Delving into the Latest Updates on Y-20487 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Mechanism

3',5'-cyclic-AMP phosphodiesterases inhibitors

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Heart Failure

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization-

Inactive Organization

Mitsubishi Pharma Corp.

Mitsubishi Tanabe Pharma Corp.

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC12H11N3O2S

InChIKeyQPPSCFGHRUEFFS-UHFFFAOYSA-N

CAS Registry103969-58-0

The effect of a new cardiotonic agent Y-20487 [6-(3,6-dihydro-2-oxo-2H-1,3,4-thiadiazin-5-yl)-3,4-dihydro-2(1H)- quinolinone] on cyclic AMP levels of rat ventricular cardiomyocytes and the contractile force of papillary muscles was investigated in comparison with selective cyclic AMP phosphodiesterase (PDE) inhibitors, milrinone (PDE-III selective), rolipram and Ro 20-1724 (PDE-IV selective), and a nonselective inhibitor 3-isobutyl-1-methylxanthine (IBMX). Rolipram and Ro 20-1724 did not elicit cyclic AMP accumulation and positive inotropy, but they potentiated the isoproterenol (ISO)-induced cyclic AMP accumulation more effectively than IBMX. Rolipram was more effective than Ro 20-1724 in enhancing ISO-induced cyclic AMP accumulation but was less effective in enhancing the ISO-induced positive inotropic effect, indicating that these agents produce a differential action on cyclic AMP metabolism and inotropy. Milrinone and Y-20487 elicited cyclic AMP accumulation and positive inotropy by themselves. Whereas milrinone scarcely affected the ISO-induced effects, Y-20487 shifted the concentration-response curve for the positive inotropic effect of ISO to the left to the same extent that IBMX did. Y-20487, however, was much less effective than IBMX in enhancing the ISO-induced cyclic AMP accumulation. The present results indicate that in rat ventricular myocardium, PDE-IV may play a crucial role in breakdown of cyclic AMP generated by beta-adrenoceptor stimulation, whereas other types of PDE isoenzymes, including PDE-III, may be responsible for the cyclic AMP accumulation and direct positive inotropic effect induced by PDE inhibitors.(ABSTRACT TRUNCATED AT 250 WORDS)

100 Deals associated with Y-20487

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Heart Failure	Phase 1	-	Mitsubishi Tanabe Pharma Corp.	-
Heart Failure	Phase 1	-	Mitsubishi Tanabe Pharma Corp.	-
Heart Failure	Phase 1	JP	Mitsubishi Pharma Corp.	-
Heart Failure	Phase 1	JP	Mitsubishi Pharma Corp.	-