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[3H]DSTBULET, a new linear hexapeptide with both an improved selectivity and a high affinity for delta-opioid receptors. 1986

P Delay-Goyet, and C Seguin, and V Daugé, and G Calenco, and J L Morgat, and G Gacel, and B P Roques
Département de Chimie Organique, U 266 INSERM, UA 498 CNRS, Faculté de Pharmacie, Paris.

The binding properties of the new agonist Tyr-D-Ser(OtBu)-Gly-Phe-Leu-Thr, DSTBULET, in rat brain tissue shows that insertion of a bulky t.butyl group into the sequence of DSLET leads to a conformationally-induced large increase in selectivity for delta opioid receptors (KI(delta)/KI(mu) = 0.012). In addition to its similar selectivity to that of the cyclic enkephalins DPDPE and DPLPE, the affinity of [3H]DSTBULET for delta sites (KD = 2.9 nM) is significantly better than that of [3H]DPDPE (KD approximately 10.5 nM) or DPLPE (KI (delta) approximately 19 nM). DSTBULET is therefore the most appropriate probe for both binding studies and pharmacological investigations of delta-receptors as illustrated by a comparison of the analgesic properties of DAGO, DSTBULET and DPLPE.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D011957 Receptors, Opioid Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known. Endorphin Receptors,Enkephalin Receptors,Narcotic Receptors,Opioid Receptors,Receptors, Endorphin,Receptors, Enkephalin,Receptors, Narcotic,Receptors, Opiate,Endorphin Receptor,Enkephalin Receptor,Normorphine Receptors,Opiate Receptor,Opiate Receptors,Opioid Receptor,Receptors, Normorphine,Receptors, beta-Endorphin,beta-Endorphin Receptor,Receptor, Endorphin,Receptor, Enkephalin,Receptor, Opiate,Receptor, Opioid,Receptor, beta-Endorphin,Receptors, beta Endorphin,beta Endorphin Receptor,beta-Endorphin Receptors
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D002462 Cell Membrane The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells. Plasma Membrane,Cytoplasmic Membrane,Cell Membranes,Cytoplasmic Membranes,Membrane, Cell,Membrane, Cytoplasmic,Membrane, Plasma,Membranes, Cell,Membranes, Cytoplasmic,Membranes, Plasma,Plasma Membranes
D004745 Enkephalins One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla. Enkephalin
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D017465 Receptors, Opioid, delta A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins. Opioid Receptors, delta,Receptors, delta,Receptors, delta Opioid,delta Receptors,delta Opioid Receptor,delta Receptor,Opioid Receptor, delta,Receptor, delta,Receptor, delta Opioid,delta Opioid Receptors
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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