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Potent δ-opioid receptor positive allosteric modulator (EC50 = 30 nM). Exhibits 100-fold selectivity for δ over μ-opioid receptor. Enhances affinity of [Leu5]-Enkephalin (Cat.No. 1889), SNC 80 (Cat.No. 0764) and TAN 67 (Cat.No. 0921) for the δ-opioid receptor.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 470.61. 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|
|0.2 mM||10.62 mL||53.12 mL||106.25 mL|
|1 mM||2.12 mL||10.62 mL||21.25 mL|
|2 mM||1.06 mL||5.31 mL||10.62 mL|
|10 mM||0.21 mL||1.06 mL||2.12 mL|
References are publications that support the biological activity of the product.
Burford et al (2015) Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. J.Med.Chem. 58 4220 PMID: 25901762
Shang et al (2016) Proposed mode of binding and action of positive allosteric modulators at opioid receptors. ACS Chem.Biol. 11 1220 PMID: 26841170
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and 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.
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.