[6-O-methyl-11C]Diprenorphine
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Leung K
[6-O-methyl-11C]Diprenorphine
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- PubMed ID
- 20641600 [ View in PubMed]
- Abstract
Opioids such as morphine are commonly used analgesics in clinical practice. Three opioid receptors (mu, micro; delta, delta; and kappa, kappa) that mediate opioid effects have been identified by molecular cloning: delta (enkephalin-preferring), kappa (dynorphin-preferring), and micro (morphine and ss-endorphin-preferring) (1). Each type of opioid receptors consists of subtypes of receptors as suggested by pharmacological studies (2, 3). Their specificity and ubiquitous location are present in both the central and peripheral nervous system. The opioid receptors (G-protein coupled, resulting in decrease in adenylyl cyclase activity) play an important role in the regulation of analgesia, shock, appetite, thermoregulation, cardiovascular, mental and endocrine function (2-5). Although micro opioid receptors are the major receptor to mediate the analgesic effects of opioids, delta and kappa receptors are also important in antinociception. Opioids have been found to protect cells from ischemia injury in the heart and brain via the delta receptors. On the other hand, kappa antagonist prevents neurodegeneration. The micro opioid receptors are localized predominately in the hypothalamus and thalamus, and the delta opioid receptors are localized predominately in the striatum, limbic system, and cerebral cortex (6, 7). The kappa opioid receptors (kappa1 and kappa2 ) are the most abundant brain opioid receptors and are widely distributed in deeper layers of the neocortex (particularly temporal, parietal, and frontal cortices), striatum, amygdala, and thalamus, with lower levels in the hippocampus, occipital cortex, and cerebellum (8-10). The kappa opioid receptors have been implicated in several clinical brain disorders, including drug abuse (11), epilepsy (12), Tourette's syndrome (13), and Alzheimer's disease (14). Diprenorphine is a highly potent and nonselective opioid receptors antagonist with subnanomolar affinity (7). Diprenorphine has been labeled as [6-O-methyl-11C]diprenorphine ([11C]DPN) (15, 16). [11C]DPN is being developed as a PET agent for the non-invasive study of opioid receptors in the brain.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Diprenorphine Delta-type opioid receptor Protein Humans YesAntagonistDetails Diprenorphine Kappa-type opioid receptor Protein Humans UnknownAntagonistDetails Diprenorphine Mu-type opioid receptor Protein Humans YesAntagonistDetails