Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist

P G Wyatt; M J Allen; J Chilcott; G Hickin; N D Miller; P M Woollard

doi:10.1016/s0960-894x(01)00202-5

Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist

Bioorg Med Chem Lett. 2001 May 21;11(10):1301-5. doi: 10.1016/s0960-894x(01)00202-5.

Authors

P G Wyatt¹, M J Allen, J Chilcott, G Hickin, N D Miller, P M Woollard

Affiliation

¹ Department of Medicinal Chemistry, GlaxoSmithKline, Medicines Research Centre, Stevenage, Herts, UK. [email protected]

PMID: 11392542
DOI: 10.1016/s0960-894x(01)00202-5

Abstract

We have investigated the structure-activity relationships of the 1- and 3-substituents and replacements of the 5-phenyl group of GW405212X 1, a potent selective oxytocin antagonist. The effect of these modifications on oxytocin binding antagonism and on pharmacokinetic parameters is reported.

MeSH terms

Administration, Oral
Animals
Benzodiazepines / chemical synthesis
Benzodiazepines / pharmacokinetics
Benzodiazepines / pharmacology*
Biological Availability
Dogs
Humans
Inhibitory Concentration 50
Injections, Intravenous
Oxytocin / antagonists & inhibitors*
Oxytocin / metabolism
Peptide Library
Protein Binding
Receptors, Oxytocin / metabolism
Structure-Activity Relationship
Tocolytic Agents / chemical synthesis*
Tocolytic Agents / pharmacokinetics
Tocolytic Agents / pharmacology

Substances

Peptide Library
Receptors, Oxytocin
Tocolytic Agents
Benzodiazepines
Oxytocin