Benzodiazepines: Relationship between pharmacological activity in the rat and in vivo receptor binding

T. Mennini; S. Cotecchia; S. Caccia; S. Garattini

doi:10.1016/0091-3057(82)90409-9

Benzodiazepines: Relationship between pharmacological activity in the rat and in vivo receptor binding

T. Mennini, S. Cotecchia, S. Caccia, S. Garattini

Istituto di Ricerche Farmacologiche "Mario Negri"

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

Abstract

When given at ED₅₀ antileptazol several benzodiazepines displace ³H-Diazepam bound in vivo to rat brain by about 50%, in spite of the differences between pharmacological potencies and metabolism. No displacement is found in cerebellum, even when the concentrations of displacing drugs are comparable. The possibility of the presence of multiple benzodiazepine receptors in brain and cerebellum is discussed in relation with their pharmacological activity.

Original language	English
Pages (from-to)	529-532
Number of pages	4
Journal	Pharmacology, Biochemistry and Behavior
Volume	16
Issue number	4
DOIs	https://doi.org/10.1016/0091-3057(82)90409-9
Publication status	Published - 1982

Keywords

Antileptazol activity
Anxiolytic effect
Benzodiazepine receptors
Camazepam
Clobazam
Diazepam
In vivo receptor binding
Oxazepam
Temazepam

ASJC Scopus subject areas

Biochemistry
Behavioral Neuroscience
Pharmacology

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10.1016/0091-3057(82)90409-9

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abstract = "When given at ED50 antileptazol several benzodiazepines displace 3H-Diazepam bound in vivo to rat brain by about 50%, in spite of the differences between pharmacological potencies and metabolism. No displacement is found in cerebellum, even when the concentrations of displacing drugs are comparable. The possibility of the presence of multiple benzodiazepine receptors in brain and cerebellum is discussed in relation with their pharmacological activity.",

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AU - Mennini, T.

AU - Cotecchia, S.

AU - Caccia, S.

AU - Garattini, S.

PY - 1982

Y1 - 1982

N2 - When given at ED50 antileptazol several benzodiazepines displace 3H-Diazepam bound in vivo to rat brain by about 50%, in spite of the differences between pharmacological potencies and metabolism. No displacement is found in cerebellum, even when the concentrations of displacing drugs are comparable. The possibility of the presence of multiple benzodiazepine receptors in brain and cerebellum is discussed in relation with their pharmacological activity.

AB - When given at ED50 antileptazol several benzodiazepines displace 3H-Diazepam bound in vivo to rat brain by about 50%, in spite of the differences between pharmacological potencies and metabolism. No displacement is found in cerebellum, even when the concentrations of displacing drugs are comparable. The possibility of the presence of multiple benzodiazepine receptors in brain and cerebellum is discussed in relation with their pharmacological activity.

KW - Antileptazol activity

KW - Anxiolytic effect

KW - Benzodiazepine receptors

KW - Camazepam

KW - Clobazam

KW - Diazepam

KW - In vivo receptor binding

KW - Oxazepam

KW - Temazepam

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Benzodiazepines: Relationship between pharmacological activity in the rat and in vivo receptor binding

Abstract

Keywords

ASJC Scopus subject areas

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