Delving into the Latest Updates on FR-76830 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

ATPase

Mechanism

ATPase stimulants

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication-

Inactive Indication

Angina Pectoris

Originator Organization

Fujisawa Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Fujisawa Pharmaceutical Co., Ltd.

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

STUDY OBJECTIVEThe aim was to investigate the effects of a newly synthesised bradycardiac agent, FR 76830, on cardiac mechanical function and metabolism during ischaemia and reperfusion.DESIGNFR 76830 and diltiazem were infused during 15 min before ischaemia. Hearts were then subjected to ischaemia (40 min) followed by reperfusion (40 min). High energy phosphate compounds and myocardial pH were assessed by 31P-NMR. The effects of bradycardia induced by FR 76830 before induction of ischaemia on the metabolic derangement resulting from ischaemia and on functional and metabolic recovery after reperfusion were examined in comparison with diltiazem.EXPERIMENTAL MATERIALMale Wistar rats (about 250 g) were used.MEASUREMENTS AND MAIN RESULTSFR 76830 and diltiazem produced a dose dependent decrease in heart rate before ischaemia. However, the decrease in the double product (heart rate x left ventricular pressure) was observed only with diltiazem. Both FR 76830 and diltiazem attenuated the fall in myocardial pH during early ischaemia and improved the level of ATP during late ischaemia. Diltiazem also produced an improvement in myocardial acidosis during late ischaemia and in the level of ATP during early ischaemia.CONCLUSIONSThe importance of bradycardia in protection of the myocardial cells during early ischaemia and in preservation of ATP content during late ischaemia and after reperfusion was shown. However, to produce an improvement in myocardial pH during late ischaemia a decrease in the double product is needed.

100 Deals associated with FR-76830

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