Delving into the Latest Updates on TZE-5316 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Action-

Mechanism-

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Kyoto Prefectural University of Medicine

Active Organization-

Inactive Organization

Kyoto Prefectural University of Medicine

License Organization-

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H22O4

InChIKeyNJCVVDNNBCUQAG-JPVZDGGYSA-N

CAS Registry217476-05-6

Endothelin (ET) is a vasoconstrictor peptide produced by endothelial cells.Among three isoforms, ET-1 has been found to be an important factor regulating vasoconstriction both in normal and pathol. conditions, such as pregnancy-induced hypertension (PIH).PIH is considered induced by various factors.Among these factors, endothelial cell injury is regarded as one of the most important, and elevated serum lipid peroxide in PIH is toxic to endothelial cells.T-butylhydroperoxide (TBH), one of the lipid peroxides, revealed its oxidative effect by increasing ⁵¹Cr release from human umbilical vein endothelial cells (HUVEC).Ascorbic acid, a strong antioxidative substance, suppressed TBH-induced injury.TBH decreased ET-1 production and release from HUVEC at 60 min, but increased it later at 120 and 300 min.In ET-1 mRNA expression, TBH initially decreased this expression at 30 min, but it was later increased at 60 and 120 min.This suggested that TBH initially decreased ET-1 production, then later increased it.In ET-A receptor (ET_AR) mRNA expression, there was no specific change noted.In ET-B receptor (ET_BR) mRNA expression, there was no change recognized at 30 min.However, TBH decreased this expression at 60 min, then increased it at 120 min compared with control values.A newly synthesized estrogen derivative, TZE-5316 (2,3-dihydroxy-D-homo-17-oxaestra-1,3,5(10)-trien-17a-one) has a strong antioxidative effect as strong as ascorbic acid.TZE-5316 suppressed all oxidative changes of TBH described above.This new steroid was suggested to be an effective agent for PIH.

100 Deals associated with TZE-5316

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