Deltorphin II (trifluoroacetate salt) (Synonyms: DADELT II, D-Ala2Deltorphin II, D-Ala2, Glu4Deltorphin II, Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2)

Deltorphin II is a peptide agonist of δ₂-opioid receptors.^1,2 It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (K_is = 0.0033, >1, and >1 µM, respectively) and induces [³⁵S]GTPγS binding in mouse brain membrane preparations (EC₅₀ = 0.034 µM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ₂-opioid receptor antagonist naltriben but not the δ₁-opioid receptor antagonist BNTX.³ Intrathecal administration of deltorphin II (15 µg/animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.⁴

1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)