Lee P H, Nguyen T M, Chung N N, Schiller P W, Chang K J
Division of Cell Biology, Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA.
Eur J Pharmacol. 1995 Jul 4;280(2):211-4. doi: 10.1016/0014-2999(95)00248-j.
The binding properties and pharmacological activities of H-Tyr(3'-I)-Tic-Phe-Phe-OH ([Tyr(3'-I)1]TIPP) were studied. Similar to the delta-opioid receptor antagonist H-Tyr-Tic-Phe-Phe-OH (TIPP), [Tyr(3'-I)1]TIPP is a selective and potent ligand at delta-opioid receptors. The displacement curve of [3H]diprenorphine binding by [Tyr(3'-I)1]TIPP was shifted to the right in the presence of Na+ and 5'-guanylylimidodiphosphate, suggesting that it acted as a delta-opioid receptor agonist. [Tyr(3'-I)1]TIPP also behaved as a full agonist in the mouse vas deferens assay and its effect was both naloxone- and TIPP-reversible. These data show that monoiodination at the 3'-position of the N-terminal tyrosine aromatic ring of TIPP converted it from a potent and selective antagonist to a full agonist at delta-opioid receptors.
研究了H-Tyr(3'-I)-Tic-Phe-Phe-OH（[Tyr(3'-I)1]TIPP）的结合特性和药理活性。与δ-阿片受体拮抗剂H-Tyr-Tic-Phe-Phe-OH（TIPP）相似，[Tyr(3'-I)1]TIPP是δ-阿片受体的选择性强效配体。在存在Na+和5'-鸟苷酰亚胺二磷酸的情况下，[Tyr(3'-I)1]TIPP对[3H]二丙诺啡结合的置换曲线向右移动，表明它作为δ-阿片受体激动剂起作用。[Tyr(3'-I)1]TIPP在小鼠输精管试验中也表现为完全激动剂，其作用可被纳洛酮和TIPP逆转。这些数据表明，TIPP的N端酪氨酸芳香环3'-位的单碘化将其从强效选择性拮抗剂转变为δ-阿片受体的完全激动剂。
