High affinity [3H]zolpidem binding in the rat brain: an imidazopyridine with agonist properties at central benzodiazepine receptors. Pharmacological profile of the imidazopyridine zolpidem at benzodiazepine receptors and electrocorticogram in rats. Discriminative stimulus properties of chlordiazepoxide and zolpidem. Agonist and antagonist effects of CGS 9896 and ZK 91296. Autoradiographic localization of [3H]zolpidem binding sites in the rat CNS: comparison with the distribution of [3H]flunitrazepam binding sites. Investigation of the actions of the benzodiazepine antagonists Ro 15-1788 and CGS 8216 using the schedule-controlled behavior of rats. Ambien online references

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Eur J Pharmacol. 1986 Nov 4;130(3):257-63.
High affinity [3H]zolpidem binding in the rat brain: an imidazopyridine with agonist properties at central benzodiazepine receptors.

Arbilla S, Allen J, Wick A, Langer SZ.

[3H]Zolpidem, a novel hypnotic drug possessing a chemical structure unrelated to that of benzodiazepine (BZD) was employed as a new ligand to determine its binding characteristics to membrane preparations of rat cerebral cortex and cerebellum. In both structures, the imidazopyridine [3H]zolpidem bound with high affinity to a single population of recognition sites. The cerebellum possessed a similar number of [3H]zolpidem and [3H]diazepam binding sites, while the cerebral cortex possessed a lower density of [3H]zolpidem than [3H]diazepam binding sites. In contrast to [3H]diazepam binding, [3H]zolpidem binding was not detectable in the spinal cord. In the cortex, BZDs had a similar potency to displace [3H]zolpidem and [3H]diazepam binding while non-BZDs were more potent to inhibit [3H] zolpidem binding than [3H]diazepam binding. The binding of [3H]zolpidem was enhanced by GABA to the same extent as [3H]diazepam binding. The increase in [3H] zolpidem binding caused by chloride ions was less pronounced than that in [3H]diazepam binding. It is concluded that [3H]zolpidem possesses selectivity for BZD receptors with the pharmacological characteristics and regional distribution of the BZD1 receptor subtype. [3H]Zolpidem as a radioligand offers a useful additional tool to study the mechanism of action of hypnotics acting through BZD receptor subtypes.

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Naunyn Schmiedebergs Arch Pharmacol. 1985 Sep;330(3):248-51.
Pharmacological profile of the imidazopyridine zolpidem at benzodiazepine receptors and electrocorticogram in rats.

Arbilla S, Depoortere H, George P, Langer SZ.

Zolpidem is a novel non-benzodiazepine related hypnotic, which possesses an imidazopyridine structure. This drug has preferential affinity for the 3H-diazepam binding site in the rat cerebellum, while it is only weakly active at inhibiting 3H-Ro 5-4864 binding to the rat kidney. The potency of zolpidem at displacing 3H-Ro 15-1788 binding to rat cerebral cortex membranes is enhanced in the presence of GABA. On the sleep pattern of the electrocorticogram in the curarised rat, zolpidem induces a physiological type of slow wave sleep with rapid onset of action. Zolpidem differs from classical benzodiazepine drugs, in possessing an atypical binding profile to 3H-benzodiazepine receptors, and because it does not affect the sleep patterns.

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Neuropharmacology. 1987 May;26(5):499-505.
Discriminative stimulus properties of chlordiazepoxide and zolpidem. Agonist and antagonist effects of CGS 9896 and ZK 91296.

Sanger DJ, Zivkovic B.

In previous studies the effects of CGS 9896, a pyrazoloquinoline ligand at benzodiazepine receptors, in rats trained to discriminate benzodiazepines from vehicle, have been variable. The present experiment confirmed that this compound produced responding on the drug-lever in rats trained to discriminate 5 mg/kg of chlordiazepoxide from saline, and showed that CGS 9896 did not antagonise the effect of chlordiazepoxide in this test. In contrast, CGS 9896 antagonised the stimulus properties of zolpidem (2 mg/kg), a non-benzodiazepine hypnotic, which displaces benzodiazepines from their binding sites. The drug CGS 9896 also antagonised responding on the drug-lever produced by chlordiazepoxide in rats trained with zolpidem. The beta-carboline, ZK 91296, produced effects similar to those of CGS 9896, giving rise to responding on the drug-lever in rats trained with chlordiazepoxide and antagonising the zolpidem cue. These results demonstrate the mixed agonist-antagonist effects of CGS 9896 and ZK 91296 and suggest that the stimulus properties of chlordiazepoxide and zolpidem may be mediated by different sub-types of benzodiazepine receptors.

