Cayman Methyl- Betacyclodextrin; Size- 5 G

Endomorphin 2 is an endogenous neuropeptide and μ-opioid receptor agonist (K_i = 0.69 nM) that has analgesic, negative reinforcing, and gastrointestinal properties.^, It is found in the spinal cord and, to a lesser extent, in the brain. It is selective for μ- over δ- and κ-opioid receptors (K_is = 9,233 and 5,240 nM, respectively). Endomorphin 2 also binds to mouse brain membranes and rat recombinant μ-opioid receptors expressed in CHO cells (K_is = 1.37 and 0.58 nM, respectively). It inhibits cAMP accumulation induced by forskolin in CHO cells expressing rat recombinant μ-opioid receptors and in SH-SY5Y human neuroblastoma cells (IC₅₀s = 7.08 and 7.76 nM, respectively). 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 μg, respectively) and induces conditioned place aversion when administered intracerebroventricularly at a dose of 10 μg. It also decreases gastrointestinal transit time in mice when administered intracerebroventricularly at a dose of 3 μg.

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