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75 years of opioid research: the exciting but vain quest for the Holy Grail
The historical pathway of opioid research that has led to the current state of knowledge is reviewed and greater understanding of the processes by which opioids produce the euphoria that gives rise to the intense craving for these drugs in opioid addicts is reviewed. Expand
The orphan opioid receptor and its endogenous ligand--nociceptin/orphanin FQ.
The contentious issue of whether activation of this receptor results in hyperalgesia or analgesia is addressed, and a novel endogenous peptide for the orphan opioid receptor has been isolated and sequenced. Expand
Dynorphin1–8 and dynorphin1–9 are ligands for the κ-subtype of opiate    receptor
It is generally accepted that there are three subtypes of opiate receptor: µ, δ and κ. The main endogenous ligands for the µ-and δ-sites are Met5-enkephalin, Leu5-enkephalin and β-endorphin, whereasExpand
Pharmacological studies on the "orphan" opioid receptor in central and peripheral sites.
The response to nociceptin in functional studies and in radioligand binding inhibitory assays was resistant to antagonism/displacement by naloxone and a range of other opioid receptor antagonists, thus displaying a very different pharmacological profile from that of the "classical" opioids. Expand
Radioligands for probing opioid receptors.
The three endogenous opioid precursors of almost 30000 Da are pro-opiocortin, proenkephalin and prodynorphin, which have selective agonist or antagonist action at only one site and the main opioid binding sites are mu, delta and kappa. Expand
Increase in potencies of opioid peptides after peptidase inhibition.
It may now be possible to inhibit enzymatic degradation of opioid peptides sufficiently to measure their release from neurones activated by electrical field stimulation. Expand
Gabapentin inhibits the substance P-facilitated K+-evoked release of [3H]glutamate from rat caudal trigeminal nucleus slices
An effect of gabapentin is found and characterized that is of possible mechanistic relevance to the anti‐hyperalgesic/allodynic actions of this compound. Expand
Nociceptin induced inhibition of K+ evoked glutamate release from rat cerebrocortical slices
Nociception inhibits 46 mM K+‐stimulated glutamate release from rat perfused cerebrocortical slices with an IC50 of 51 nM and implicates a role for nociceptin in glutamatergic neurotransmission. Expand
The interaction of the NK1 receptor antagonist CP‐96,345 with L‐type calcium channels and its functional consequences
The results indicate that in addition to possessing affinity for the NK1 receptor, the non‐peptide antagonist, CP‐96,345, displays high affinity for [3H]‐diltiazem binding sites on L‐type calcium channels in rat cerebral cortex membranes. Expand
Bombesin Receptors as a Novel Anti-Anxiety Therapeutic Target: BB1 Receptor Actions on Anxiety through Alterations of Serotonin Activity
It is suggested that endogenous BB-like peptides at the DRN evoke the release of 5-HT from the limbic nerve terminals originating from the raphé, specifically at the ventral hippocampus, resulting in anxiogenesis. Expand