PMID: 2104987Jan 1, 1990Paper

Acute reversal of flunitrazepam effects by Ro 15-1788 and Ro 15-3505: inverse agonism, tolerance, and rebound

Psychopharmacology
V GentilJ M Singer

Abstract

A phase 1 double blind crossover comparison of a new benzodiazepine antagonist (Ro 15-3505) with Ro 15-1788 and placebo, in the reversal of sedative and psychophysiological effects of single IV doses of flunitrazepam (2 mg), was carried out in 12 normal volunteers. The antagonists were equally effective, leading to full reversal of all effects with a potency ratio of approximately 2.5 mg Ro 15-1788 for 1 mg Ro 15-3505. Inverse agonism, in the form of unpleasant feelings and symptoms, was reported by all subjects following Ro 15-3505 but none after Ro 15-1788. Adaptational phenomena such as acute tolerance and rebound of sedative effects of flunitrazepam were also detected and their potential implications are discussed.

References

Jul 1, 1975·Electroencephalography and Clinical Neurophysiology·S Soltysik
Nov 1, 1978·Electroencephalography and Clinical Neurophysiology·G S RichardsonM M Mitler
Apr 1, 1975·British Journal of Clinical Pharmacology·M H GreenwoodG Curzon
Jun 1, 1989·Journal of Clinical Psychopharmacology·V GentilJ M Singer
Jan 1, 1985·Neuroscience and Biobehavioral Reviews·S E File
Jan 1, 1985·Pharmacopsychiatry·W Haefely
Jan 1, 1986·Psychopharmacology·S E File, S Pellow
Jan 1, 1972·Psychopharmacologia·A J Bond, M H Lader
Jan 1, 1983·Psychopharmacology·E H EllinwoodD W Molter
Jan 1, 1983·Journal of Psychoactive Drugs·W Haefely
Jan 1, 1983·Psychopharmacology·C Gorenstein, V Gentil
Apr 9, 1981·Nature·W HunkelerW Haefely
Oct 1, 1984·British Journal of Clinical Pharmacology·I GathH Hadad
Oct 1, 1982·Neuropharmacology·S E FileD J Nutt
Sep 1, 1955·Journal of Abnormal Psychology·J E DOPPELT, W L WALLACE

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Citations

Jan 1, 1991·Psychopharmacology·H V Curran
Feb 1, 1996·Progress in Neuro-psychopharmacology & Biological Psychiatry·G GriebelR J Blanchard
Jan 27, 1998·Pharmacology, Biochemistry, and Behavior·M D Schechter
Feb 26, 1998·Pharmacology, Biochemistry, and Behavior·S E ColdwellD S Ramsay
May 5, 2001·Pharmacology & Therapeutics·J J SandfordD J Nutt
Aug 29, 1998·Behavioural Brain Research·G G BerntsonJ T Cacioppo
Aug 7, 1998·Journal of Psychopharmacology·M A BernikA H Vieira Filho
Jan 1, 1991·Journal of Psychopharmacology·M A BernikV Gentil
Mar 1, 2007·Indian Journal of Otolaryngology and Head and Neck Surgery : Official Publication of the Association of Otolaryngologists of India·Nitin AnandRajni Prasad
Feb 1, 1992·The British Journal of Psychiatry : the Journal of Mental Science·D Nutt, C Lawson

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