Clonazepam selectively increases saccharin ingestion in a two-choice test. Imidazopyridines as a tool for the characterization of benzodiazepine receptors: a proposal for a pharmacological classification as omega receptor subtypes. Specificity within the GABAA receptor supramolecular complex: a consideration of the new omega 1-receptor selective imidazopyridine hypnotic zolpidem. Distribution of central omega 1 (benzodiazepine1) and omega 2 (benzodiazepine2) receptor subtypes in the monkey and human brain. An autoradiographic study with [3H]flunitrazepam and the omega 1 selective ligand [3H]zolpidem. The interaction between zolpidem and beta-CMC: a clue to the identification of receptor sites involved in the sedative effect of zolpidem. Ambien online references

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Brain Res. 1988 Jul 19;456(1):173-6.
Clonazepam selectively increases saccharin ingestion in a two-choice test.

Cooper SJ, Yerbury RE.

Department of Psychology, University of Birmingham, U.K.

Twenty-two-hour water-deprived rats were trained with a choice between a sodium saccharin solution (0.01% or 0.05%) and water in a 30-min drinking test. The potent benzodiazepine agonist, clonazepam, produced highly significant dose-related (0.1-1.0 mg/kg, i.p.) increases in total fluid consumption. The most important finding was that clonazepam selectively enhanced ingestion of the preferred 0.05% solution, while producing no change in the consumption of water. It did not selectively affect ingestion of the marginally preferred 0.01% solution. These data can be linked to recent evidence that benzodiazepines facilitate positive ingestive reactions elicited by palatable tastes. Together, the evidence indicates that benzodiazepines can selectively affect consumption of preferred solutions through enhancement of positive reactions to palatable tastes. In contrast to the results with clonazepam, the novel compound zolpidem, which binds preferentially to cerebellar-type benzodiazepine sites, failed to affect fluid intake or sweet taste preference. This suggests that hippocampal-type, as distinct from cerebellar-type receptors, may be necessary in the mediation of effects of benzodiazepines on taste-palatability processing and ingestion.

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Pharmacol Biochem Behav. 1988 Apr;29(4):763-6.
Imidazopyridines as a tool for the characterization of benzodiazepine receptors: a proposal for a pharmacological classification as omega receptor subtypes.

Langer SZ, Arbilla S.

Department of Biology, Laboratoires d'Etudes et de Recherches Synthelabo (L.E.R.S.), Paris, France.

At present, the nomenclature of benzodiazepine (BZ) receptors is based on its historical association with the BZ structure. However, it is mainly through the new compounds chemically unrelated to BZs that the central and peripheral subtypes of BZ receptors have been characterized. We therefore propose the nomenclature of a greek letter omega, as omega 1, omega 2 and omega 3 to designate respectively the central BZ1, BZ2 and the peripheral BZ receptor. Among the several classes of non-BZ drugs with affinity for different receptors, the imidazopyridines provide a valuable tool for the characterization of omega receptor subtypes. Most BZs are non selective ligands for the central omega 1 and omega 2 receptors while the selectivity for omega 1 receptor subtypes is present in several non BZ chemical series: imidazopyridines (zolpidem), triazolopyridazines (CL 218872), betacarbolines (beta-CCE) and pyrazoloquinolines (CGS 8216). Selective ligands for the omega 2 subtype are not available so far. The so called peripheral BZ receptor is also present in the central nervous system, therefore the proposed nomenclature of omega 3 receptors resolves this paradox because it does not designate location and it is defined in terms of pharmacological specificity. Selective ligands for omega 3 receptors include the BZ Ro 5-4864, and the isoquinolinecarboxamide PK 11195, while the imidazopyridine alpidem is the ligand with the highest affinity for this receptor subtype.

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Pharmacol Biochem Behav. 1988 Apr;29(4):781-3.
Specificity within the GABAA receptor supramolecular complex: a consideration of the new omega 1-receptor selective imidazopyridine hypnotic zolpidem.

Lloyd KG, Zivkovic B.

Laboratoires d'Etudes et de Recherche's Synthelabo (L.E.R.S.), Bagneux, France.

The relative contribution of different recognition sites within the GABAA receptor supramolecular complex (GRSC) to the pharmacological effects of anxiolytic and hypnotic drugs is unknown. The development of the omega 1 (ex BZ1) specific hypnotic zolpidem allows a more direct approach to the problem. In contrast to many benzodiazepine hypnotic/anxiolytics (e.g., flunitrazepam, diazepam), zolpidem shows a specificity for GABAergic function, e.g., selectively reversing isoniazide-induced seizures. Furthermore, zolpidem produces a highly specific hypnotic action as compared to myorelaxant or amnesic effects (ratio of ED50's greater than 4.0 for zolpidem; less than 1 for flunitrazepam). Zolpidem exerts its action within the GRSC as it enhances 35S-TBPS binding, as do mixed omega 1/omega 2 compounds or GABA agonists. Both the in vivo and in vitro actions of zolpidem are reversed by flumazenil and the enhanced 35S-TBPS binding is also bicuculline-sensitive. Thus, omega 1 recognition site stimulation (e.g., by zolpidem) is sufficient to produce potent pharmacological effects and modulation of the GABAA receptor-gated chloride ionophore.

