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2 edition of Structure-activity relationships of opioid ligands found in the catalog.

Structure-activity relationships of opioid ligands

Iain James McFadyen

Structure-activity relationships of opioid ligands

by Iain James McFadyen

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  • 29 Currently reading

Published .
Written in English


Edition Notes

Thesis (Ph.D.) - Loughborough University, 1999.

Statementby Iain James McFadyen.
ID Numbers
Open LibraryOL20925490M

The opioid binding characteristics of the rat (PAG) and the signal transduction mechanisms of the opioid receptors were examined with in vitro radioligand binding, GTPase, adenylyl cyclase, and inositol phosphate assays. The nonselective ligand {sup 3}H-ethylketocyclazocine (EKC), the {mu} and. The discovery and characterization of two classes of kappa opioid receptor agonists that are biased for G protein over βarrestin signaling are described. Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor. Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, Cited by: 8.

Introduction. Frontiers in Medicinal Chemistry is a book series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. Frontiers in Medicinal Chemistry covers all the areas of medicinal chemistry, including developments in rational drug design, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound Cited by: In this section we will describe the process of developing TRK, including the structure–activity relationship (SAR) studies on NTI derivatives and the difficulties encountered in overcoming a defect in the metabolism of a prototype clinical candidate, TRK Antitussive Effects of Opioid Ligands.

• Design and synthesis of bivalent morphinan ligands specific for the opioid receptors. This study was designed to explain some interesting structure-activity relationships discovered while Title: Organic Chemist.   The structure-activity relationships among enkephalin peptides are elaborated in Chapter 8. The last chapter is devoted to the clinical significance of opioid peptides in humans. This publication is a good reference for biologists, specialists, and researchers concerned with peptides and Edition: 1.


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Structure-activity relationships of opioid ligands by Iain James McFadyen Download PDF EPUB FB2

The main focus is on the structure-activity relationship studies of peptide ligands for three main opioid receptor types (μ, δ, κ), their selectivities and pharmacological activities in vitro. Chemical modifications that led to obtaining potent and selective agonists and antagonists for these receptors are discussed.

Opioid Receptor Ligands. This review will discuss the structure–activity relationships, as they are currently understood, with regard to each of the major classes of compounds that interact.

The concept of “ligand bias” at G protein coupled receptors has been introduced to describe ligands which preferentially stimulate one intracellular signaling pathway over another. There is growing interest in developing biased G protein coupled receptor ligands to yield safer, better tolerated, and more efficacious drugs.

The classical μ opioid morphine elicited increased efficacy and Cited by: On the basis of the structure-activity relationships of delta-opioid-selective peptide ligands and on a model of the proposed bioactive conformation for a potent and selective, conformationally. Abstract: Morphiceptin (Tyr-Pro-Phe-Pro-NH2) is one of the most selective agonists for the μ-opioid receptor.

In this review structure-activity relationships of morphiceptin analogues and studies resulting in defining low energy conformations are by: The structure-activity relationships among enkephalin peptides are elaborated in Chapter 8.

The last chapter is devoted to the clinical significance of opioid peptides in humans. This publication is a good reference for biologists, specialists, and researchers concerned with peptides and proteins. The opioid receptors modulate a variety of biological functions, including pain, mood, and reward.

As a result, opioid ligands are being explored as potential therapeutics for a variety of indications. Multifunctional opioid ligands, which act simultaneously at more than one type of opioid receptor, show promise for use in the treatment of addiction, pain, and other : Montgomery D, Anand Jp, Baber Ma, Twarozynski Jj, Hartman Jg, Delong Lj, Traynor, Mosberg Hi.

Structure–Activity Relationships of Morphine Derivatives. Synthetic Analogues of Thebaine Further Define Morphinan SAR. Compounds of the Morphinan Skeleton Produce New Agents. Further Reduction of the Morphinan Skeleton Produced the Benzomorphans.

