presence of a peripherally acting adenosine antagonist, 
      demonstrating that, under these conditions, the agonist reaches receptors in 
      significant amounts.
FAU - Fernandez, M
AU  - Fernandez M
AD  - Department of Physiology and Pharmacology, Divison of Molecular 
      Neuropharmacology, Karolinska Institutet, Stockholm, Sweden.
FAU - Svenningsson, P
AU  - Svenningsson P
FAU - Fredholm, B B
AU  - Fredholm BB
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Life Sci
JT  - Life sciences
JID - 0375521
RN  - 0 (RNA, Messenger)
RN  - 0 (Receptors, Purinergic P1)
RN  - 0 (Xanthines)
RN  - 29193-86-0 (Phenylisopropyladenosine)
RN  - 80206-91-3 (8-(4-sulfophenyl)theophylline)
RN  - 9PTP4FOI9E (1,3-dipropyl-8-cyclopentylxanthine)
RN  - C137DTR5RG (Theophylline)
SB  - IM
MH  - Analysis of Variance
MH  - Animals
MH  - Brain/*metabolism
MH  - Caudate Nucleus/metabolism
MH  - Cerebellum/metabolism
MH  - Cerebral Cortex/metabolism
MH  - Globus Pallidus/metabolism
MH  - Hippocampus/metabolism
MH  - Male
MH  - Organ Specificity
MH  - Phenylisopropyladenosine/*pharmacology
MH  - Putamen/metabolism
MH  - RNA, Messenger/analysis/biosynthesis
MH  - Radioligand Assay
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Receptors, Purinergic P1/biosynthesis/drug effects/*metabolism
MH  - Reference Values
MH  - Theophylline/*analogs & derivatives/pharmacology
MH  - Time Factors
MH  - Xanthines/metabolism
EDAT- 1996/01/01 00:00
MHDA- 1996/01/01 00:01
CRDT- 1996/01/01 00:00
PHST- 1996/01/01 00:00 [pubmed]
PHST- 1996/01/01 00:01 [medline]
PHST- 1996/01/01 00:00 [entrez]
AID - 0024320595023550 [pii]
AID - 10.1016/0024-3205(95)02355-0 [doi]
PST - ppublish
SO  - Life Sci. 1996;58(9):769-76. doi: 10.1016/0024-3205(95)02355-0.