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Biological Activity for L-838,417
L-838,417 is a subtype-selective GABAA receptor partial agonist. Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Compound Libraries for L-838,417
Technical Data for L-838,417
|Storage||Store at +4°C|
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.
Solubility Data for L-838,417
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for L-838,417
The following data is based on the product molecular weight 399.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.01 mL||25.04 mL||50.08 mL|
|2.5 mM||1 mL||5.01 mL||10.02 mL|
|5 mM||0.5 mL||2.5 mL||5.01 mL|
|25 mM||0.1 mL||0.5 mL||1 mL|
References for L-838,417
References are publications that support the biological activity of the product.
McCabe et al (2004) Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 46 171 PMID: 14680756
McMahon and France (2006) Differential behavioural effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. Br.J.Pharmacol. 147 260 PMID: 16331290
Knabl et al (2008) Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature 451 330 PMID: 18202657
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
If you know of a relevant reference for L-838,417, please let us know.
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Keywords: L-838,417, L-838,417 supplier, Subtype-selective, GABAA, partial, agonists, Receptors, L838417, merck, 3250, Tocris Bioscience
3 Citations for L-838,417
Citations are publications that use Tocris products. Selected citations for L-838,417 include:
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
De la Luz-Cuellar et al (2019) Blockade of spinal α5-GABAA receptors differentially reduces reserpine-induced fibromyalgia-type pain in female rats. Eur J Pharmacol 858 172443 PMID: 31181208
Gee et al (2010) Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther 332 1040 PMID: 19940102
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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* 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.