Literature DB >> 186791

The opiate receptor: a model explaining structure-activity relationships of opiate agonists and antagonists.

A P Feinberg, I Creese, S H Snyder.   

Abstract

A model of the opiate receptor is proposed which explains structure-activity relationships of opiate drugs, including (i) the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine, and oripavines; (ii) the role of N-allyl substituents in conferring antagonist properties; and (iii) chemical features that afford "pure" antagonists. The model indicates mlecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.

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Year:  1976        PMID： 186791      PMCID： PMC431391          DOI： 10.1073/pnas.73.11.4215

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN： 0027-8424            Impact factor:   11.205


  17 in total

1.  Effect of 9-hydroxylation on benzomorphan antagonist activity.

Authors:  N F Albertson
Journal:  J Med Chem       Date:  1975-06       Impact factor: 7.446

2.  Purification and properties of enkephalin - the possible endogenous ligand for the morphine receptor.

Authors:  J Hughes; T Smith; B Morgan; L Fothergill
Journal:  Life Sci       Date:  1975-06-15       Impact factor: 5.037

3.  An endogenous morphine-like factor in mammalian brain.

Authors:  G W Pasternak; R Goodman; S H Snyder
Journal:  Life Sci       Date:  1975-06-15       Impact factor: 5.037

4.  Quantum chemical studies of morphine-like opiate narcotics. Effect of N-substituent variations.

Authors:  G H Loew; D S Berkowitz
Journal:  J Med Chem       Date:  1975-07       Impact factor: 7.446

5.  Morphine-like ligand for opiate receptors in human CSF.

Authors:  L TPERENIUS; A Wahlström
Journal:  Life Sci       Date:  1975-06-15       Impact factor: 5.037

6.  Isolation of an endogenous compound from the brain with pharmacological properties similar to morphine.

Authors:  J Hughes
Journal:  Brain Res       Date:  1975-05-02       Impact factor: 3.252

7.  [On a tetrahydroisoquinoline compound with analgesic action].

Authors:  H BESENDORF; B PELLMONT; H P BACHTOLD; K REBER; A STUDER
Journal:  Experientia       Date:  1962-10-15

8.  Synthetic analgesics: stereochemical considerations.

Authors:  A H BECKETT; A F CASY
Journal:  J Pharm Pharmacol       Date:  1954-12       Impact factor: 3.765

9.  Homologous N-alkylnorketobemidones. Correlation of receptor binding with analgesic potency.

Authors:  R S Wilson; M E Rogers; C B Pert; S H Snyder
Journal:  J Med Chem       Date:  1975-03       Impact factor: 7.446

10.  Identification of two related pentapeptides from the brain with potent opiate agonist activity.

Authors:  J Hughes; T W Smith; H W Kosterlitz; L A Fothergill; B A Morgan; H R Morris
Journal:  Nature       Date:  1975-12-18       Impact factor: 49.962
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  21 in total

1.  Adrenocorticotrophic hormone fragments mimic the effect of morphine in vitro.

Authors:  G J Plomp; J M Van Ree
Journal:  Br J Pharmacol       Date:  1978-10       Impact factor: 8.739

2.  Development of a conformational search strategy for flexible ligands: a study of the potent mu-selective opioid analgesic fentanyl.

Authors:  C Cometta-Morini; G H Loew
Journal:  J Comput Aided Mol Des       Date:  1991-08       Impact factor: 3.686

3.  Influence of intramolecular hydrogen bonding on the electronic structure of oxymorphone.

Authors:  S Scheiner; V M Kolb
Journal:  Proc Natl Acad Sci U S A       Date:  1980-10       Impact factor: 11.205

4.  Consensus 3D model of μ-opioid receptor ligand efficacy based on a quantitative Conformationally Sampled Pharmacophore.

Authors:  Jihyun Shim; Andrew Coop; Alexander D MacKerell
Journal:  J Phys Chem B       Date:  2011-05-12       Impact factor: 2.991

5.  Proposal for the biologically active conformation of opiates and enkephalin.

Authors:  F A Gorin; G R Marshall
Journal:  Proc Natl Acad Sci U S A       Date:  1977-11       Impact factor: 11.205

6.  Conformation-activity relationships of opiate analgesics.

Authors:  J Martin; P Andrews
Journal:  J Comput Aided Mol Des       Date:  1987-04       Impact factor: 3.686

7.  Computer-aided structure-affinity relationships in a set of piperazine and 3,8-diazabicyclo[3.2.1]octane derivatives binding to the mu-opioid receptor.

Authors:  D Barlocco; G Cignarella; G Greco; E Novellino
Journal:  J Comput Aided Mol Des       Date:  1993-10       Impact factor: 3.686

8.  NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.

Authors:  Paul Renton; Brenda Green; Shawn Maddaford; Suman Rakhit; John S Andrews
Journal:  ACS Med Chem Lett       Date:  2012-01-30       Impact factor: 4.345

9.  X-ray diffraction studies of enkephalins. Crystal structure of [(4'-bromo) Phe4,Leu5]enkephalin.

Authors:  T Ishida; M Kenmotsu; Y Mino; M Inoue; T Fujiwara; K Tomita; T Kimura; S Sakakibara
Journal:  Biochem J       Date:  1984-03-15       Impact factor: 3.857

10.  Modeling and simulation of the human delta opioid receptor.

Authors:  Mahalaxmi Aburi; Paul E Smith
Journal:  Protein Sci       Date:  2004-07-06       Impact factor: 6.725
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