Characterization of vanilloid receptors in the dorsal horn of pig spinal cord

@article{Szallasi1991CharacterizationOV,
  title={Characterization of vanilloid receptors in the dorsal horn of pig spinal cord},
  author={A. Szallasi and P. Blumberg},
  journal={Brain Research},
  year={1991},
  volume={547},
  pages={335-338}
}
Specific [3H]resiniferatoxin binding is thought to represent the postulated vanilloid (capsaicin) receptor. We have previously characterized [3H]resiniferatoxin binding to membranes from rat and pig dorsal root ganglia, which contain the cell bodies of capsaicin-sensitive primary afferent neurons. We now demonstrate specific binding of [3H]resiniferatoxin to particulate preparations from pig dorsal horn, which contains the central nerve endings of the capsaicin-sensitive primary afferent… Expand
The vanilloid (capsaicin) receptor: receptor types and species differences.
TLDR
Differences in receptor binding along with the pharmacokinetical differences in tissue equilibration and in plasma binding may form a rational basis to explain the peculiar spectrum of actions of RTX. Expand
Visualizing vanilloid (capsaicin) receptors in pig spinal cord by [3H]resiniferatoxin autoradiography
TLDR
It is concluded that [3H]RTX autoradiography may afford a novel neurochemical approach to detect localized changes in vanilloid receptor expression. Expand
[3H]resiniferatoxin binding to pig dorsal horn membranes displays positive cooperativity.
TLDR
The findings suggest that the vanilloid receptor present in the dorsal horn of the pig, like those present in human and in the rat, is a receptor cluster in which the subunits cooperate. Expand
Vanilloid (capsaicin) receptors in the rat: distribution in the brain, regional differences in the spinal cord, axonal transport to the periphery, and depletion by systemic vanilloid treatment
TLDR
The present results suggest a discrete expression of vanilloid receptors in the brain stem (sensory nuclei); although intrinsic vanilloids receptor-expressing neurons are though to exist in the rat brain, they remain undetected by the present [3H]RTX autoradiography methodology. Expand
Inhibition of [3H]resiniferatoxin binding to rat dorsal root ganglion membranes as a novel approach in evaluating compounds with capsaicin-like activity
TLDR
Comparing the structure/activity relations for binding to rat dorsal root ganglion membranes and for biological responses in the rat, using a series of vanilloids of the capsaicin and resiniferatoxin classes concludes that the [3H]resiniferat toxin binding assay may provide an efficient approach for evaluating such compounds. Expand
Binding of neuroleptic drugs (trifluoperazine and rimcazole) to vanilloid receptors in porcine dorsal horn.
TLDR
Capsazepine appears to bind to vanilloid receptors in a non-cooperative fashion, or at least with much reduced positive cooperativity in this system, which is in accord with previous findings in human spinal cord but contrast with those in the rat. Expand
Distinct structure-activity relations for stimulation of 45Ca uptake and for high affinity binding in cultured rat dorsal root ganglion neurons and dorsal root ganglion membranes.
TLDR
Structural-activity analysis of different vanilloid derivatives revealed that the various compounds have distinct potencies for receptor binding and inducing 45Ca uptake in rat dorsal root ganglion neurons. Expand
Characterization of resiniferatoxin binding sites on sensory neurons: Co-regulation of resiniferatoxin binding and capsaicin sensitivity in adult rat dorsal root ganglia
TLDR
Adult rat dorsal root ganglion neurons cultured without nerve growth factor also lost their capsaicin-sensitivity and showed reduced resiniferatoxin binding, suggesting capsicin responses in sensory neurons may be regulated by nerve growthFactor through control of the number of capsaicIn receptors. Expand
Capsaicin activates a nonselective cation channel in cultured neonatal rat dorsal root ganglion neurons
  • U. Oh, S. Hwang, D. Kim
  • Chemistry, Medicine
  • The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1996
TLDR
The properties of CAP-activated single channels in cultured neonatal rat DRG neurons are identified and described and it is shown that opening of these ligand-gated, cation-selective channels gives rise to the whole-cell CAP- activated current in DRG neuron and may underlie the neurotoxic effects of CAP. Expand
Molecular cloning of a resiniferatoxin-binding protein.
