Imaging Opiate Receptors in the Human Brain by Positron Tomography

  title={Imaging Opiate Receptors in the Human Brain by Positron Tomography},
  author={J. James Frost and Henry N. Jr. Wagner and Robert F. Dannals and Hayden T. Ravert and Jonathan M. Links and Alan A. Wilson and H. Donald Burns and Dean F. Wong and R. W. Mcpherson and Arthur E. Rosenbaum and Michael J. Kuhar and Solomon H. Snyder},
  journal={Journal of Computer Assisted Tomography},
Carfentanil is a potent, synthetic opiate that binds to mu opiate receptors with very high affinity (K1 = 0.051 n M, 37°). In rat brain, carfentanil is 90 and 250 times more selective for mu opiate receptors compared with delta and kappa opiate receptors, respectively. Carbon-11-carfentanil was synthesized by reacting [11C]methyliodide with the carboxylic acid precursor of carfentanil. Carbon-11-carfentanil was injected intravenously in man and a baboon and the distribution of the radioactivity… 
Detection and quantification of opiate receptors in Man by positron emission tomography. Potential applications to the study of pain
Several important methodological aspects of the in vivo opiate receptor labeling with PET in relation to the study of pain are considered and have the potential to reveal better ways to treat pain.
Multicompartmental Analysis of [11C]-Carfentanil Binding to Opiate Receptors in Humans Measured by Positron Emission Tomography
  • J. Frost, K. Douglass, +6 authors H. Wagner
  • Chemistry, Medicine
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 1989
The region/occipital cortex ratio can be used to quantitate changes in k3/k4 when tracer kinetic modeling is not feasible.
Mapping of Histamine H1 Receptors in the Human Brain Using [11C]Pyrilamine and Positron Emission Tomography
The availability of this method for measuring histamine H1 receptors in vivo in humans will facilitate studies on neurological and psychiatric disorders in which histamineH1 receptors are thought to be abnormal.
Mu‐opiate receptors measured by positron emission tomography are increased in temporal lobe epilepsy
Patients with complex partial seizures due to unilateral temporal seizure foci were studied by positron emission tomography using 11C‐carfentanil to measure mu‐opiate receptors and 18F‐fluoro‐deoxy‐D‐glucose to measure glucose utilization, and increased opiate receptors in the temporal neocortex may represent a tonic anticonvulsant system that limits the spread of electrical activity from other temporal lobe structures.
μ Opiate receptors are selectively labelled by [3H]carfentanil in human and rat brain
[11C]Carfentanil is a potent opioid agonist currently in use as a specific PET (position emission tomography) scan radioligand for brain μ opioid receptors. In order to investigate the receptor
Regional cerebral opioid receptor studies with [11C]diprenorphine in normal volunteers
The results with a ligand that is safe and without side-effects, suggest that this technique is suitable for studies of opioid physiology in man.
Regional distribution of the opioid receptor agonist N-(methyl-11C)pethidine in the brain of the rhesus monkey studied with positron emission tomography.
The regional distribution and kinetics in the brain of Rhesus monkeys of N-(methyl-11C)-pethidine have been studied by positron emission tomography, PET and indicates that pethidine is bound with low affinity to the opioid receptors and is a poor ligand for studies of opioid receptor function with PET.
Quantification of mu and non–mu opiate receptors in temporal lobe epilepsy using positron emission tomography
The variation in pattern of carfentanil and diprenorphine binding supports a differential regulation of opiate subtypes in unilateral temporal lobe epilepsy.
Quantification of Neuroreceptors in the Living Human Brain. II. Inhibition Studies of Receptor Density and Affinity
  • D. Wong, A. Gjedde, +4 authors M. Kuhar
  • Chemistry, Medicine
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 1986
This work varied k3 by reducing the number of available receptors with a previously administered receptor blocking agent, haloperidol, and calculated a receptor density of 9.2 pmol g−1 in the caudate nucleus of four normal volunteers, and an inhibitory constant of hal operidol of 1.4 nM by comparing tracer accumulation in the absence and the presence of the blocking agent.
Opioid receptor imaging in man
The existence of opioid receptors (OR) had long been suspected, but their demonstration in nervous tissue and the discovery of their natural ligands did not come until the 1970’s. By 1985, the study