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Chemical Compound Review

Delt-II     (4S)-4-[[1-[[(1S)-1- (aminocarbonylmethylca...

Synonyms: Deltorphin-II, Deltorphin II, Delt II, LS-72217, AC1L3XB1, ...
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Disease relevance of Deltorphin II

  • In the present study, we show that deltorphin-II is a fully functional agonist of the mu-delta heteromer, which induced desensitization and inhibited adenylyl cyclase through a pertussis toxin-insensitive G protein [1].
  • However, deltorphin II and SNC80 were less potent, and in the case of SNC80 less efficacious, in modulating the response to acute thermal nociception in comparison to hyperalgesia associated with persistent inflammation [2].
  • A similar pattern was found for the selective mu-opioid receptor antagonist, beta-funaltrexamine (5.0 microg, i.c.v.), which potentiated and blocked deltorphin II-induced hypo- and hyperthermia, respectively [3].
  • Also, naloxone potentiated hypothermia produced by a lower dose of deltorphin II (25.0 microg), which did not produce hyperthermia [3].
  • Deltorphin II given by minipump resulted in a moderate level of Salmonella in the spleen [4].

Psychiatry related information on Deltorphin II

  • Chronic administration of DPDPE (25 microg i.t.) and deltorphin II (15 microg i.t.) resulted in significant prolongation of the reaction time determined on days 2, 4 and 6 post-injury [5].
  • The substantial potency difference between deltorphin II and SNC80 in stimulating locomotor activity in habituated rats suggests pharmacological heterogeneity for these delta opioid receptor agonists [6].

High impact information on Deltorphin II

  • Deltorphin II strongly reduced the respiratory frequency in wild-type mice but not in MOR -/- mice [7].
  • The mutation also decreased alpha2-agonist-mediated spinal analgesia and blocked the synergy seen in wild-type mice with both the delta-opioid agonist deltorphin II and the micro-opioid agonist [D-ALA2,N-Me-Phe4, Gly-ol5]-Enkephalin (DAMGO) in the substance P behavioral test [8].
  • Mutation of Ser(363) in the carboxyl tail of the delta-opioid receptor to Ala completely abolished the deltorphin II-induced receptor phosphorylation but not the desensitization response [9].
  • In these mice, morphine is ineffective and the potency of spinally administered DOR agonists, deltorphin II (DELT II) and DPDPE decreased 16- and 250-fold, respectively [10].
  • The CNS distribution was also sensitive to p-aminohippurate and deltorphin II, but not digoxin, suggesting the involvement of organic anion transporters (OAT1/OAT3-like) and organic anion transporting polypeptides (OATP1/OATPA-like) [11].

Chemical compound and disease context of Deltorphin II


Biological context of Deltorphin II


Anatomical context of Deltorphin II


Associations of Deltorphin II with other chemical compounds

  • The present experiments tested moxonidine for ability to synergize with morphine, deltorphin II, and DAMGO (Tyr-D-Ala-NMe-Phe-Gly(ol)) to inhibit substance P-elicited nociceptive behavior in Institute of Cancer Research mice [20].
  • DPDPE and deltorphin II are considered prototypes, but their delta-selectivity in vivo and the true ability of delta receptors to produce analgesia remain to be demonstrated [21].
  • A functional assay, based on aequorin-derived luminescence triggered by receptor-mediated changes in intracellular calcium levels, was used to examine relative potency and efficacy of the mu-opioid agonists endomorphin-1, endomorphin-2, morphiceptin, and their position 3-substituted analogs, as well as the delta-agonist deltorphin-II [22].
  • We now report that the dextro-morphine and levo-morphine attenuated antinociception produced by delta-opioid receptor agonist deltorphin II and kappa-opioid receptor agonist U50,488H given spinally in the male mu-opioid receptor knockout mice [23].
  • Moreover, under the condition that the sodium channel blocker, tetrodotoxin (0.1 nmol), was perfused continuously into the nucleus accumbens, the deltorphin II-induced increase in extracellular levels of dopamine was reduced by 72% [24].

Gene context of Deltorphin II

  • DPDPE also was transported by rat Oatp1 (K(m) approximately 48 microM) and Oatp2 (K(m) approximately 19 microM), whereas deltorphin II was only transported by Oatp1 (K(m) approximately 137 microM) [19].
  • The delta2 receptor agonist deltorphin II (0.1-1.0 microM) decreased respiratory frequency in both groups whereas doses of the delta1 receptor agonist enkephalin[D-Pen2,5] (0.1-1.0 microM) which were ineffective in wild-type mice significantly decreased respiratory frequency in MOR-/- mice [25].
  • However, [L-Ala3]DPDPE has been found to antagonize DPDPE, but not Deltorphin II, in a moderately potent (pA2 = 5.7) and selective fashion in vivo [26].
  • The purpose of this study was therefore to determine the distribution of functional DORs, as assessed by [35S]GTPgammaS autoradiographic labeling in response to the DOR agonist deltorphin II [17].
  • The putative delta 1 receptor agonist [D-Pen2,D-Pen5]-enkephalin (DPDPE) elevated [Ca2+]i with an EC50 of 11 nM and the putative delta 2 agonist deltorphin II elevated [Ca2+]i, with an EC50 of 14 nM [27].

Analytical, diagnostic and therapeutic context of Deltorphin II

  • In addition, systemic administration of the delta-opioid receptor agonist BW373U86 (1 mg/kg, s.c.) and spinal administration of the delta(2)-opioid receptor agonist, Tyr-D-Ala-Phe-Glu-Val-Val-Gly amide ([D-Ala(2)] deltorphin II) (1 microM in the perfusion fluid) induced a significant increase of the CCK-LI level [28].
  • The delta(2)-agonist deltorphin II was introduced in the SA node by microdialysis to evaluate delta(2) responses before and after infusion of the delta(1)-agonist TAN-67 [29].
  • Dexamethasone pre-treatment prevented DAMGO-, deltorphin II- and beta-endorphin-induced seizures as well as changes in background EEG, physical parameters and overt behaviour induced by mu-opioid agonists [30].
  • The effects of the delta agonists SNC80 and deltorphin II on ambulation and rearing activity were measured in habituated and non-habituated rats [6].
  • Agonist (e.g. deltorphin II) binding causes an increase in membrane thickness because of receptor elongation, a mass density increase due to an influx of lipid molecules into the bilayer, and an increase in refractive index anisotropy due to transmembrane helix and fatty acyl chain ordering [31].


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  13. Intrahypothalamic injection of deltorphin-II alters body temperature in rats. Benamar, K., Rawls, S.M., Geller, E.B., Adler, M.W. Brain Res. (2004) [Pubmed]
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  20. Moxonidine, a selective imidazoline/alpha(2) adrenergic receptor agonist, synergizes with morphine and deltorphin II to inhibit substance P-induced behavior in mice. Fairbanks, C.A., Posthumus, I.J., Kitto, K.F., Stone, L.S., Wilcox, G.L. Pain (2000) [Pubmed]
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