Abstract:
:In this study the desensitizing power of increasing concentrations of resiniferatoxin applied topically to the bladder mucosa, and the irritating properties of the most effective desensitizing dose, were determined with the aid of the spinal expression of the proto-oncogene c-fos. Desensitization was assessed by the decrease in the number of Fos-immunoreactive spinal neurons induced by the intravesical instillation of 1% acetic acid, when the latter was preceded by resiniferatoxin in concentrations between 1 and 1000 nM. Irritation, as shown by the noxious excitation of vesical sensory innervation, was measured by the c-fos response evoked by a single application of resiniferatoxin. As to the desensitizing power, resiniferatoxin produced a dose-dependent effect with a maximum at 100 nM, which decreased Fos-immunoreactive cell numbers to less than 10% of controls. No further decrease of c-fos activation occurred at 1000 nM. As to the irritating power, the saturation dose of resiniferatoxin (100 nM) produced a very weak c-fos activation in lumbosacral spinal cord segments. These data show that in an effective desensitizing concentration, resiniferatoxin is virtually devoid of nociceptive effects, in agreement with current clinical observations.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Avelino A,Cruz F,Coimbra Adoi
10.1016/s0014-2999(99)00451-3keywords:
subject
Has Abstractpub_date
1999-07-28 00:00:00pages
17-22issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(99)00451-3journal_volume
378pub_type
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