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Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2
- Publication Year :
- 2005
- Publisher :
- Blackwell Munksgaard:PO Box 2148, Periodicals Department, DK-1016 Copenhagen K Denmark:011 45 33 755913, EMAIL: agentservices@oxon.blackwellpublishing.com, INTERNET: http://www.blackwellmunksgaard.com, Fax: 011 45 77 333377, 2005.
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Abstract
- In the present study we describe the in vitro pharmacological characterization of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) ligand Ac-RYYRWK-NH2 and the synthesis and biological evaluation of 13 Trp5 substituted Ac-RYYRWK-NH2 analogs. Results indicate that Ac-RYYRWK-NH2 behaves as a highly potent and selective partial agonist at the NOP receptors and that the whole indole moiety of the Trp5 side chain is not required, being a phenyl-ethyl side chain already sufficient for maintaining high potency.
- Subjects :
- Male
Mice, Knockout
NOP receptor
Dose-Response Relationship, Drug
nociceptin/ orphanin FQ
structure activity study
Tryptophan
Electric Stimulation
NO
Ac-RYYRWK-NH2
Amino Acids, Aromatic
Mice
Structure-Activity Relationship
Vas Deferens
nociceptin/orphanin FQ
Opioid Peptides
mouse vas deferens
Animals
Amino Acid Sequence
Oligopeptides
Cells, Cultured
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.pmid.dedup....36ef6aeed200eeb84523fa5fa544d69f