Formulation: A lyophilized powder
Formal Name: L-tyrosyl-L-prolyl-L-tryptophyl-L-phenylalaninamide, trifluoroacetate salt
Purity: ≥95%
Formula Markup: C34H38N6O5 • XCF3COOH
Formula Weight: 610,7
Shelf life (days): 1460
Notes: Endomorphin 1 is an endogenous neuropeptide and μ-opioid receptor agonist (Ki = 0.36 nM) that has analgesic, positive reinforcing, and gastrointestinal properties.{43252,43253} It is found in the brain and, to a lesser extent, in the spinal cord.{43255} It is selective for μ- over δ- and κ-opioid receptors (Ki = 1,506 and 5,428 nM, respectively).{43252} Endomorphin 1 also binds to mouse brain membranes and rat recombinant μ-opioid receptors expressed in CHO cells (Kis = 0.94 and 0.66 nM, respectively).{43253} It inhibits cAMP accumulation induced by forskolin in CHO cells expressing rat recombinant μ-opioid receptors and in SH-SY5Y human neuroblastoma cells (IC50s = 9.33 and 19.1 nM, respectively).{43254} In mice, endomorphin 1 increases analgesia in a radiant heat tail-flick assay following intracerebroventricular or intrathecal administration (ED50s = 4.75 and 0.726 μg, respectively) and induces conditioned place preference when administered intracerebroventricularly at a dose of 10 μg.{43253,43256} Endomorphin 1 (12 μg, i.c.v.) also decreases gastrointestinal transit time in mice.{43253}
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