Assessment of benzodiazepine receptor heterogeneity in vivo: apparent pA2 and pKB analyses from behavioral studies

@article{Rowlett1996AssessmentOB,
  title={Assessment of benzodiazepine receptor heterogeneity in vivo: apparent pA2 and pKB analyses from behavioral studies},
  author={J. K. Rowlett and W. Woolverton},
  journal={Psychopharmacology},
  year={1996},
  volume={128},
  pages={1-16}
}
Abstract The purpose of this review was to establish in vivo apparent pA2 and pKB values for antagonism of the discriminative stimulus effects of benzodiazepine ligands, and to compare these values to those obtained from other behavioral procedures. Articles were chosen from the Medline data base from January 1976 to August 1995. This literature consisted of studies with flumazenil (Ro 15–1788) as the antagonist, as well as other benzodiazepine ligands (β-carbolines, CGS 9896, CGS 8216). The… Expand
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Drugs that bind to benzodiazepine recognition sites of g-aminobutyric acid type A receptor complexes may function as agonists in some behavioral assays and as antagonists in other behavioral assays.Expand
Apparent pA2 values of benzodiazepine antagonists and partial agonists in monkeys.
  • C. Paronis, J. Bergman
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1999
TLDR
The results indicate that in vivo pA(2) values may be determined for benzodiazepine-site ligands, e. Expand
Antagonism of triazolam self-administration in rhesus monkeys responding under a progressive-ratio schedule: In vivo apparent pA2 analysis.
TLDR
These findings were not entirely consistent with blockade of α1GABAA receptors and are consistent with the possibility of α2GabAA and/or α3GAB AA subtype involvement in antagonism of the reinforcing effects of triazolam. Expand
Antagonism of the discriminative stimulus effects of positive gamma-aminobutyric acid(A) modulators in rhesus monkeys discriminating midazolam.
TLDR
Slopes of Schild plots obtained with flumazenil and Ro 15-4513 support the notion that a single benzodiazepine receptor subtype mediates the effects of midazolam, triazol am, or diazepam, while beta-CCE and midAZolam do not appear to interact in a simple, competitive manner. Expand
Triazolam discrimination in squirrel monkeys distinguishes high-efficacy agonists from other benzodiazepines and non-benzodiazepine drugs
TLDR
BZ agonists can be distinguished on the basis of substitution for triazolam and, thus, the triazlam discrimination may be a useful tool for identifying compounds of different efficacy at BZ receptors. Expand
Discriminative stimulus effects of ethyl-β-carboline-3-carboxylate at two training doses in rats
TLDR
The results indicated that the stimulus effects of the high dose of β-CCE appeared consistent with mediation by the drug’s partial inverse agonist effects at BZ receptors, although the discriminative stimulus effects at the lower training dose appeared to be relatively non-specific. Expand
Discriminative Stimulus Effects of Drugs Acting at GABAA Receptors Differential Profiles and Receptor Selectivity
TLDR
BZ1 (omega1)-selective drugs substitute for the discriminative stimulus produced by chlordiazepoxide only partially and at sedative doses, consistent with the view that sedative effects of BZ(omega) receptor agonists are mediated by the BZ1(omeg1) receptor subtype, whereas the discrim inative stimulusproduced by chlordsiazepoxide may be produced by activity at the Bz2(omego2) subtype. Expand
Discriminative stimulus effects of zolpidem in squirrel monkeys: comparison with conventional benzodiazepines and sedative-hypnotics.
TLDR
The view that zolpidem's selectivity for the alpha1-subunit of the BZ/gamma-aminobutyric acid(A) receptor complex confers a distinctive profile of interoceptive effects that overlaps partially with those of typical BZs but not withThose of barbiturates is supported. Expand
Zolpidem generalization and antagonism in male and female cynomolgus monkeys trained to discriminate 1.0 or 2.0 g/kg ethanol.
TLDR
Ethanol and zolpidem share similar discriminative stimulus effects most likely through GABA(A) receptors that contain alpha(1) subunits, however, antagonism by Ro15-4513 of zolPidem generalization from the lower training dose of ethanol (1.0 g/kg) may involve additional zol pidem-sensitive GABA(B) receptor subtypes (e.g., alpha(2/3) and alpha(5)). Expand
Anti-conflict effects of benzodiazepines in rhesus monkeys: relationship with therapeutic doses in humans and role of GABAA receptors
TLDR
Evidence is provided that anxiolytic-like effects of BZs can occur with relatively low intrinsic efficacy at GABAA receptors and are reduced by α1GABAA receptor selectivity. Expand
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CGS 8216, a pyrazoloquinolinone benzodiazepine receptor ligand, was administered alone and concomitantly with diazepam in order to assess its agonist and diazepam-antagonist properties on severalExpand
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