TLDR
RBP-26 is expressed in non-neuronal and capsaicin-insensitive neuronal tissues, and shows distinct binding characteristics from the resiniferatoxin binding site defined on DRG membranes, and the functional role of RBP-26 remains to be established. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 15 REFERENCES
Specific binding of resiniferatoxin, an ultrapotent capsaicin analog, by dorsal root anglion membranes
TLDR
Specific binding of [3H]RTX to particulate preparations from dorsal root ganglia (DRG), a target tissue of both RTX and Capsaicin action, appears to represent the postulated capsaicin receptor. Expand
Similarities and differences in the action of resiniferatoxin and capsaicin on central and peripheral endings of primary sensory neurons
TLDR
Comparing the ability of capsaicin and resiniferatoxin, a natural diterpene present in the latex of plants of the Euphorbia family, to excite and desensitize Capsaicin-sensitive primary afferents in a variety of models suggests a slower penetration rate in the tissue. Expand
Roles of substance P and somatostatin on transmission of nociceptive information induced by formalin in spinal cord.
TLDR
The results suggest that SP participates in the transient pain induced by such acute stimuli as hot plate, tail pinch and the first phase of Formalin response and that SST participate in the prolonged and inflammatory paininduced by stimuli such as acetic acid and the second phase response. Expand
The sensory-efferent function of capsaicin-sensitive sensory neurons.
TLDR
Development of drugs capable of controlling the sensory-efferent functions of the capsaicin-sensitive sensory neurons represent a new and very promising area of research for pharmacological treatment of various human diseases. Expand
Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper
TLDR
It is concluded that resiniferatoxin acts as an ultrapotent capsaicin analog and hypothesize that it may distinguish between subclasses of Capsicum response, as well as investigate its mechanism of action. Expand
Duration of desensitization and ultrastructural changes in dorsal root ganglia in rats treated with resiniferatoxin, an ultrapotent capsaicin analog
TLDR
The duration of desensitization following acute treatment with the maximal tolerated dose of resiniferatoxin is examined to find that, in comparison with capsaicin treatment, RTX caused more long-lasting desensItization as well as a distinct spectrum of response. Expand
Tachykinins and calcitonin gene-related peptide enhance release of endogenous glutamate and aspartate from the rat spinal dorsal horn slice
  • I. Kangrga, M. Randić
  • Chemistry, Medicine
  • The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1990
TLDR
The results indicate that tachykinins (SP and NKA) and CGRP are capable of modulating the basal and electrically evoked release of endogenous Glu and Asp, and these actions may provide an important mechanism by which the peptides contribute to the regulation of the primary afferent synaptic transmission. Expand
Perspectives of Capsaicin-Type Agents in Pain Therapy and Research
There is a “ painfully” absent chapter in pharmacological textbooks, which could be entitled: “Drugs acting on sensory neurons” or “Sensory neuron-blocking analgesics.” For over 100 years, varietiesExpand
Structure/activity analysis of resiniferatoxin analogs
Resiniferatoxin (RTX), unlike the structurally related phorbol esters, acts as an ultrapotent analog of capsaicin, the pungent principle of the red pepper. A homovanillyl group is an essentialExpand
Ligand: a versatile computerized approach for characterization of ligand-binding systems.
TLDR
This approach provides two major advantages compared with other available methods: it uses an exact mathematical model of the ligand-binding system, thereby avoiding the possible biases introduced by several commonly used approximations and it uses a statistically valid, appropriately weighted least-squares curve-fitting algorithm with objective measurement of goodness of fit. Expand
...
1
2
...