N-(3-acyloxy-2-benzylpropyl)-N'-dihydroxytetrahydrobenzazepine and tetrahydroisoquinoline thiourea analogues as vanilloid receptor ligands.
Bioorg Med Chem
; 9(7): 1713-20, 2001 Jul.
Article
in En
| MEDLINE
| ID: mdl-11425572
ABSTRACT
The vanilloid receptor represents a promising target for drug development. Building on our previous strategies which have generated potent agonists for VR1, we now describe a series of novel N-(3-acyloxy-2-benzylpropyl)-N'-dihydroxytetrahydrobenzazepine and tetrahydroisoquinoline thiourea analogues, several of which are potent VR1 antagonists. We report here the rationale for the design, the synthesis, and the in vitro characterization of activity in assays for [(3)H]resiniferatoxin binding and (45)Ca influx using heterologously expressed rat VR1.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, Drug
/
Thiourea
/
Benzazepines
/
Isoquinolines
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2001
Document type:
Article