Endomorphin 2 (trifluoro<wbr/>acetate salt)

Endomorphin 2 (trifluoroacetate salt)

CAT N°: 23281
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Endomorphin 2 is an endogenous neuropeptide and ?-opioid receptor agonist (Ki = 0.69 nM) that has analgesic, negative reinforcing, and gastrointestinal properties.{43252,43253} It is found in the spinal cord and, to a lesser extent, in the brain.{43255} It is selective for ?- over ?- and ?-opioid receptors (Kis = 9,233 and 5,240 nM, respectively).{43252} Endomorphin 2 also binds to mouse brain membranes and rat recombinant ?-opioid receptors expressed in CHO cells (Kis = 1.37 and 0.58 nM, respectively).{43253} It inhibits cAMP accumulation induced by forskolin in CHO cells expressing rat recombinant ?-opioid receptors and in SH-SY5Y human neuroblastoma cells (IC50s = 7.08 and 7.76 nM, respectively).{43254} In mice, endomorphin 2 increases analgesia in a radiant heat tail-flick assay in mice following intracerebroventricular (i.c.v.) or intrathecal administration (ED50s = 1.99 and 3.81 ?g, respectively) and induces conditioned place aversion when administered intracerebroventricularly at a dose of 10 ?g.{43253} It also decreases gastrointestinal transit time in mice when administered intracerebroventricularly at a dose of 3 ?g.{43253}

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