PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam

Kelvin W. Gee; Roberta E. Brinton; Henry I. Yamamura

doi:10.1016/0006-8993(83)91138-1

PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam

Kelvin W. Gee, Roberta E. Brinton, Henry I. Yamamura

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

23 Scopus citations

Abstract

PK 8165 and PK 9084 are two quinoline derivatives reported to interact with the benzodiazepine receptor and possess selective anxiolytic properties in vivo. In the present study we demonstrate that these two compounds antagonize the anticonvulsant effects of diazepam. In addition, in vitro binding studies indicate that both PK 8165 and PK 9084 interact competitively with [³H]flunitrazepam for brain benzodiazepine receptors. Based upon these findings, we propose the hypothesis that PK 8165 and PK 9084 act as partial agonists at the benzodiazepine receptor.

Original language	English (US)
Pages (from-to)	168-172
Number of pages	5
Journal	Brain Research
Volume	264
Issue number	1
DOIs	https://doi.org/10.1016/0006-8993(83)91138-1
State	Published - Mar 28 1983
Externally published	Yes

Keywords

(+)bicuculline
PK 8165
PK 9084
benzodiazepine receptor
benzodiazepine receptor antagonist
diazepam
quinoline derivatives
selective anxiolytic

ASJC Scopus subject areas

General Neuroscience
Molecular Biology
Clinical Neurology
Developmental Biology

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10.1016/0006-8993(83)91138-1

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title = "PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam",

abstract = "PK 8165 and PK 9084 are two quinoline derivatives reported to interact with the benzodiazepine receptor and possess selective anxiolytic properties in vivo. In the present study we demonstrate that these two compounds antagonize the anticonvulsant effects of diazepam. In addition, in vitro binding studies indicate that both PK 8165 and PK 9084 interact competitively with [3H]flunitrazepam for brain benzodiazepine receptors. Based upon these findings, we propose the hypothesis that PK 8165 and PK 9084 act as partial agonists at the benzodiazepine receptor.",

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T1 - PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam

AU - Gee, Kelvin W.

AU - Brinton, Roberta E.

AU - Yamamura, Henry I.

PY - 1983/3/28

Y1 - 1983/3/28

N2 - PK 8165 and PK 9084 are two quinoline derivatives reported to interact with the benzodiazepine receptor and possess selective anxiolytic properties in vivo. In the present study we demonstrate that these two compounds antagonize the anticonvulsant effects of diazepam. In addition, in vitro binding studies indicate that both PK 8165 and PK 9084 interact competitively with [3H]flunitrazepam for brain benzodiazepine receptors. Based upon these findings, we propose the hypothesis that PK 8165 and PK 9084 act as partial agonists at the benzodiazepine receptor.

AB - PK 8165 and PK 9084 are two quinoline derivatives reported to interact with the benzodiazepine receptor and possess selective anxiolytic properties in vivo. In the present study we demonstrate that these two compounds antagonize the anticonvulsant effects of diazepam. In addition, in vitro binding studies indicate that both PK 8165 and PK 9084 interact competitively with [3H]flunitrazepam for brain benzodiazepine receptors. Based upon these findings, we propose the hypothesis that PK 8165 and PK 9084 act as partial agonists at the benzodiazepine receptor.

KW - (+)bicuculline

KW - PK 8165

KW - PK 9084

KW - benzodiazepine receptor

KW - benzodiazepine receptor antagonist

KW - diazepam

KW - quinoline derivatives

KW - selective anxiolytic

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PK 8165 and PK 9084, two quinoline derivatives with anxiolytic properties, antagonize the anticonvulsant effects of diazepam

Abstract

Keywords

ASJC Scopus subject areas

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