Converting a peptide into a drug: strategies to improve stability and bioavailability

C Adessi, C Soto - Current medicinal chemistry, 2002 - ingentaconnect.com
The discovery of peptide hormones, growth factors and neuropeptides implicated in vital
biological functions of our organism has increased interest in therapeutic use of short …

Five decades of research on opioid peptides: current knowledge and unanswered questions

LD Fricker, EB Margolis, I Gomes, LA Devi - Molecular pharmacology, 2020 - ASPET
In the mid-1970s, an intense race to identify endogenous substances that activated the
same receptors as opiates resulted in the identification of the first endogenous opioid …

The Concise Guide to PHARMACOLOGY 2013/14: G protein‐coupled receptors

SPH Alexander, HE Benson… - British journal of …, 2013 - Wiley Online Library
Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

Autoradiographic differentiation of mu, delta, and kappa opioid receptors in the rat forebrain and midbrain

A Mansour, H Khachaturian, ME Lewis… - Journal of …, 1987 - Soc Neuroscience
While there is an abundance of pharmacological and biochemical evidence to suggest the
existence of multiple opioid receptors, their precise localization within the brain is unclear …

Molecular insights into the biased signaling mechanism of the μ-opioid receptor

X Cong, D Maurel, H Déméné, I Vasiliauskaité-Brooks… - Molecular Cell, 2021 - cell.com
GPCR functional selectivity opens new opportunities for the design of safer drugs. Ligands
orchestrate GPCR signaling cascades by modulating the receptor conformational …

Pharmacology of nociceptin and its receptor: a novel therapeutic target

G Calo', R Guerrini, A Rizzi… - British journal of …, 2000 - Wiley Online Library
Nociceptin (NC), alias Orphanin FQ, has been recently identified as the endogenous ligand
of the opioid receptor‐like 1 receptor (OP4). This new NC/OP4 receptor system belongs to …

Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.

HI Mosberg, R Hurst, VJ Hruby, K Gee… - Proceedings of the …, 1983 - National Acad Sciences
The conformationally restricted, cyclic, disulfide-containing, enkephalin analogs [2-D-
penicillamine, 5-L-penicillamine] enkephalin [(D-Pen2, L-Pen5] enkephalin) and [2-D …

Neuroanatomical patterns of the mu, delta, and kappa opioid receptors of rat brain as determined by quantitative in vitro autoradiography.

A Tempel, RS Zukin - … of the National Academy of Sciences, 1987 - National Acad Sciences
Highly specific radioligands and quantitative autoradiography reveal strikingly different
neuroanatomical patterns for the mu, delta, and kappa opioid receptors of rat brain. The mu …

Roles of mu, delta and kappa opioid receptors in spinal and supraspinal mediation of gastrointestinal transit effects and hot-plate analgesia in the mouse.

F Porreca, HI Mosberg, R Hurst, VJ Hruby… - Journal of Pharmacology …, 1984 - ASPET
The opioid receptors involved in the mediation of thermal analgesia (55 degrees C hot-
plate) and inhibition of gastrointestinal transit at the spinal and supraspinal levels were …

Insights into opioid action in the intestinal tract

A De Luca, IM Coupar - Pharmacology & therapeutics, 1996 - Elsevier
Opioids have been used for centuries as antidiarrhoeal drugs. In recent years, their
mechanism and sites of action in exerting their antidiarrhoeal effect have been studied …