Critical reviews and theoretical articles
A review of recently-developed ligands for neuronal benzodiazepine receptors and their pharmacological activities

https://doi.org/10.1016/0278-5846(92)90099-ZGet rights and content

Abstract

Gardner, Colin R: A Review of Recently-developed Ligands for Neuronal Benzodiazepine Receptors and Their Pharmacological Activities. Prog. Neuro-Psychopharmacol. & Biol. Psychiat. 1992, 16(6): 755–781.

  • 1.

    1. There has recently been a large increase in the number of new benzodiazepine receptor ligands, some with benzodiazepine structures, but many with other chemical structures.

  • 2.

    2. The pharmacological activities of these ligands have been interpreted on the basis of a continuum of efficacy ranging from full agonist through different degrees of partial agonism to antagonist and through partial to full inverse agonists.

  • 3.

    3. Inconsistencies with this hypothesis are considered in terms of alternative hypotheses, particularly the existence of functionally separable receptor subtypes.

  • 4.

    4. The potential of partial agonists as non-sedative anxiolytic agents with reduced potential of dependence and of weak partial inverse agonists as pro-cognitive agents is discussed.

  • 5.

    5. A pharmacophore for benzodiazepine receptors is proposed and supporting evidence presented.

References (41)

  • S. Arbilla et al.

    Differential intrinsic activities at ω receptor subtypes of zolpidem and other selective ω1 (BZ1) receptor ligands

  • T.M. Bare et al.

    Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents

    J.Med.Chem.

    (1989)
  • R.M.J. Deacon et al.

    RU33965: A novel benzodiazepine receptor ligand with partial inverse agonist activity

    Psychopharmacol.

    (1990)
  • R.M.J. Deacon et al.

    Investigation of potential cognitive enhancing properties of RU33965, a benzodiazepine receptor partial inverse agonist

    Psychopharmacol.

    (1990)
  • R.M.J. Deacon et al.

    Effects of selected imidazopyrimidine ligands for benzodiazepine receptors in rodent models of anxiety and behavioural impairment

    Drug Dev.Res.

    (1991)
  • C.R. Gardner

    Discriminative stimulus properties of the non-sedative anxiolytic benzodiazepine receptor ligand RU32698

    Drug Dev.Res.

    (1989)
  • C.R. Gardner et al.

    Bidirectional efficacy at benzodiazepine receptors of a series of imidazopyrimidines illustrated in drug discrimination studies

    Drug Dev.Res.

    (1991)
  • C.R. Gardner et al.

    The relationship between structure and efficacy at central benzodiazepine receptors for a series of imidazopyrimidines and imidazoquinolines

    Drug Dev.Res.

    (1991)
  • A.P. Guy et al.

    An interaction between cholinergic and benzodiazepine receptor-mediated systems observed in a water maze model

  • L.H. Jensen et al.

    Oxadiazolylimidazobenzodiazepines, a new class of benzodiazepine receptor ligands

  • Cited by (0)

    View full text