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Piperazinyl benzamidines: Synthesis and affinity for the delta opioid receptor
- Source :
- Bioorganic & Medicinal Chemistry Letters. 11:1741-1743
- Publication Year :
- 2001
- Publisher :
- Elsevier BV, 2001.
-
Abstract
- Piperazinyl benzamidines were prepared and found to bind to the rat delta (δ) opioid receptor. The most active compounds had a N,N -diethylcarboxamido group and a N -benzyl piperazine. The most potent among these was N,N -diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide ( 27 ) with a 1.22 nM K i for the rat δ opioid receptor and ca. 1000× selectivity relative to the μ opioid subtype.
- Subjects :
- Stereochemistry
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Chemical synthesis
Piperazines
δ-opioid receptor
chemistry.chemical_compound
Opioid receptor
Receptors, Opioid, delta
Drug Discovery
medicine
Animals
Benzamide
Molecular Biology
Trifluoromethyl
Organic Chemistry
Benzamidines
Rats
Piperazine
chemistry
Opioid
Molecular Medicine
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....fe9ff93efab48169b8e2c8795ff77591