Another Simplified Version of Morphine Creates a New Class of Opioid LigandCited by: 3. Halfpenny PR, Horwell DC, Hughes J, Hunter JC, Rees DC () Highly selective κ-opioid analgesics. Synthesis and structure-activity relationships of novel N-[2-(pyrrolidinyl) or substituted-cyclohexyl]arylacetamide derivatives.

J Med Chem – PubMed Google ScholarCited by: Extensive research has recently been performed to uncover the structure-activity relationships (SAR) of this class of ligands, thereby providing valuable tools for the pharmacological characterization of.

Research and development of opioid-related ligands. [Mei-Chuan Ko; Stephen M Husbands;] Development of new ligands: Buprenorphine and related orvinols / Stephen M.

Husbands. Structure-activity relationships of nociceptin receptor (NOP) ligands and the design of bifunctional NOP/Mu opioid receptor-targeted ligands / Nurulain T.

Zaveri. Structure-Activity Relationships. Most opioid analgesics are related to morphine (Figure ). Distinctive features of morphine include 5 rings, 3- and 6-hydroxyl groups (phenolic and alcoholic), piperidine ring with an N-methyl group, and a quaternary carbon at position Highly opioid analgesics.

Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivativesCited by:   Chavkin C, Goldstein A () Specific receptor for the opioid peptide dynorphin: structure–activity relationships.

PNAS – CrossRef Google Scholar Connor K, Ramamoorthy K, Moore M, Mustain M, Chen I, Safe S et al () Hydroxylated polychlorinated biphenyls (PCBs) as estrogens and antiestrogens: structure–activity : Mageshwaran Lakshmanan.

Get this from a library. The steric factor in medicinal chemistry: dissymmetric probes of pharmacological receptors. [Alan F Casy; George H Dewar] -- A reference providing source material on stereochemical influences in medicinal chemistry and pharmacology in a coordinated account which presents both the biological data and details (together with.

The rapidly burgeoning research of the past two decades on agonist-antagonist analgesics and opioid receptors makes this exhaustive review of opioid anal gesics particularly relevant and timely. After an introductory chapter the additional 12 chapters begin logically with morphine and congeners (4- epoxymorphinans) and end with opioid s: 1.

Book chapter Full text access Aldose Reductase Inhibitors: Structure–Activity Relationships and Therapeutic Potential. The multiple modality concept based on the structure-activity relationships of opioid ligands led to the proposal of multiple opioid receptors (), which at that time was a departure from the prevailing view of a single receptor type.

The κ-opioid receptor (KOR) is a G protein-coupled receptor that in humans is encoded by the OPRK1 KOR is coupled to the G protein G i /G 0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these effects include altering nociception, consciousness, motor control, and s: OPRK1, K-OR-1, KOR, KOR-1, OPRK, opioid.

NT Zaveri, D Yasuda, VB Journigan, PR Daga, F Jiang, C Olsen, Structure-Activity Relationships of Nociceptin Receptor (NOP) Ligands and the Design of Bifunctional NOP/Mu Opioid Receptor-Targeted Ligands.

In ACS Symposium Series, Research and Development of Opioid-Related Ligands; Ko M, Husbands SM, Eds.Chapter 8,3. Opioid receptors mediate the actions of endogenous and exogenous opioids on many physiological processes, including the regulation of pain, respiratory drive, mood, and - in the case of {kappa}-opioid receptor ({kappa}-OR) - dysphoria and psychotomimesis.

Here we report the crystal structure of the.Structure-activity relationships of nociceptin receptor (NOP) ligands and the design of bifunctional NOP/Mu opioid receptor-targeted ligands / Nurulain T. Zaveri, Dennis Yasuda, Blair V.

Journigan, Pankaj R. Daga, Faming Jiang, and Cris Olsen.Metazocine is an opioid analgesic related to metazocine has significant analgesic effects, mediated through a mixed agonist–antagonist action at the mu opioid receptor, its clinical use is limited by dysphoric and hallucinogenic effects which are most likely caused by activity at kappa opioid receptors (where it is a high-efficacy agonist) and/or sigma status: CA: Schedule I, DE: Anlage I .