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J Neurochem. 1987 Sep;49(3):890-9.
Autoradiographic localization of [3H]zolpidem binding sites in the rat CNS: comparison with the distribution of [3H]flunitrazepam binding sites.

Niddam R, Dubois A, Scatton B, Arbilla S, Langer SZ.

The regional distribution of [3H]zolpidem, a novel imidazopyridine hypnotic possessing preferential affinity for the BZD1 (benzodiazepine subtype 1) receptor, has been studied autoradiographically in the rat CNS and compared with that of [3H]flunitrazepam. The binding of [3H]zolpidem to rat brain sections was saturable, specific, reversible, and of high affinity (KD = 6.4 nM). It occurred at a single population of sites whose pharmacological characteristics were similar to those of the benzodiazepine receptors labeled with [3H]flunitrazepam. However, ethyl-beta-carboline-3-carboxylate and CL 218,872 were more potent displacers of [3H]zolpidem than of [3H]flunitrazepam. The autoradiographic brain distribution of [3H]zolpidem binding sites was qualitatively similar to that previously reported for benzodiazepine receptors. The highest levels of [3H]-zolpidem binding sites occurred in the olfactory bulb (glomerular layer), inferior colliculus, ventral pallidum, nucleus of the diagonal band of Broca, cerebral cortex (layer IV), medial septum, islands of Calleja, subthalamic nucleus, and substantia nigra pars reticulata, whereas the lowest densities were found in parts of the thalamus, pons, and medulla. Comparative quantitative autoradiographic analysis of the binding of [3H]zolpidem and [3H]flunitrazepam [a mixed BZD1/BZD2 (benzodiazepine subtype 2) receptor agonist] in the CNS revealed that the relative density of both 3H-labeled ligands differed in several brain areas. Similar levels of binding for both ligands were found in brain regions enriched in BZD1 receptors, e.g., substantia nigra pars reticulata, inferior colliculus, cerebellum, and cerebral cortex lamina IV. The levels of [3H]zolpidem binding were five times lower than those of [3H]flunitrazepam binding in those brain regions enriched in BZD2 receptors, e.g., nucleus accumbens, dentate gyrus, and striatum. Moreover, [3H]zolpidem binding was undetectable in the spinal cord (which contains predominantly BZD2 receptors). Finally, like CL 218,872 and ethyl-beta-carboline-3-carboxylate, zolpidem was a more potent displacer of [3H]flunitrazepam binding in brain regions enriched in BZD1 receptors than in brain areas enriched in BZD2 receptors. The present data add further support to the view that zolpidem, although structurally unrelated to the benzodiazepines, binds to the benzodiazepine receptor and possesses selectivity for the BZD1 receptor subtype.

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Pharmacol Biochem Behav. 1986 Sep;25(3):537-41.
Investigation of the actions of the benzodiazepine antagonists Ro 15-1788 and CGS 8216 using the schedule-controlled behavior of rats.

Sanger DJ.

Ro 15-1788 and CGS 8216 antagonise many of the pharmacological effects of benzodiazepines but both of these compounds have also been shown to exert behavioral effects when administered alone. In the present study the effects of Ro 15-1788 and CGS 8216, alone and in combination with diazepam and with the benzodiazepine receptor ligand zolpidem, were investigated. Diazepam and zolpidem produced dose-related decreases in rates of food-reinforced lever-pressing maintained by a fixed-ratio (FR 10) schedule. CGS 8216 also reduced response rates although Ro 15-1788, at several doses, produced small, but statistically significant, increases in responding. When the diazepam and zolpidem dose-response curves were re-established in the presence of a dose of Ro 15-1788 or CGS 8216 the depressant effects of the higher doses were antagonised. However, neither diazepam nor zolpidem blocked the rate reducing effect of CGS 8216 which may not therefore be due to an action at benzodiazepine receptors.

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