TT-232. Somatostatin sst1/sst4 receptor agonist, treatment of neuropathic pain, treatment of inflammation

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Abstract

The treatment of the neurogenic component of inflammatory diseases and neuropathic pain remains an unresolved issue in pharmacotherapy. A novel endogenous antiinflammatory/analgesic mechanism mediated by somatostatin released from capsaicin-sensitive sensory nerve terminals has been identified and reported by our research group. These findings raised the possibility of targeting somatostatin receptors to decrease inflammation and nociception. Native somatostatin cannot be used in clinical practice due to its short plasma half-life and broad range of actions, but stable and selective synthetic analogues might open new perspectives for drug development. A cyclic heptapeptide analogue, TT-232, showing the greatest affinity for the somatostatin sst4 receptor subtype was synthesized at the Peptide Chemistry Research Group of the Hungarian Academy of Sciences and proved to have no endocrine activity. On the other hand, it exerted significant inhibitory effects in several acute and chronic inflammatory and nociceptive animal models, including chronic arthritis, mono- and polyneuropathy conditions. TT-232 is therefore considered a promising lead molecule for the development of a completely new type of antiinflammatory/analgesic agents.

Original languageEnglish
Pages (from-to)558-566
Number of pages9
JournalDrugs of the Future
Volume30
Issue number6
DOIs
Publication statusPublished - Jun 2005

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Somatostatin Receptors
Neuralgia
Somatostatin
Analgesics
Anti-Inflammatory Agents
Mononeuropathies
Inflammation
Nociception
Polyneuropathies
Capsaicin
Research
Arthritis
Half-Life
Animal Models
Drug Therapy
Peptides
Therapeutics
Pharmaceutical Preparations
TT2-32
somatostatin receptor subtype-4

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

Cite this

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title = "TT-232. Somatostatin sst1/sst4 receptor agonist, treatment of neuropathic pain, treatment of inflammation",
abstract = "The treatment of the neurogenic component of inflammatory diseases and neuropathic pain remains an unresolved issue in pharmacotherapy. A novel endogenous antiinflammatory/analgesic mechanism mediated by somatostatin released from capsaicin-sensitive sensory nerve terminals has been identified and reported by our research group. These findings raised the possibility of targeting somatostatin receptors to decrease inflammation and nociception. Native somatostatin cannot be used in clinical practice due to its short plasma half-life and broad range of actions, but stable and selective synthetic analogues might open new perspectives for drug development. A cyclic heptapeptide analogue, TT-232, showing the greatest affinity for the somatostatin sst4 receptor subtype was synthesized at the Peptide Chemistry Research Group of the Hungarian Academy of Sciences and proved to have no endocrine activity. On the other hand, it exerted significant inhibitory effects in several acute and chronic inflammatory and nociceptive animal models, including chronic arthritis, mono- and polyneuropathy conditions. TT-232 is therefore considered a promising lead molecule for the development of a completely new type of antiinflammatory/analgesic agents.",
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AB - The treatment of the neurogenic component of inflammatory diseases and neuropathic pain remains an unresolved issue in pharmacotherapy. A novel endogenous antiinflammatory/analgesic mechanism mediated by somatostatin released from capsaicin-sensitive sensory nerve terminals has been identified and reported by our research group. These findings raised the possibility of targeting somatostatin receptors to decrease inflammation and nociception. Native somatostatin cannot be used in clinical practice due to its short plasma half-life and broad range of actions, but stable and selective synthetic analogues might open new perspectives for drug development. A cyclic heptapeptide analogue, TT-232, showing the greatest affinity for the somatostatin sst4 receptor subtype was synthesized at the Peptide Chemistry Research Group of the Hungarian Academy of Sciences and proved to have no endocrine activity. On the other hand, it exerted significant inhibitory effects in several acute and chronic inflammatory and nociceptive animal models, including chronic arthritis, mono- and polyneuropathy conditions. TT-232 is therefore considered a promising lead molecule for the development of a completely new type of antiinflammatory/analgesic agents.

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