Opioids and Their Receptors : Present and Emerging Concepts in Opioid Drug Discovery

The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors repre...

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Year of Publication:2020
Language:English
Physical Description:1 electronic resource (358 p.)
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spelling Spetea, Mariana edt
Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
Opioids and Their Receptors
Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute 2020
1 electronic resource (358 p.)
text txt rdacontent
computer c rdamedia
online resource cr rdacarrier
The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.
English
Medicine bicssc
opioid receptors
neurokinin-1 receptor
peptide synthesis
receptor binding studies
functional assay
writhing test
tolerance
Leu-enkephalin
beta-arrestin
mu opioid receptor
delta opioid receptor
biased signaling
DADLE
ischemia
plasma stability
morphinan
BNTX
δ opioid receptor antagonist
1H-NMR experiments
mechanism elucidation
peripheral antinociception
14-methoxycodeine-6-O-sulfate
codeine-6-O-sulfate
opioid peptides and peptidomimetics
DAMGO
DALDA
[Dmt1]DALDA
KGOP01
binding
molecular docking
structure-activity relationships
β2-amino acids
β2-Homo-amino acids
µ-opioid receptor
opioid peptides
TAPP
racemic synthesis of β2-amino acids
peripheral µ-opioid receptors
analgesia
peripheral analgesic tolerance
dysbiosis
opioid
bifunctional ligands
(−)-N-phenethylnorhydromorphone analogs
[35S]GTPgammaS assay
forskolin-induced cAMP accumulation assays
β-arrestin recruitment assays
MOR and DOR agonists
respiratory depression
bias factor
molecular modeling &amp
simulation
δ opioid receptor
NTI derivative
sulfonamide
inverse agonist
neutral antagonist
agonist
opioids
mu receptor
opioid side effects
biased agonism
partial agonism
zerumbone
chronic constriction injury (CCI)
allodynia
hyperalgesia
potassium channels
over-the-counter drugs
misuse
abuse
opioid drugs
pharmacology
codeine
dihydrocodeine
loperamide
opioid peptide
macrocyclic tetrapeptide
multifunctional ligands
kappa opioid receptor
analgesics
opioid liabilities
μ opioid receptor
receptor model
biased ligands
dependence
pain therapy
neonatal opioid withdrawal syndrome
naltrexone
6β-naltrexol
buprenorphine
G-protein bias
arrestin recruitment
respiration
mitragynine
heteromer
internalization
primary hippocampal culture
lysosomes
µ opioid receptor
molecular dynamics
docking
interaction fingerprints
biased agonists
SR-17018
PZM21
morphine
fentanyl
diphenethylamines
design and synthesis
partial agonist
biased agonist
antagonist
binding affinity
selectivity
3-0365-0046-4
3-0365-0047-2
Schmidhammer, Helmut edt
Spetea, Mariana oth
Schmidhammer, Helmut oth
language English
format eBook
author2 Schmidhammer, Helmut
Spetea, Mariana
Schmidhammer, Helmut
author_facet Schmidhammer, Helmut
Spetea, Mariana
Schmidhammer, Helmut
author2_variant m s ms
h s hs
author2_role HerausgeberIn
Sonstige
Sonstige
title Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
spellingShingle Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
title_sub Present and Emerging Concepts in Opioid Drug Discovery
title_full Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
title_fullStr Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
title_full_unstemmed Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
title_auth Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery
title_alt Opioids and Their Receptors
title_new Opioids and Their Receptors
title_sort opioids and their receptors present and emerging concepts in opioid drug discovery
publisher MDPI - Multidisciplinary Digital Publishing Institute
publishDate 2020
physical 1 electronic resource (358 p.)
isbn 3-0365-0046-4
3-0365-0047-2
illustrated Not Illustrated
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