1024829-72-8Relevant academic research and scientific papers
KAPPA OPIOID RECEPTOR PEPTIDE AMIDE AGONISTS
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Paragraph 0089; 0091, (2021/02/12)
The present invention provides kappa opioid receptor peptide agonists, methods for preparing these compounds, compositions comprising these kappa opioid receptor peptide agonists, and methods of using the kappa opioid receptor peptide agonists to treat pain or other conditions.
POLYAMIDE COMPOUND AND USE THEREOF
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Paragraph 0190, (2019/08/20)
The invention relates to a polyamide compound and a use thereof. Specifically, the invention relates to a type of polyamide compound (which preferably comprise one or more amide bonds formed by condensation of same or different L-amino acids or D-amino acids), or stereoisomers, crystalline polymorphs, solvates, metabolites, prodrugs or pharmaceutically acceptable salts or esters thereof, or pharmaceutical compositions thereof, as well as a method for preparing the polyamide compound and a use thereof in the prevention or treatment of diseases associated with κ-opioid receptor. The polyamide compound of the invention has excellent κ-opioid receptor agonistic activity and hydrophilicity, thus having a lesser ability of penetrating the blood-brain barrier and a lower capacity for entering the brain. The compound of the invention has higher selectivity for a κ-opioid receptor, lower addictiveness, improved pharmacokinetic properties, and improved safety (lower toxicity and/or fewer side effects), good patient compliance, and/or lesser propensity for developing tolerance, among other excellent medicinal properties.
Synthetic peptide amides
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Page/Page column 6; 63; 64; sheet 4, (2008/12/07)
The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
