GABA(A)-receptor subtypes: Clinical efficacy and selectivity of benzodiazepine site ligands

Annals of Medicine

Volumn 29, Issue 4, 1997, Pages 275-282

  Korpi, Esa R ^a   Mattila, Mauri J ^b   Wisden, William ^c   Lüddens, Hartmut ^d  

^a UNIVERSITY OF TURKU   (Finland)

^b UNIVERSITY OF HELSINKI   (Finland)

^c MRC LABORATORY OF MOLECULAR BIOLOGY   (United Kingdom)

^d JOHANNES GUTENBERG UNIVERSITY   (Germany)

Author keywords

Anxiety; Benzodiazepines; GABA(A) receptor; Partial agonism; Sleep induction; Subtype selectivity

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; ANESTHETIC AGENT; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE DERIVATIVE; BENZODIAZEPINE RECEPTOR; HYPNOTIC AGENT; LIGAND; NEUROTRANSMITTER RECEPTOR; RECEPTOR SUBTYPE;

BINDING SITE; BRAIN; COGNITION; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; REVIEW; SEDATION; SIDE EFFECT; TRANQUILIZING ACTIVITY;

EID: 0030758836     PISSN: 07853890     EISSN: None     Source Type: Journal    
DOI: 10.3109/07853899708999348     Document Type: Review

References (26)

1. A receptor subunits. Trends Pharmacol Sci 1991; 12: 49-51.
2. A receptor channels: from subunits to functional entities. Curr Opin Neurobiol 1992; 2: 263-9.
3. A receptor channels. Annu Rev Neurosci 1994; 17: 569-602.
4. A/ benzodiazepine receptor heterogeneity. J Psychiat Res 1995; 29: 77-94.
5. A receptor research. Synapse 1995; 21: 189-274.
6. A receptor subtypes. Pharmacol Rev 1995; 47: 181-234.
7. A receptors. Biochem J 1995; 310: 1-9.
8. A receptors: pharmacology, behavioural roles, and motor disorders. Neuroscientist 1996; 2: 15-23.
9. A-receptor subtypes really occur in the brain? Trends Neurosci 1996; 19: 139-43.
10. Ferry G. Cloned: the key to a tranquil brain. New Scientist 1937; 6: 26-7.
11. Gardner CR, Tully WR, Hedgecock CJR. The rapidly expanding range of neuronal benzodiazepine receptor ligands. Prog Neurobiol 1993; 40: 1-61.
12. Hunkeler W, Möhler H, Pieri L, et al. Selective antagonists of benzodiazepines. Nature 1981; 290: 514-6.
13. Lamb RJ, Griffiths RR. Effects of repeated Ro15-788 administration in benzodiazepine-dependent baboons. Eur J Pharmacol 1985; 110: 257-61.
14. Buck KJ, Heim H, Harris RA. Reversal of alcohol dependence and tolerance by a single administration of flumazenil. J Pharmacol Exp Ther 1991; 257: 984-9.
15. Harrisonread PE, Tyrer P, Lawson E, Lacks S, Fernades C, File S. Flumazenil-precipitated panic and dysforia in patients dependent on benzodiazepines - a possible aid to abstinence. J Psychopharmacol 1996; 10: 89-97.
16. Bonetti EP, Burkard WP, Gabl M, et al. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav 1989; 31: 733-49.
17. Martin JR, Pieri L, Bonetti EP, et al. Ro 16-6028: a novel anxiolytic acting as a partial agonist at the benzodiazepine receptor. Pharmacopsychiatry 1988; 21: 360-2.
18. A receptors. J Pharmacol Exp Ther 1993; 266: 1018-28.
19. A receptors. Eur J Pharmacol - Mol Pharmacol Sect 1993; 244: 29-35.
20. Lader M Rebound insomnia and newer hypnotics. Psychopharmacology 1992; 108: 248-55.
21. Varhe A. Interactions of Triazolam with Inhibitors of CYP3A4 enzymes (Doctoral thesis). Helsinki: University of Helsinki, 1996.
22. Stephens DN, Schneider HH, Kehr W, et al. Abecarnil, a metabolically stable, anxioselective β-carboline acting at benzodiazepine receptors. J Pharmacol Exp Ther 1990; 253: 334-43.
23. Ballenger JC, McDonald S, Noyes R, et al. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist, abecarnil (ZK 112-19), in generalized anxiety disorder. Adv Biochem Psychopharmacol 1992; 47: 431-47.
24. Duka T, Shutt B, Krause W, et al. Human studies on abecarnil, a new β-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. Br J Clin Pharmacol 1993; 35: 386-94.
25. Salva P, Costa J. Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications. Clin Pharmacokinet 1995; 29: 142-53.
26. Criswell HE, Simson PE, Duncan GE, et al. Molecular basis for regionally specific action of ethanol on γ-amino-butyric acidA receptors: generalization to other ligand-gated ion channels. J Pharmacol Exp Ther 1993; 267: 522-37.