Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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: 2006-05-18
NEW ENGLAND MEDICAL CENT HOSPITALS +1
View PDF3 Cites 14 Cited by
  • 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, which helps in treating pain. The chimeric peptide can have multiple opioid and nociceptive moieties, which can be directed towards the same or different receptors. The chimeric peptides are soluble and can be administered through various routes such as intrathecally, intracerebrovertricularlly, or systemically. The chimeric peptides produce effective pain relief without causing tolerance."

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0067] 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.

[0068] 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 / ml bacitracin, 30 μg / ml bestatin and 5 mM MgCl1) 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...

example 2

Characterization of the Analgesic Properties of ESP7

[0072] 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.

[0073] 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 ESP7 does not contribute to the analgesia, but rather plays an inte...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
pHaaaaaaaaaa
volumeaaaaaaaaaa
diameteraaaaaaaaaa
Login to View More

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 AS fibers and C fibers. AS fibers are small diameter, 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 AS or C from the damaged periphery synapse release a va...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): C07K14/675A61K38/22A61K38/00C07K7/22C07K19/00
CPCA61K38/00C07K7/22C07K19/00A61P25/00
Inventor CARR, DANIELLIPKOWSKI, ANDRZEJKREAM, RICHARDMISICKA-KESIK, ALEKSANDRA
Owner NEW ENGLAND MEDICAL CENT HOSPITALS
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com