Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680

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

doi:10.1016/0014-2999(94)90104-X

Activation of adenosine A₁ receptors underlies anticonvulsant effect of CGS21680

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

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

Abstract

Focal injection of the adenosine A_2A 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 language	English (US)
Pages (from-to)	239-243
Number of pages	5
Journal	European Journal of Pharmacology
Volume	255
Issue number	1-3
DOIs	https://doi.org/10.1016/0014-2999(94)90104-X
State	Published - Apr 1 1994
Externally published	Yes

All Science Journal Classification (ASJC) codes

Pharmacology

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@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.}",

note = "Funding Information: This work was supported by U.S. Public Health Service Grant NS-23227 to T.F.M. and Sigma Xi Grant-in-Aid research award to G.Z.",

year = "1994",

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

AU - Zhang, Ge

AU - Franklin, Paul H.

AU - Murray, Thomas F.

N1 - Funding Information: This work was supported by U.S. Public Health Service Grant NS-23227 to T.F.M. and Sigma Xi Grant-in-Aid research award to G.Z.

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.

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