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Novel Chimeric Analgesic Peptides

a peptide and chimeric technology, applied in the field of pain treatment methods and compositions, can solve the problems of lowering the threshold for activation of nociceptors, frequent side effects, pruritis, etc., and achieves the effects of inhibiting the development of tolerance, enhancing the solubility of chimeric peptides, and reducing the risk of side effects

Inactive Publication Date: 2009-12-03
NEW ENGLAND MEDICAL CENT HOSPITALS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a new chimeric peptide that can bind to both an opioid receptor and a nociceptive receptor, such as NK1. This peptide can be used to treat pain by administering it alone or in combination with other opioid drugs. The advantage of this invention is that it produces effective pain relief without causing tolerance. The details of the invention are described in the accompanying patent text.

Problems solved by technology

Repeated stimulation of pain fibers can lead to hyperalgesia, or a lowering of the threshold for activation of nociceptors.
While opioids can be effective for the treatment of chronic pain, they frequently have side effects, including respiratory depression, urinary retention, nausea and vomiting, pruritis, and sedation.
Moreover, repeated daily administration of opioids eventually produces tolerance, whereby the dose of the drug must be increased in order to maintain adequate analgesia, and may also initiate physical dependence.
If tolerance develops and the level of opioids is insufficient, withdrawal symptoms such as diarrhea, sweating, tremors, anxiety, and fever may result.

Method used

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  • Novel Chimeric Analgesic Peptides
  • Novel Chimeric Analgesic Peptides
  • Novel Chimeric Analgesic Peptides

Examples

Experimental program
Comparison scheme
Effect test

example 1

In Vitro Binding of ESP7 to Opioid and SP Receptors in Rat Brain Preparations

[0068]In order to assess the binding affinity of ESP7 to opioid and SP receptor, binding assays to opioid and SP receptors were performed with crude rat brain plasma membranes prepared using a modified procedure of Zadina. Zadina et al., Life Sci, 55: 461-466 (1994). These assays showed that ESP7 has a strong affinity for both the μ receptor and the NK1 receptor in rat brain.

[0069]For binding assays to opioid receptors, frozen rat brains (−80° C.) were homogenized in 40 volumes of standard Tris buffer (50 mM Tris HCl (pH 7.4), 0.2 mg / ml BSA, 2.5 mM EDTA, 40 μg / m bacitracin, 30 μg / ml bestatin and 5 mM MgCl2) and centrifuged at 15,000×g for 20 minutes. 100 mM NaCl was added to the buffer, in order to remove endogenous ligands, and the centrifugation was repeated. After a wash with standard buffer, the membrane preparation was finally resuspended in 10 volumes of incubation buffer (standard buffer with 4 μg / ml...

example 2

Characterization of the Analgesic Properties of ESP7

[0073]ESP7 was tested clinically in rats to determine analgesic effect and tolerance. The classical tail flick test was used to measure pain response and thermal pain was mimicked using a heat source. This system was controlled using standard opioids. The drug was administered with cyclodextran to increase solubility of the peptide in an aqueous solution.

2.1 Intrathecal Administration of ESP7 in Rats and the Effects of Naltrexone and RP67580 Blockades

[0074]Intrathecal administration of ESP7 produced long-lasting analgesia without any significant development of tolerance. The opioid antagonist naltrexone blocked this analgesia, indicating that the analgesia was opioid in nature. Additionally, when the SP portion was antagonized with RP67580, an NK1 antagonist, tolerance to the drug developed within three days. These results indicate that the SP moiety of ESPY does not contribute to the analgesia, but rather plays an integral role in...

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Abstract

The present invention provides a novel chimeric peptide containing an opioid peptide moiety and a nociceptive peptide moiety for producing analgesia.

Description

FIELD OF THE INVENTION[0001]The present invention relates generally to methods and compositions for the treatment of pain. More specifically, the present invention relates to novel chimeric peptides for the treatment of pain.BACKGROUND OF THE INVENTION[0002]Two million people in the United States suffer from chronic pain. Pain is caused by a highly complex perception of an aversive or unpleasant sensation. The sensation of pain begins with noxious stimulation of free nerve endings, which leads to activation of different types of nociceptive afferent fibers. These fibers include Aδ fibers and C fibers. Aδ fibers are small diameters, thinly myelinated fibers that transmit sharp, prickling pain. C fibers are unmyelinated and conduct more slowly and transmit dull aching pain. Repeated stimulation of pain fibers can lead to hyperalgesia, or a lowering of the threshold for activation of nociceptors.[0003]Primary afferent fibers Aδ or C from the damaged periphery synapse release a variety ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/17A61K38/02A61K38/08A61K38/07A61P25/00A61K38/00C07K7/22C07K19/00
CPCA61K38/00C07K19/00C07K7/22A61P25/00
Inventor CARR, DANIEL B.LIPKOWSKI, ANDRZEJ W.KREAM, RICHARDMISICKA-KESIK, ALEKSANDRA
Owner NEW ENGLAND MEDICAL CENT HOSPITALS
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