Cat. No. 0495
Chemical Name: trans-(±)-3,4-Dichloro-N-methyl-N-[2
Biological ActivitySelective κ-opioid agonist. At higher concentrations blocks Na+ channels. Separate isomers (+)-U-50488 and (-)-U-50488 also available (Cat. Nos. 0471 and 0496 respectively).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Su et al (1998) Blockade of the development of morphine tolerance by U-50,488, an AVP antagonist or MK 801 in the rat hippocampal slice. Br.J.Pharmacol. 123 625. PMID: 9517380.
Pao-Luh Tao et al (1994) U-50,488 blocks the development of morphine tolerance and dependence at a very low dose in guinea pigs. Eur.J.Pharmacol. 256 281. PMID: 8045272.
Suarez-Roca and Maixner (1993) Activation of kappa opioid receptors by U-50488H and morphine enhances the release of substance P from rat trigeminal nucleus slices. J.Pharmacol.Exp.Ther. 264 648. PMID: 7679733.
Pugsley et al (1992) Cardiovascular actions of the κ-agonist, U-50-488H, in the absence and presence of opioid receptor blockade. Br.J.Pharmacol. 105 521. PMID: 1320979.
If you know of a relevant reference for (±)-U-50488 hydrochloride please let us know.
Citations are publications that use Tocris products. Selected citations for (±)-U-50488 hydrochloride include:
Polter (2017) Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapsesfollowing acute stress Elife 6 e23785. PMID: 28402252.
Kharmate et al (2013) Inhibition of tumor promoting signals by activation of SSTR2 and opioid receptors in human breast cancer cells. Cancer Cell Int 13 93. PMID: 24059654.
Zhou et al (2013) Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem 288 36703. PMID: 24187130.
Grachev et al (2012) GPR54-dependent stimulation of luteinizing hormone secretion by neurokinin B in prepubertal rats. Pain 7 e44344. PMID: 23028524.
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Keywords: (±)-U-50488 hydrochloride, supplier, selective, agonists, κ-opioid, kappa-opioid, KOP, Receptors, OP2, Tocris Bioscience, κ Opioid Receptor Agonist products