General Pharmacology and Neuropharmacology of Benzodiazepine Derivatives

Haefely, W.; Pieri, L.; Polc, P.; Schaffner, R.

doi:10.1007/978-3-642-67767-0_2

Cited by 114 publications

(33 citation statements)

References 825 publications

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“…However, a smaller dose of DZP inhibited the ulceration accompanying a slight increase of the activity. Smaller doses of benzodiazepines are known to increase locomotor activity in mice (19). SLD is available as a neuroleptic as well as an antidepressant.…”

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confidence: 99%

Effects of Psychotropic Drugs on the Development of Activity-Stress Ulcer in Rats

Hara

Ogawa

1984

Japanese Journal of Pharmacology

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confidence: 99%

Effects of Psychotropic Drugs on the Development of Activity-Stress Ulcer in Rats

Hara

Ogawa

1984

Japanese Journal of Pharmacology

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“…The benzodiazepines, in addition to their anxiolytic and anticonvulsant properties, have sedative effects (Fink & Swinyard, 1962;Haefely et al, 1981), and the use of these drugs is associated with the development of tolerance and dependence (Allgulander, 1978). As a result there has been a continuing effort to develop selective, non-sedative anxiolytic drugs.…”

Section: Introductionmentioning

confidence: 99%

Effects of non‐sedative anxiolytic drugs on responses to GABA and on diazepam‐induced enhancement of these responses on mouse neurones in cell culture

Deyn

Macdonald

1988

British J Pharmacology

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1 Intracellular microelectrode recording techniques were performed on mouse spinal cord and cerebral hemisphere neurones grown in primary dissociated cell culture. The effects of several anxiolytics applied by local pressure ejection on responses to y-aminobutyric acid (GABA) evoked by iontophoresis were investigated. Responses to GABA were depolarizing since intracellular chloride ion concentration was increased by injection from potassium chloride (3M)-filled recording micropipettes and neurones were held at large negative membrane potentials (-70 to -90mV). The agents studied were six 'non-sedative anxiolytics ', CL 218, 1,2,4-triazolo(4,3-b) pyridazine), PK 8165 (2-phenyl-442-(4-piperidinyl)5]decane-7,9-dione), and two sedative anxiolytics, diazepam and zopiclone ([6-5-2 Direct effects on responses to GABA were studied for all drugs applied in varying concentrations. For the drugs which significantly altered responses to GABA, the effects of the benzodiazepine receptor antagonists Ro 15-1788 (ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo4H-imidazo(1,5a) (1,4)benzodiazepine-3-carboxylate) and CGS 8216 (2-phenylpyrazolo(4,3-c)-quinolin-3(5H-one) were evaluated. For

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“…GABA is the predominant inhibitory neurotransmitter of the mammalian central nervous system (1)(2)(3). The GABAA receptor contains complex multisubunits that bind GABA, -3-carbolines, and benzodiazepines with high affinity (4,5) and a chloride ion channel (6).…”

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Cloning and expression of cDNA for human diazepam binding inhibitor, a natural ligand of an allosteric regulatory site of the gamma-aminobutyric acid type A receptor.

Gray¹,

Glaister²,

Seeburg³

et al. 1986

Proc. Natl. Acad. Sci. U.S.A.

125

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Diazepam binding inhibitor (DBI) is a protein that displaces ligands bound to the f-carbolmne/benzodiazepine recognition site, an allosteric modulatory site of the type A -aminobutyric acid receptor complex. An incomplete rat cDNA clone coding for DBI was isolated. This rat sequence was utilized to identify a cDNA done that encoded the entire 104 residues of human DBI. This sequence was engineered for expression in E. coli, and recombinant DBI exhibits identical biochemical and antigenic characteristics of natural human DBI. DBI is encoded by a multigene family of at least five members, but a single gene appears to account for the majority ofDBI expression. DBI is expressed in a tissue-specific manner. Expression is found in central nervous system tissues and appears to extend to peripheral tissues rich in the peripheral type of high-affinity benzodiazepine recognition sites. The role of these sites and DBI in adrenal gland, testis, and kidney remains to be determined. MATERIALS AND METHODS Isolation of DBI cDNA. Two synthetic oligonucleotide probes were designed to code for the partial amino acid sequence determined for rat DBI (9). The DNA 5'-ATGCTG-TTCATCTACTCCCACTTCAAGCAGGCTACTGTCGGC was designed to encode the sequence Met-Leu-Phe-Ile-TyrSer-His-Phe-Lys-Gln-Ala-Thr-Val-Gly, and the DNA 5'-GACGTCAACACTGACAGACCTGGCCTGCTGGAC-CTGAAGGGCAAG was designed for the sequence Asp-ValAsn-Thr-Asp-Arg-Pro-Gly-Leu-Leu-Asp-Leu-Lys-Gly-Lys. The two probes were labeled with [y-32P]ATP (Amersham) and T4 polynucleotide kinase (New England Biolabs). The radiolabeled probes were utilized to screen (13) a rat hypothalamic cDNA library (14) in phage XgtlO (15). A library of 640,000 phage was grown on sixteen 15-cm plates, and duplicate nitrocellulose filters were hybridized independently with the two probes. Hybridization was performed at reduced stringency in 20% formamide containing 5 x NaCl/Cit (lx NaCl/Cit is 0.15 M sodium chloride/0.015 M sodium citrate), 1% polyvinylpyrrolidone (Sigma), 1% Ficoll, 1% bovine serum albumin (Sigma, fraction V), 0.05 M sodium phosphate (pH 6.5), and 50 ng of sonicated salmon sperm DNA (Sigma) per ml. After the overnight hybridization at 420C, filters were washed extensively at 420C in 0.2X NaCl/Cit containing 0.1% sodium dodecyl sulfate. Numerous plaques were identified that hybridized with both synthetic DNA probes. Phage DNA was isolated from several purified plaques (13). Three different rat cDNA inserts were isolated and sequenced by the dideoxy chain-termination technique (16 7547The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked "advertisement" in accordance with 18 U.S.C. §1734 solely to indicate this fact.

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General Pharmacology and Neuropharmacology of Benzodiazepine Derivatives

Cited by 114 publications

References 825 publications

Effects of Psychotropic Drugs on the Development of Activity-Stress Ulcer in Rats

Effects of Psychotropic Drugs on the Development of Activity-Stress Ulcer in Rats

Effects of non‐sedative anxiolytic drugs on responses to GABA and on diazepam‐induced enhancement of these responses on mouse neurones in cell culture

Cloning and expression of cDNA for human diazepam binding inhibitor, a natural ligand of an allosteric regulatory site of the gamma-aminobutyric acid type A receptor.

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