Adenosine receptors in brain membranes

Binding of N6-cyclohexyl[3H]adenosine and 1,3-diethyl-8-[3H]phenylxanthine

R. F. Bruns, J. W. Daly, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

N6-Cyclohexyl[3H]adenosine ([3H]CHA) and 1,3-diethyl-8-[3H]phenylxanthine ([3H]DPX) bind to adenosine receptors in brain membranes. The agonist [3H]CHA has high affinity in both bovine and guinea pig brain (Kd, 0.7 nM and 6 nM, respectively). [3H]CHA binding kinetics are slow (dissociation t1/2; 60 min); binding is much higher at 25°C than at 0°C and is inhibited by guanine nucleotides. Potencies of nucleosides and xanthines in competing for [3H]CHA sites indicate that specific binding is entirely to A1 adenosine receptors. In bovine brain, the antagonist [3H]DPX exhibits high-affinity binding (Kd, 5 nM) to the same A1 receptors that bind [3H]CHA. Binding kinetics are rapid (dissociation t1/2, 1 min), and binding is moderately higher at 0°C than at 25°C. In guinea pig brain, [3H]DPX binding has only moderate affinity (Kd, 50 nM), and about 60% of specific binding is to sites that resemble A2 adenosine receptors.

Original languageEnglish (US)
Pages (from-to)5547-5551
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Volume77
Issue number9 II
StatePublished - 1980

Fingerprint

Purinergic P1 Receptors
Membranes
Brain
Guinea Pigs
Xanthines
Adenosine A2 Receptors
Adenosine A1 Receptors
Guanine Nucleotides
Nucleosides
N(6)-cyclohexyladenosine
1,3-diethyl-8-phenylxanthine

ASJC Scopus subject areas

  • General
  • Genetics

Cite this

@article{daeecc1929224296a5e6a9fd222f9676,
title = "Adenosine receptors in brain membranes: Binding of N6-cyclohexyl[3H]adenosine and 1,3-diethyl-8-[3H]phenylxanthine",
abstract = "N6-Cyclohexyl[3H]adenosine ([3H]CHA) and 1,3-diethyl-8-[3H]phenylxanthine ([3H]DPX) bind to adenosine receptors in brain membranes. The agonist [3H]CHA has high affinity in both bovine and guinea pig brain (Kd, 0.7 nM and 6 nM, respectively). [3H]CHA binding kinetics are slow (dissociation t1/2; 60 min); binding is much higher at 25°C than at 0°C and is inhibited by guanine nucleotides. Potencies of nucleosides and xanthines in competing for [3H]CHA sites indicate that specific binding is entirely to A1 adenosine receptors. In bovine brain, the antagonist [3H]DPX exhibits high-affinity binding (Kd, 5 nM) to the same A1 receptors that bind [3H]CHA. Binding kinetics are rapid (dissociation t1/2, 1 min), and binding is moderately higher at 0°C than at 25°C. In guinea pig brain, [3H]DPX binding has only moderate affinity (Kd, 50 nM), and about 60{\%} of specific binding is to sites that resemble A2 adenosine receptors.",
author = "Bruns, {R. F.} and Daly, {J. W.} and Snyder, {Solomon H}",
year = "1980",
language = "English (US)",
volume = "77",
pages = "5547--5551",
journal = "Proceedings of the National Academy of Sciences of the United States of America",
issn = "0027-8424",
number = "9 II",

}

TY - JOUR

T1 - Adenosine receptors in brain membranes

T2 - Binding of N6-cyclohexyl[3H]adenosine and 1,3-diethyl-8-[3H]phenylxanthine

AU - Bruns, R. F.

AU - Daly, J. W.

AU - Snyder, Solomon H

PY - 1980

Y1 - 1980

N2 - N6-Cyclohexyl[3H]adenosine ([3H]CHA) and 1,3-diethyl-8-[3H]phenylxanthine ([3H]DPX) bind to adenosine receptors in brain membranes. The agonist [3H]CHA has high affinity in both bovine and guinea pig brain (Kd, 0.7 nM and 6 nM, respectively). [3H]CHA binding kinetics are slow (dissociation t1/2; 60 min); binding is much higher at 25°C than at 0°C and is inhibited by guanine nucleotides. Potencies of nucleosides and xanthines in competing for [3H]CHA sites indicate that specific binding is entirely to A1 adenosine receptors. In bovine brain, the antagonist [3H]DPX exhibits high-affinity binding (Kd, 5 nM) to the same A1 receptors that bind [3H]CHA. Binding kinetics are rapid (dissociation t1/2, 1 min), and binding is moderately higher at 0°C than at 25°C. In guinea pig brain, [3H]DPX binding has only moderate affinity (Kd, 50 nM), and about 60% of specific binding is to sites that resemble A2 adenosine receptors.

AB - N6-Cyclohexyl[3H]adenosine ([3H]CHA) and 1,3-diethyl-8-[3H]phenylxanthine ([3H]DPX) bind to adenosine receptors in brain membranes. The agonist [3H]CHA has high affinity in both bovine and guinea pig brain (Kd, 0.7 nM and 6 nM, respectively). [3H]CHA binding kinetics are slow (dissociation t1/2; 60 min); binding is much higher at 25°C than at 0°C and is inhibited by guanine nucleotides. Potencies of nucleosides and xanthines in competing for [3H]CHA sites indicate that specific binding is entirely to A1 adenosine receptors. In bovine brain, the antagonist [3H]DPX exhibits high-affinity binding (Kd, 5 nM) to the same A1 receptors that bind [3H]CHA. Binding kinetics are rapid (dissociation t1/2, 1 min), and binding is moderately higher at 0°C than at 25°C. In guinea pig brain, [3H]DPX binding has only moderate affinity (Kd, 50 nM), and about 60% of specific binding is to sites that resemble A2 adenosine receptors.

UR - http://www.scopus.com/inward/record.url?scp=0007761382&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0007761382&partnerID=8YFLogxK

M3 - Article

VL - 77

SP - 5547

EP - 5551

JO - Proceedings of the National Academy of Sciences of the United States of America

JF - Proceedings of the National Academy of Sciences of the United States of America

SN - 0027-8424

IS - 9 II

ER -