• Publications
  • Influence
Proenkephalin A gene products activate a new family of sensory neuron–specific GPCRs
TLDR
A newly identified family of 'orphan' G protein–coupled receptors (GPCRs) is cloned and it is demonstrated that bovine adrenal medulla peptide 22 and a number of its fragments bind to and activate these receptors with nanomolar affinities. Expand
Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: Selective actions via GalR1 and GalR2 receptors
TLDR
Data indicate that a low dose of galanin has a nociceptive role at the spinal cord level mediated by GalR2 receptors, whereas the antiallodynic effect of high-dose galan in on neuropathic pain is mediated by the GalR1 receptors. Expand
The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor
TLDR
The identification of an MCH receptor could have implications for the development of new anti-obesity therapies and is consistent with the known central effects of MCH. Expand
Cloning and Characterization of a cDNA Encoding a Novel Subtype of Rat Thyrotropin-releasing Hormone Receptor*
TLDR
A novel, pharmacologically distinct receptor for thyrotropin-releasing hormone that appears to be more restricted to the central nervous system particularly to the sensory neurons of spinothalamic tract and spinal cord dorsal horn, which may account for the sensory antinociceptive actions of TRH. Expand
FMRFamide receptors in Helix aspersa
  • K. Payza
  • Medicine, Biology
  • Peptides
  • 1 November 1987
TLDR
The results suggest that the effects of FMRFamide in Helix are receptor-mediated, and that the heptapeptide analogs of FLRFamide were stimulatory on the heart at low doses, but were inhibitory at moderate to high doses. Expand
Preclinical Pharmacology of AZD2327: A Highly Selective Agonist of the δ-Opioid Receptor
TLDR
Data support the role of the δ-opioid receptor in the regulation of mood, and data suggest that AZD2327 may possess unique antidepressant and anxiolytic activities that could make a novel contribution to the pharmacotherapy of psychiatric disorders. Expand
Effects of galanin receptor agonists on locus coeruleus neurons
TLDR
The results suggest that it mainly is the GALR1 receptor that mediates hyperpolarization of LC neurons, and not the selective Gal(2-11)-NH(2) agonist much weaker than AR-M961. Expand
Pharmacologic Profile of Naloxegol, a Peripherally Acting µ-Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation
TLDR
These findings corroborate phase 3 clinical studies demonstrating that naloxegol relieves OIC-associated symptoms in patients with chronic noncancer pain by antagonizing the µ-opioid receptor in the ENS while preserving CNS-mediated analgesia. Expand
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
TLDR
Two general approaches have been established for the synthesis of these compounds, based on dehydration of benzhydryl alcohols and Suzuki coupling reactions of vinyl bromide, and are herewith reported. Expand
Characterization and solubilization of the FMRFamide receptor of squid.
TLDR
It is suggested that F MRFamide is a neurotransmitter in squid optic lobe, and that this tissue is a good source from which to purify FMRFamide receptors. Expand
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