Antagonism of benzodiazepine binding in rat and human brain by antiliriumR

K. V. Speeg; Sherry Wang; George R. Avant; M. Lawrence Berman; Steven Schenker

doi:10.1016/0024-3205(79)90003-1

Antagonism of benzodiazepine binding in rat and human brain by antilirium^R

K. V. Speeg, Sherry Wang, George R. Avant, M. Lawrence Berman, Steven Schenker

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

9 Scopus citations

Abstract

Physostigmine (Antilirium^R) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits ³H-diazepam and ³H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its "receptor" such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism.

Original language	English (US)
Pages (from-to)	1345-1350
Number of pages	6
Journal	Life Sciences
Volume	24
Issue number	15
DOIs	https://doi.org/10.1016/0024-3205(79)90003-1
State	Published - Apr 9 1979
Externally published	Yes

ASJC Scopus subject areas

Biochemistry, Genetics and Molecular Biology(all)
Pharmacology, Toxicology and Pharmaceutics(all)

Access to Document

10.1016/0024-3205(79)90003-1

Cite this

@article{51cf9e5a817544b2be75dadd13b065a6,

title = "Antagonism of benzodiazepine binding in rat and human brain by antiliriumR",

abstract = "Physostigmine (AntiliriumR) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits 3H-diazepam and 3H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its {"}receptor{"} such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism.",

author = "Speeg, {K. V.} and Sherry Wang and Avant, {George R.} and {Lawrence Berman}, M. and Steven Schenker",

note = "Funding Information: research was supported by USPHS grants AA00267 and RR05424 . K .V . Speeg, and S . Schenker are recipients of Veterans Administration Career Develop- Awards .",

year = "1979",

month = apr,

day = "9",

doi = "10.1016/0024-3205(79)90003-1",

language = "English (US)",

volume = "24",

pages = "1345--1350",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "15",

}

TY - JOUR

T1 - Antagonism of benzodiazepine binding in rat and human brain by antiliriumR

AU - Speeg, K. V.

AU - Wang, Sherry

AU - Avant, George R.

AU - Lawrence Berman, M.

AU - Schenker, Steven

N1 - Funding Information: research was supported by USPHS grants AA00267 and RR05424 . K .V . Speeg, and S . Schenker are recipients of Veterans Administration Career Develop- Awards .

PY - 1979/4/9

Y1 - 1979/4/9

N2 - Physostigmine (AntiliriumR) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits 3H-diazepam and 3H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its "receptor" such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism.

AB - Physostigmine (AntiliriumR) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits 3H-diazepam and 3H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its "receptor" such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism.

UR - http://www.scopus.com/inward/record.url?scp=0018372014&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0018372014&partnerID=8YFLogxK

U2 - 10.1016/0024-3205(79)90003-1

DO - 10.1016/0024-3205(79)90003-1

M3 - Article

C2 - 39204

AN - SCOPUS:0018372014

VL - 24

SP - 1345

EP - 1350

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

IS - 15

ER -

Antagonism of benzodiazepine binding in rat and human brain by antilirium^R

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this