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  • selective
  • 11 C]carfentanil, a selective μ-opioid receptor (MOR) radiotracer, was used to assess baseline receptor availability in vivo [binding potential (BP)] in patients and pain-free control participants. (jneurosci.org)
  • In addition to its reversibility, BU09059 is much more selective for the KOR than JDTic, showing 15-fold and 616-fold preference for the KOR over the μ- and δ-opioid receptors (Ki = 1.72 nM, 26.5 nM, and 1060 nM, respectively). (wikipedia.org)
  • variants
  • You can calculate the theoretical MW of the receptor proteins from their amino acid sequences, but then the party is spoilt by post-traslational modifications, not to mention the many isoforms/splice variants of opioid receptors that exist, all of which have different MW's. (histosearch.com)
  • Based on receptor binding studies, three variants of the KOR designated κ1, κ2, and κ3 have been characterized. (wikipedia.org)
  • Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. (wikipedia.org)
  • effects of opioids
  • It is thought that the hallucinogenic and dysphoric effects of opioids such as butorphanol, nalbuphine, and pentazocine serve to limit their abuse potential. (wikipedia.org)
  • Inhibition
  • It could be demonstrated that inhibition of excitatory amino acid (EA) receptors [ 6 , 7 ] and stimulation of GABA-A and GABA-B receptor [ 5 , 8 ] resulted in pain suppression. (hindawi.com)
  • NOP activation also causes indirect inhibition of opioid receptors MOP and KOP, resulting in anti-opioid activity in certain tissues. (wikipedia.org)
  • The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. (wikipedia.org)
  • Stimulation of these receptors on central nervous system neurons causes an intracellular inhibition of adenylate cyclase, closing of influx membrane calcium channels, and opening of membrane potassium channels. (wikipedia.org)
  • exogenous opioids
  • Although no trials of exogenous opioids in FM have been performed, opioids are not anecdotally found to be useful in treating this and related conditions ( Rao and Clauw, 2004 ). (jneurosci.org)
  • The G allele, even when present heterozygously, has been linked to increased alcohol cravings and influences the response to exogenous opioids, likely by affecting receptor expression and signaling efficiency (3,4,5). (salimetrics.com)
  • pathways in the brain
  • Another long-term adaptation to opioid use can be upregulation of glutamate and other pathways in the brain which can exert an opioid-opposing effect, so reduce the effects of opioid drugs by altering downstream pathways, regardless of MOR activation. (wikipedia.org)
  • humans
  • In humans, this paralogon resulting from a double tetraploidization event resulted in the receptor genes being located on chromosomes 1, 6, 8, and 20. (wikipedia.org)
  • In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain. (wikipedia.org)
  • respiratory depression
  • It lacks most of the side effects of other opioids such as adverse effects on the cardiovascular system and respiratory depression, but it can cause sedation (although to a lesser degree of typical opioids), and in some patients it may induce hallucinations (probably via binding to and activating the κ-opioid receptor). (wikipedia.org)
  • drugs
  • By the mid-1960s, it had become apparent from pharmacologic studies that opiate drugs were likely to exert their actions at specific receptor sites, and that there were likely to be multiple such sites. (wikipedia.org)
  • The addiction liability of these drugs has led to the current epidemic of opioid abuse in the US. (jci.org)
  • The receptors can be activated by drugs, which can cause addictions. (wikipedia.org)
  • this gives butorphanol a lower potential for abuse than other opioid drugs. (wikipedia.org)
  • fentanyl
  • It means that butyrfentantyl is a less potent opioid-agonist than fentanyl. (wikipedia.org)
  • Binding studies have helped to explain the increased potency of N-phenethylnormorphine, showing that the phenethyl group extends out to reach an additional binding point deeper inside the μ-opioid receptor cleft, analogous to the binding of the phenethyl group on fentanyl. (wikipedia.org)