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Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 25:30-33
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- It has been shown that under chronic pain or nerve injury conditions, up-regulated dynorphin A (Dyn A) interacts with bradykinin receptors (BRs) to cause hyperalgesia in the spinal cord. Thus BRs antagonist can modulate hyperalgesia by blocking Dyn A’s interaction with the BRs in the central nervous system. In our earlier structure–activity relationship (SAR) study, [des-Arg 7 ]-Dyn A-(4–11) 13 was discovered as a minimum pharmacophore for rat brain BRs with its antagonist activity (anti-hyperalgesic effect) in in vivo tests using naive or injured animals. We have pursued further modification on the [des-Arg 7 ]-Dyn A analogues and identified a key insight into the pharmacophore of the rat brain BRs: amphipathicity.
- Subjects :
- medicine.medical_specialty
Clinical Biochemistry
Central nervous system
Pharmaceutical Science
Bradykinin
Dynorphin
Pharmacology
Dynorphins
Biochemistry
Article
Structure-Activity Relationship
chemistry.chemical_compound
Internal medicine
Drug Discovery
medicine
Animals
Molecular Biology
Chemistry
Receptors, Bradykinin
fungi
Organic Chemistry
Antagonist
Brain
Dynorphin A
respiratory system
Rats
Endocrinology
medicine.anatomical_structure
Opioid
Hyperalgesia
Molecular Medicine
medicine.symptom
Pharmacophore
circulatory and respiratory physiology
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....0c07cfebda0e4078ede1b61566162e4e