Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia

@article{Pintr2002PharmacologicalCO,
  title={Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia},
  author={Erika Pint{\'e}r and Zsuzsanna Helyes and J{\'o}zsef N{\'e}meth and R{\'o}bert P{\'o}rsz{\'a}sz and G{\'a}bor Peth{\"o} and Márta Thán and György Kéri and Anikó Horváth and Bal{\'a}zs Jakab and János Szolcsányi},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2002},
  volume={366},
  pages={142-150}
}
Abstract.The putative anti-inflammatory and anti-nociceptive activity of the heptapeptide somatostatin analogue TT-232 (D-Phe-Cys-Tyr-D-Thr-Lys-Cys-Thr-NH2) was investigated in the rat and mouse, as well as its effect on neuropathic hyperalgesia, gastric ulceration and the release of sensory neuropeptides. In the rat, carrageenin-induced paw oedema was inhibited dose dependently by TT-232 (3×2.5–20 µg/kg i.v.). Evans blue accumulation induced by intraarticular bradykinin injection (0.5 nmol in… 

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References

SHOWING 1-10 OF 49 REFERENCES

Anti‐inflammatory effect of synthetic somatostatin analogues in the rat

It is concluded that somatostatin analogues without endocrine functions as TT‐232 are promising compounds with a novel site of action for inhibition of non‐neurogenic and neurogenic inflammatory processes.

Release of somatostatin and its role in the mediation of the anti‐inflammatory effect induced by antidromic stimulation of sensory fibres of rat sciatic nerve

The inhibitory effect of antidromic sciatic nerve excitation on plasma extravasation in response to vagal nerve stimulation was also prevented by somatostatin antiserum pretreatment, and plasma levels of som atostatin increased more than 4 fold after stimulation of both sciatic nerves.

Somatostatin analogues suppress the inflammatory reaction in vivo.

The effects of two Sms octapeptide analogues on the inflammatory reaction in vivo suggest that Sms analogues have significant antiinflammatory effects in vivo, associated with suppression of proinflammatory cytokines and neuropeptides, and suggest thatSms agonists may be useful in the control of inflammatory reaction.

Somatostatin and Chronic Pain Management

There is increasing information that nonopioid peptides in the central nervous system play a role in pain physiology and pathophysiology, and somatostatin is apparently one of the most significant neuropeptides.

Reduction of non-steroidal anti-inflammatory drug induced gastric injury and leucocyte endothelial adhesion by octreotide.

Octreotide protects the stomach from NSAIDs induced gastric injury, probably via its ability to reduce NSAID induced neutrophilic adhesion to the microvasculature.

Inhibition by nociceptin of neurogenic inflammation and the release of SP and CGRP from sensory nerve terminals

Nociceptin inhibits the release of sensory neuropeptides from terminals of nociceptive neurones in rat isolated tracheae in response to electrical field stimulation.

Substance P, neurokinin A, and neurokinin B induce generation of IL-1-like activity in P388D1 cells. Possible relevance to arthritic disease.

The results suggest that activation of immune cells by neuromodulators can contribute to the maintenance of the chronic inflammatory state and the immunopathology observed in arthritic disease mediated by IL-1, and suggest that one approach to the treatment of rheumatoid arthritis might be to attempt to inhibit the local effects of immuno-modulatory neuropeptides in affected joints.