Add time:08/17/2019         Source:sciencedirect.com

Deltorphins show a high affinity and selectivity for δ opioid receptors. Analogs of deltorphins with substitution of Val5,6 residues with more hydrophobic lle5,6 appear to have a higher in vitro activity and selectivity than parent deltorphins. In our study, changes in the nociceptive threshold after intrathecally injected deltorphin I (DELT I), deltorphin II (DELT II) and their lle5,6-derivatives (ILE-DELT I and ILE-DELT II, respectively) were investigated in a tail-flick (TF) and a paw pressure (PP) tests. Male Wistars rats (260–350 g) with a chronically implanted catheter in the lumbar enlargement of the spinal cord were used. DELT I and DELT II, injected i.th. in doses of 0.15, 1.5 and 15 μg, increased the TF latency in a dose-dependent manner. The effect of their derivatives was similar, but the action of ILEDELT II was shorter than that of the parent peptide. In the PP test, the antinociceptive effects of DELT I and their derivative ILE-DELT I were similar, but the effect of a higher dose of ILE-DELT I lasted longer in comparison with the parent peptide. Both DELT II and ILE-DELT II exhibited a low and short-lasting antinociceptive potency in the PP test. The effect of DELT 1 (1.5 μg) was antagonized by pretreatment with NTI (30 μg), a non-selective δ opioid receptor antagonist, as well as by the δ2 receptor antagonist NTB (3 μg) and the δ1 antagonist BNTX (1 μg) in both those tests used. The antinociceptive effect of DELT II(1.5 μg) was antagonized by pretreatment with NTI (30 μg) and NTB (3 μg) in the TF test, but not in the PP test. In the latter test, the antinociceptive effect of DELT II was potentiated by pretreatment with BNTX (1 μg). The effects of both the derivatives ILE-DELT I and ILE-DELT II were antagonized by NTl (30 μg) in the TF test, and by NTI (30 μg) and NTB (3 μg) in the PP test. Like in the case of the parent peptide, the effect of ILE-DELT II was potentiated by pretreatment with the δ1 antagonist BNTX (1 μg). Summing up, modification of the DELT I and II by substituting lle5,6 for Val5,6 residues appears to influence the δ1 selectivity rather then the potency of the peptides at spinal δ receptors.

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