Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680

Ge Zhang, Paul H. Franklin, Thomas F. Murray

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

Focal injection of the adenosine A2A receptor agonist CGS21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethyl-carboxamidoadenosine) in the rat prepiriform cortex produced a reduction in the severity of bicuculline methiodide-induced motor seizures. The anticonvulsant effect of CGS21680 exhibited dose-dependency and modest potency (ED50=605±47 pmol/rat). Pharmacological characterization of the anticonvulsant response in the prepiriform cortex revealed a significant correlation between the potency of adenosine analogs as anticonvulsants and their respective affinities for adenosine A1 receptors in vitro. These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the anticonvulsant activity of this compound in the rat prepiriform cortex.

Original languageEnglish
Pages (from-to)239-243
Number of pages5
JournalEuropean Journal of Pharmacology
Volume255
Issue number1-3
DOIs
StatePublished - Apr 1 1994
Externally publishedYes

Fingerprint

Adenosine A1 Receptors
Anticonvulsants
Adenosine A2 Receptor Agonists
Adenosine
Seizures
Pharmacology
Injections
2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
Piriform Cortex

All Science Journal Classification (ASJC) codes

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680. / Zhang, Ge; Franklin, Paul H.; Murray, Thomas F.

In: European Journal of Pharmacology, Vol. 255, No. 1-3, 01.04.1994, p. 239-243.

Research output: Contribution to journalArticle

@article{dc5e36f49ee24593bfc5a3b0ede2d322,
title = "Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680",
abstract = "Focal injection of the adenosine A2A receptor agonist CGS21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethyl-carboxamidoadenosine) in the rat prepiriform cortex produced a reduction in the severity of bicuculline methiodide-induced motor seizures. The anticonvulsant effect of CGS21680 exhibited dose-dependency and modest potency (ED50=605±47 pmol/rat). Pharmacological characterization of the anticonvulsant response in the prepiriform cortex revealed a significant correlation between the potency of adenosine analogs as anticonvulsants and their respective affinities for adenosine A1 receptors in vitro. These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the anticonvulsant activity of this compound in the rat prepiriform cortex.",
author = "Ge Zhang and Franklin, {Paul H.} and Murray, {Thomas F.}",
year = "1994",
month = "4",
day = "1",
doi = "10.1016/0014-2999(94)90104-X",
language = "English",
volume = "255",
pages = "239--243",
journal = "European Journal of Pharmacology",
issn = "0014-2999",
publisher = "Elsevier",
number = "1-3",

}

TY - JOUR

T1 - Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680

AU - Zhang, Ge

AU - Franklin, Paul H.

AU - Murray, Thomas F.

PY - 1994/4/1

Y1 - 1994/4/1

N2 - Focal injection of the adenosine A2A receptor agonist CGS21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethyl-carboxamidoadenosine) in the rat prepiriform cortex produced a reduction in the severity of bicuculline methiodide-induced motor seizures. The anticonvulsant effect of CGS21680 exhibited dose-dependency and modest potency (ED50=605±47 pmol/rat). Pharmacological characterization of the anticonvulsant response in the prepiriform cortex revealed a significant correlation between the potency of adenosine analogs as anticonvulsants and their respective affinities for adenosine A1 receptors in vitro. These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the anticonvulsant activity of this compound in the rat prepiriform cortex.

AB - Focal injection of the adenosine A2A receptor agonist CGS21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethyl-carboxamidoadenosine) in the rat prepiriform cortex produced a reduction in the severity of bicuculline methiodide-induced motor seizures. The anticonvulsant effect of CGS21680 exhibited dose-dependency and modest potency (ED50=605±47 pmol/rat). Pharmacological characterization of the anticonvulsant response in the prepiriform cortex revealed a significant correlation between the potency of adenosine analogs as anticonvulsants and their respective affinities for adenosine A1 receptors in vitro. These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the anticonvulsant activity of this compound in the rat prepiriform cortex.

UR - http://www.scopus.com/inward/record.url?scp=0028178137&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0028178137&partnerID=8YFLogxK

U2 - 10.1016/0014-2999(94)90104-X

DO - 10.1016/0014-2999(94)90104-X

M3 - Article

VL - 255

SP - 239

EP - 243

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 1-3

ER -