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Potent and selective peripherally acting δ opioid antagonist; Ki values are 0.47, 5.31 and 36.56 nM at hDOR, hKOR, and hMOR, respectively. Kb values are 0.21, 7.18 and 9.43 nM, respectively. Attenuates morphine-induced side effects in vivo. Antianalgesic.
|Storage||Store at -20°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 486.56. 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|
|1 mM||2.06 mL||10.28 mL||20.55 mL|
|5 mM||0.41 mL||2.06 mL||4.11 mL|
|10 mM||0.21 mL||1.03 mL||2.06 mL|
|50 mM||0.04 mL||0.21 mL||0.41 mL|
References are publications that support the biological activity of the product.
Lattanzi et al (2018) In vitro and in vivo pharmacological activities of 14-O-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice. Front.Pharmacol. 9 10.3389/fphar.2018.0 PMID: 30233377
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Keywords: TAN 452, TAN 452 supplier, TAN452, Potent, selective, peripherally, acting, delta, opioid, antagonists, antagonism, antianalgesic, Delta, Opioid, Receptors, 6729, Tocris Bioscience
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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!
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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.