Literature DB >> 6089246

ZK 91296, a partial agonist at benzodiazepine receptors.

E N Petersen, L H Jensen, T Honoré, C Braestrup, W Kehr, D N Stephens, H Wachtel, D Seidelman, R Schmiechen.   

Abstract

5-benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylate) is a potent and selective ligand for benzodiazepine (BZ) receptors. Biochemical investigations indicate that ZK 91296 may be a partial agonist at BZ receptors. Such partial agonism may explain to some extent why ZK 91296 needs higher BZ receptor occupancy than diazepam for the same effect against chemical convulsants and for behavioural effects. The lack of sedative effects, and the very potent inhibition of reflex epilepsy, spontaneous epilepsy and DMCM-induced seizures suggest, furthermore, that ZK 91296 may possess pharmacological selectivity for a particular type of BZ receptor interaction, perhaps including topographic as well as receptor subtype differentiation.

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Year:  1984        PMID: 6089246     DOI: 10.1007/bf00464788

Source DB:  PubMed          Journal:  Psychopharmacology (Berl)        ISSN: 0033-3158            Impact factor:   4.530


  39 in total

1.  Muscimol binding in rat brain: association with synaptic GABA receptors.

Authors:  K Beaumont; W S Chilton; H I Yamamura; S J Enna
Journal:  Brain Res       Date:  1978-06-09       Impact factor: 3.252

2.  Spiperone: a ligand of choice for neuroleptic receptors. 2. Regional distribution and in vivo displacement of neuroleptic drugs.

Authors:  P M Laduron; P F Janssen; J E Leysen
Journal:  Biochem Pharmacol       Date:  1978-02-01       Impact factor: 5.858

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Authors:  R S Chang; S H Snyder
Journal:  Eur J Pharmacol       Date:  1978-03-15       Impact factor: 4.432

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Journal:  Eur J Pharmacol       Date:  1968-09       Impact factor: 4.432

5.  Benzodiazepine receptors: differential interaction of benzodiazepine agonists and antagonists after photoaffinity labeling with flunitrazepam.

Authors:  H Möhler
Journal:  Eur J Pharmacol       Date:  1982-06-04       Impact factor: 4.432

6.  A water lick conflict paradigm using drug experienced rats.

Authors:  E N Petersen; J B Lassen
Journal:  Psychopharmacology (Berl)       Date:  1981       Impact factor: 4.530

7.  d-LSD binding to brain homogenates: possible relationship to serotonin receptors.

Authors:  J L Bennett; G K Aghajanian
Journal:  Life Sci       Date:  1974-12-01       Impact factor: 5.037

8.  Ethyl beta-carboline-3-carboxylate shows differential benzodiazepine receptor interaction.

Authors:  M Nielsen; C Braestrup
Journal:  Nature       Date:  1980-08-07       Impact factor: 49.962

9.  CGS 8216: receptor binding characteristics of a potent benzodiazepine antagonist.

Authors:  A J Czernik; B Petrack; H J Kalinsky; S Psychoyos; W D Cash; C Tsai; R K Rinehart; F R Granat; R A Lovell; D E Brundish; R Wade
Journal:  Life Sci       Date:  1982-01-25       Impact factor: 5.037

10.  Selective antagonists of benzodiazepines.

Authors:  W Hunkeler; H Möhler; L Pieri; P Polc; E P Bonetti; R Cumin; R Schaffner; W Haefely
Journal:  Nature       Date:  1981-04-09       Impact factor: 49.962

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  16 in total

1.  Safety signal withdrawal: a behavioural paradigm sensitive to both "anxiolytic" and "anxiogenic" drugs under identical experimental conditions.

Authors:  M H Thiébot; L Dangoumau; G Richard; A J Puech
Journal:  Psychopharmacology (Berl)       Date:  1991       Impact factor: 4.530

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

Authors:  P P De Deyn; R L Macdonald
Journal:  Br J Pharmacol       Date:  1988-09       Impact factor: 8.739

3.  Behavioural effects of the benzodiazepine receptor partial agonist RO 16-6028 in mice.

Authors:  C Belzung; R Misslin; E Vogel
Journal:  Psychopharmacology (Berl)       Date:  1989       Impact factor: 4.530

4.  The effect of the beta-carboline FG 7142 on the behaviour of male rats in a living cage: an ethological analysis of social and nonsocial behaviour.

Authors:  C H Beck; S J Cooper
Journal:  Psychopharmacology (Berl)       Date:  1986       Impact factor: 4.530

5.  Effect on hypothalamic self-stimulation of the novel beta-carbolines ZK 93 426 (a benzodiazepine receptor antagonist) and ZK 91 296 (a putative partial agonist).

Authors:  L J Herberg; A M Montgomery; S E File; S Pellow; D N Stephens
Journal:  J Neural Transm       Date:  1986       Impact factor: 3.575

6.  Trends in drug discrimination research analysed with a cross-indexed bibliography, 1984-1987.

Authors:  I P Stolerman; F Rasul; P J Shine
Journal:  Psychopharmacology (Berl)       Date:  1989       Impact factor: 4.530

7.  "Anxiolytic" and "anxiogenic" benzodiazepines and beta-carbolines: effects on aggressive and social behavior in rats and squirrel monkeys.

Authors:  E M Weerts; W Tornatzky; K A Miczek
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

8.  Beta-carbolines can enhance or antagonize the effects of punishment in mice.

Authors:  D N Stephens; W Kehr
Journal:  Psychopharmacology (Berl)       Date:  1985       Impact factor: 4.530

9.  Discriminative stimulus properties of beta-carbolines characterized as agonists and inverse agonists at central benzodiazepine receptors.

Authors:  D N Stephens; G T Shearman; W Kehr
Journal:  Psychopharmacology (Berl)       Date:  1984       Impact factor: 4.530

10.  Differential potentiation of GABAA receptor function by two stereoisomers of diimidazoquinazoline analogues.

Authors:  H K Im; W B Im; J F Pregenzer; J D Petke; B J Hamilton; D B Carter; P F Von Voigtlander; H C Hansen; M Kristiansen
Journal:  Br J Pharmacol       Date:  1992-10       Impact factor: 8.739

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