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J Pharmacol Exp Ther. 1988 Oct;247(1):309-22.
Distribution of central omega 1 (benzodiazepine1) and omega 2 (benzodiazepine2) receptor subtypes in the monkey and human brain. An autoradiographic study with [3H]flunitrazepam and the omega 1 selective ligand [3H]zolpidem.

Dennis T, Dubois A, Benavides J, Scatton B.

Laboratoires d'Etudes et de Recherches Synthelabo Biology Department, Bagneux, France.

The distribution of the central omega 1 (benzodiazepine1; BZD1) and omega 2 (BZD2) receptor subtypes has been studied autoradiographically in monkey and human brain sections using [3H]flunitrazepam (which binds indiscriminately to omega 1 and omega 2 subtypes) and [3H]zolpidem (which recognizes selectively the omega 1 subtype). Both ligands labeled an homogeneous population of binding sites (Kd values approximately equal to 1.5 nM and approximately equal to 5 nM, respectively) whose pharmacological characteristics were similar to those of central omega (BZD) receptors. Regional displacement studies in monkey brain showed that zolpidem was a more effective displacer of [3H]flunitrazepam from omega 1-than from omega 2-enriched areas. For example, it was 73-fold more potent in the cerebellum (omega 1-enriched) than in the dentate gyrus (omega 2-enriched). Zolpidem thus selectively recognizes omega 1 sites in primate brain. The autoradiographic distribution of [3H]flunitrazepam (omega 1 + omega 2) binding sites in primate brain was highly heterogeneous. Very high densities were observed in lamina IV of the neocortex (with higher densities in the occipital than in the frontal pole), the substantia innominata and molecular layer of the dentate gyrus. Intermediate densities were found in other neocortical laminae, cerebellum (molecular layer), claustrum, globus pallidus, caudate-putamen, nucleus accumbens, dentate gyrus (granular layer) and the majority of thalamic nuclei. Structures displaying low binding densities included the substantia nigra and the subthalamic nucleus. The regional distribution pattern of [3H]zolpidem binding sites was qualitatively similar to that of [3H]flunitrazepam but the relative density of the 3H-ligands differed in several brain regions. The relative density of omega 1 and omega 2 subtypes in each particular primate brain region was evaluated by measuring 1) the ratio of [3H]zolpidem to [3H]flunitrazepam binding; 2) [3H]flunitrazepam binding in the presence and in the absence of 100 nM zolpidem. With both approaches, a preferential enrichment in omega 1 sites was observed in lamina IV of sensorimotor cortical regions and in the extrapyramidal motor system (globus pallidus, ventral thalamic complex, subthalamic nucleus, substantia nigra and cerebellum). In contrast, omega 2 sites predominated in limbic areas (e.g., the dentate gyrus, amygdala, nucleus accumbens, cingulate and parahippocampal gyri) and in the anterior thalamic nucleus and caudate nucleus.(ABSTRACT TRUNCATED AT 400 WORDS)

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Eur J Pharmacol. 1988 Nov 1;156(2):189-96.
The interaction between zolpidem and beta-CMC: a clue to the identification of receptor sites involved in the sedative effect of zolpidem.

Perrault G, Morel E, Sanger DJ, Zivkovic B.

Laboratoires d'Etudes et de Recherches Synthelabo (L.E.R.S.), Bagneux, France.

The interaction of beta-CMC, an amino beta-carboline recently described as a selective antagonist of the sedative effect of diazepam, with zolpidem, an imidazopyridine hypnotic, which like beta-CMC binds preferentially to the omega 1 (BZ-1) site of the GABA benzodiazepine chloride channel receptor complex, was investigated. In mice, beta-CMC antagonized the effect of zolpidem against isoniazid-induced convulsions without affecting its activity against convulsions induced by pentylenetetrazole or electroshock. beta-CMC also antagonized the decrease in locomotor activity and the impairment in muscle strength provoked by zolpidem. In rats trained to discriminate zolpidem, beta-CMC antagonized both the interoceptive stimulus and the decrease in the rate of lever pressing produced by zolpidem. This selective antagonism, inhibition of effects of zolpidem exerted by low doses (locomotor activity and isoniazid-induced convulsions) as well as effects produced by high doses (muscle strength) but not those provoked by intermediate doses (pentylenetetrazole and electroshock-induced convulsions), could not be explained by a receptor occupancy hypothesis. These results suggest that the anticonvulsant and sedative effects of zolpidem do not involve the same receptor subtype and that the hypnoselective properties of zolpidem may be linked to its selectivity for the omega 1 (BZ-1) site of the GABAA receptor.

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