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OT antagonist 1

Names

[ CAS No. ]:
479080-38-1

[ Name ]:
OT antagonist 1

Biological Activity

[Description]:

OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor
Research Areas >> Endocrinology

[Target]

Ki: 50 nM (Oxytocin)[1]


[In Vitro]

Oxytocin (OT) is a nonapeptide hormone that acts on the OT receptor, a seven-transmembrane (7TM) (Gq-coupled) receptor. The OT receptor has no subtypes but is related to the vasopressin receptors V1A, V1B and V2. OT antagonists have therapeutic potential in a number of areas including pre-term labour: Benign Prostatic Hyperplasia and sexual dysfunction. As a result there is significant interest in the identification of potent, selective, orally bioavailable OT antagonists[1].

[References]

[1]. Brown A, et al. Design and optimization of potent, selective antagonists of Oxytocin. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4278-81.


[Related Small Molecules]

Oxytocin acetate | Carbetocin Acetate | PF-3274167 | OT-R antagonist 1 | L-368,899 hydrochloride | GSK 557296 | OT antagonist 3 | Retosiban

Chemical & Physical Properties

[ Molecular Formula ]:
C22H22N4O3

[ Molecular Weight ]:
390.44


Related Compounds