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Benzodiazepine agonist with high selectivity for α1-subunit-containing GABAA receptors (BZ/ω1 site) and very high intrinsic activity. Ki values are 20, 400 and ≥ 5000 nM for α1-, α2-/α3-, and α5-containing GABAA receptors respectively. Hypnotic that does not induce physical dependence.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Arbilla et al (1986) High affinity [3H]zolpidem binding in the rat brain: an imidazopyridine with agonist properties at central benzodiazepine receptors. Eur.J.Pharmacol. 130 257 PMID: 2878820
Crestani et al (2000) Mechanism of action of the hypnotic zol. in vivo. Br.J.Pharmacol. 131 1251 PMID: 11090095
Depoortere et al (1986) Zolpidem, a novel nonbenzodiazepine hypnotic. 1. Neuropharmacological and behavioural effects. J.Pharmacol.Exp.Ther. 237 649 PMID: 2871178
Perrault et al (1992) Lack of tolerance and physical dependence upon repeated treatment with the novel hypnotic zol. J.Pharmacol.Exp.Ther. 263 298 PMID: 1403792
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 158 339 PMID: 30121248
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Keywords: Zolpidem, Zolpidem supplier, Benzodiazepine, agonists, GABAA, Receptors, 0655, Tocris Bioscience
7 Citations for Zolpidem
Citations are publications that use Tocris products. Selected citations for Zolpidem include:
Letra-Vilela et al (2016) Distinct roles of N-acetyl and 5-methoxy groups in the antiproliferative and neuroprotective effects of melatonin Molecular and Cellular Endocrinology 434 238 PMID: 27402603
Geracitano et al (2012) Functional expression of the GABA(A) receptor α2 and α3 subunits at synapses between intercalated medial paracapsular neurons of mouse amygdala. Front Neural Circuits 6 32 PMID: 22666188
Bowser et al (2002) Altered kinetics and benzodiazepine sensitivity of a GABAA receptor subunit mutation [gamma 2(R43Q)] found in human epilepsy. Proc Natl Acad Sci U S A 99 15170 PMID: 12415111
Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. J Neurosci 18 2098 PMID: 18222937
Lazarus and Huang (2011) Distinct maturation profiles of perisomatic and dendritic targeting GABAergic interneurons in the mouse primary visual cortex during the critical period of ocular dominance plasticity. J Neurophysiol 106 775 PMID: 21613595
Wulff et al (2007) From synapse to behavior: rapid modulation of defined neuronal types with engineered GABAA receptors. Nat Neurosci 10 923 PMID: 17572671
Seifi et al (2014) Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon. Br J Cancer 34 10361 PMID: 25080596
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.