TY - JOUR
T1 - Adenosine receptors in the central nervous system
T2 - Relationship to the central actions of methylxanthines
AU - Daly, John W.
AU - Bruns, Robert F.
AU - Snyder, S. H.
N1 - Funding Information:
The researchp rogramh as beens upportedi n part (R.F.B. and S.H.S.) by a grant from the International Life Science Institute and by USPHS grantsM H-18501a nd DA-00266a nd a granto f the McKnightF oundation.
PY - 1981/5/11
Y1 - 1981/5/11
N2 - Adenosine has a significant role in many functions of the central nervous system. Behaviorally, adenosine and adenosine analogs have marked depressant effects. Electrophysiologically, adenosine reduces spontaneous neuronal activity and inhibits transsynaptic potentials via interaction with extracellular receptors. Biochemically, adenosine inhibits adenylate cyclase via a "high" affinity receptor, and activates adenylate cyclase via a "low" affinity receptor. These receptors, called "A1" and "A2" respectively, show differing profiles for activation by adenosine analogs. Radioactive N6-cyclohexyladenosine binds selectively to the "high" affinity receptor. One major class of antagonists is known at adenosine receptors: the alkylxanthines, including caffeine and theophylline. Radioactive 1,3-diethyl-8-phenylxanthine, a particularly potent antagonist, appears to bind to both low and high affinity adenosine receptors. Behavioral, electrophysiological, and biochemical effects of alkylxanthines are consistent with the hypothesis that the central stimulatory actions of caffeine and theophylline are due in large part to antagonism of central adenosine receptors.
AB - Adenosine has a significant role in many functions of the central nervous system. Behaviorally, adenosine and adenosine analogs have marked depressant effects. Electrophysiologically, adenosine reduces spontaneous neuronal activity and inhibits transsynaptic potentials via interaction with extracellular receptors. Biochemically, adenosine inhibits adenylate cyclase via a "high" affinity receptor, and activates adenylate cyclase via a "low" affinity receptor. These receptors, called "A1" and "A2" respectively, show differing profiles for activation by adenosine analogs. Radioactive N6-cyclohexyladenosine binds selectively to the "high" affinity receptor. One major class of antagonists is known at adenosine receptors: the alkylxanthines, including caffeine and theophylline. Radioactive 1,3-diethyl-8-phenylxanthine, a particularly potent antagonist, appears to bind to both low and high affinity adenosine receptors. Behavioral, electrophysiological, and biochemical effects of alkylxanthines are consistent with the hypothesis that the central stimulatory actions of caffeine and theophylline are due in large part to antagonism of central adenosine receptors.
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U2 - 10.1016/0024-3205(81)90614-7
DO - 10.1016/0024-3205(81)90614-7
M3 - Article
C2 - 6114369
AN - SCOPUS:0019829170
SN - 0024-3205
VL - 28
SP - 2083
EP - 2097
JO - Life Sciences
JF - Life Sciences
IS - 19
ER -