Biochemical characterization of putative central purinergic receptors by using 2-chloro[3H]adenosine, a stable analog of adenosine.
- 1 November 1980
- journal article
- research article
- Published by Proceedings of the National Academy of Sciences in Proceedings of the National Academy of Sciences
- Vol. 77 (11), 6892-6896
- https://doi.org/10.1073/pnas.77.11.6892
Abstract
After pretreatment of rat brain synaptic membrane with adenosine deaminase to remove endogenous adenosine, 2-chloro[3H]adenosine, a stable analog of adenosine, binds to 2 sites with Kd values of 1.3 and 16 nM and corresponding Bmax values of 207 and 380 fmol/mg of protein. Binding is reversible and the highest density of sites occurs in enriched synaptosomal fractions. In peripheral tissue, negligible binding is observed in heart, kidney and liver, while testicle has 11 fmol of binding sites/mg of protein. In brain, caudate and hippocampus have the highest density of sites and spinal cord and hypothalamus have the lowest. This high-affinity binding is stereospecific: the L diasteromer of N6-phenylisopropyladenosine is .apprx. 30 times more potent as a displacer of 2-chloro[3H]adenosine than the D isomer and is sensitive to theophylline (IC50 = 8.8 .mu.M) and other purine-related compounds. Several putative neurotransmitters, neurotransmitter antagonists and other centrally active compounds have no effect on binding. The data are consistent with the hypothesis that 2-chloro[3H]adenosine is binding to central purinergic receptors.This publication has 35 references indexed in Scilit:
- Protective effect of adenosine and nicotinamide against audiogenic seizureBiochemical Pharmacology, 1974
- Rat cerebral-cortex adenosine deaminase activity and its subcellular distributionBiochemical Journal, 1974
- A Cyclic Adenosine Monophosphate Link in the Catecholamine Enhancement of Transmitter Release at the Neuromuscular JunctionThe Journal of general physiology, 1974
- Adenosine-elicited accumulation of cyclic AMP in brain slices: Potentiation by agents which inhibit uptake of adenosineLife Sciences, 1974
- Preliminary data on the possible hypnogenic role of adenosine1Journal of Neurochemistry, 1973
- Adenine derivatives as neurohumoral agents in the brain. The quantities liberated on excitation of superfused cerebral tissuesBiochemical Journal, 1972
- Effects of catecholamines and adenosine derivatives given into the brain of fowlsBritish Journal of Pharmacology, 1972
- Effects of Caffeine and Theophylline on Activity of Rats in Relation to Brain Xanthine ConcentrationsExperimental Biology and Medicine, 1972
- The effect of adenosine and adenine nucleotides on the cyclic adenosine 3', 5'-phosphate content of guinea pig cerebral cortex slices.1970
- REGIONAL STUDIES OF CATECHOLAMINES IN THE RAT BRAIN‐IJournal of Neurochemistry, 1966