Extremely rapid degradation of [3H] methionine-enkephalin by various rat tissues and

Dupont, André; Cusan, Lionel; Garon, Marie; Alvarado-Urbina, Gabriel; Labrie, Fernand

doi:10.1016/0024-3205(77)90254-5

Cited by 111 publications

(21 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The distinct differences in the response to divalent cations and potencies of the various peptides and alkaloid in displacing the 3H-labeled ligands suggests a difference in the binding sites between f3-endorphin and enkephalin. This dissimilarity in the nature of these peptides' binding also suggests that rapid hydrolysis of enkephalin by brain homogenates (25) might not be the sole explanation for the lack of in vivo analgesic effect displayed by the pentapeptide (11,26). Although [D-Ala2 [Metlenkephalin had potent in vivo analgesic effect (27), the alteration in the secondary structure of the peptide (28) by the D amino acid could not be ignored.…”

Section: Methodsmentioning

confidence: 99%

Properties and localization of beta-endorphin receptor in rat brain.

Law¹,

Loh²,

1979

Proc. Natl. Acad. Sci. U.S.A.

View full text Add to dashboard Cite

Thus, by using such a washing procedure with the rapid filtration method, we were able to demonstrate a proteindependent and temperature-dependent high-affinity association of the 13h-[3H]endorphin with the brain membrane (7). Moreover, this high-affinity binding can be demonstrated to be stereospecific (7). The stereoactive isomer levorphanol or (-)naloxone was at least 1000-fold more potent in displacing 3h-[3H]endorphin binding than was the inactive isomer dextrorphan or (+)naloxone, respectively. When the binding of this radioactive ligand was determined at various concentrations and the binding data were analyzed by the method of Scatchard (10), a two-component or single site with negative cooperativity typical of the opiate binding was observed (Fig. 1). The Kd values (with 95% confidence limits) determined from linear regression analysis of the two binding Abbreviation: LPH, lipotropin. 5455The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked "advertisement" in accordance with 18 U. S. C. §1734 solely to indicate this fact.

show abstract

Section: Methodsmentioning

confidence: 99%

Properties and localization of beta-endorphin receptor in rat brain.

Law¹,

Loh²,

1979

Proc. Natl. Acad. Sci. U.S.A.

View full text Add to dashboard Cite

show abstract

“…Replacing Boc-N-methyl-phenylalanine in the preparation of fragment 7b by Boc-p-chloro-Lphenylalanine, Boc-p-nitro-L-phenylalanine or Boc-N-methyl-p-nitro-L-phenylalanine (25b) and coupling the resulting dipeptidyl alcohols with fragment 7f, as in the synthesis of 7, gave analogues 23, 24 and 25 respectively.…”

mentioning

confidence: 99%

Synthesis, Opiate Receptor Binding and Analgesic Activity of Enkephalin Analogues

Pless¹,

Bauer²,

Cardinaux³

et al. 1979

Helvetica Chimica Acta

View full text Add to dashboard Cite

SummaryThe synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants for an opiate receptor site and of analgesic potency in the tail-flick test in mouse. The effects on opioid activity of modifying various parts of the enkephalin molecule are discussed. Tyr-D-Ala-Gly-MePheMet (O)-oll) (FK 33-824), which was highly active in these tests, was subsequently selected for clinical testing.The use of two complementary models -in vitro binding studies and in vivo test for analgesia -for the assessment of biological activity in the evaluation of analogues is explained.

show abstract

“…Perhaps a more significant problem is the lack of robust metabolic stability in blood, tissue, and at the BBB, due to the presence of numerous, soluble and membrane associated, peptidases (Brownson et al, 1994). This is particularly true for the endogenous, opioid peptide Met-enkephalin, which, has a plasma half-life of around five seconds (Dupont et al, 1977). However, this did not stop Abba and his team who carried out several studies on Met-enkephalin analogs showing brain entry via what was termed a Brain Uptake Index (BUI) (Kastin et al, 1976).…”

Section: “Ouch There Goes My Blood Brain Barrier”mentioning

confidence: 99%

Peptides at the blood brain barrier: Knowing me knowing you

2015

View full text Add to dashboard Cite

When the Davis Lab was first asked to contribute to this special edition of Peptides to celebrate the career and influence of Abba Kastin on peptide research, it felt like a daunting task. It is difficult to really understand and appreciate the influence that Abba has had, not only on a generation of peptide researchers, but also on the field of blood brain barrier (BBB) research, unless you lived it as we did. When we look back at our careers and those of our former students, one can truly see that several of Abba’s papers played an influential role in the development of our personal research programs.

show abstract

Extremely rapid degradation of [3H] methionine-enkephalin by various rat tissues and

Cited by 111 publications

References 14 publications

Properties and localization of beta-endorphin receptor in rat brain.

Properties and localization of beta-endorphin receptor in rat brain.

Synthesis, Opiate Receptor Binding and Analgesic Activity of Enkephalin Analogues

Peptides at the blood brain barrier: Knowing me knowing you

Contact Info

Product

Resources

About