INAMRINONE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H9N3O
Molecular Weight	187.198
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

NC1=CC(=CNC1=O)C2=CC=NC=C2

InChI

InChIKey=RNLQIBCLLYYYFJ-UHFFFAOYSA-N

InChI=1S/C10H9N3O/c11-9-5-8(6-13-10(9)14)7-1-3-12-4-2-7/h1-6H,11H2,(H,13,14)

HIDE SMILES / InChI

Molecular Formula	C10H9N3O
Molecular Weight	187.198
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Inamrinone (Amrinone) is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. Inamrinone is a phosphodiesterase inhibitor (PDE3), resulting in increased cAMP and cGMP which leads to an increase in the calcium influx like that caused by beta-agonists resulting in increased inotropic effect. Inamrinone is used in the treatment of congestive heart failure.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Phosphodiesterase 3A 7	Inhibitor 8,504	16.7 µM [IC50]
Phosphodiesterase 3B 8	Inhibitor 8,504	31.2 µM [IC50]
platelet aggregation 80	Inhibitor 8,504	61.0 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Congestive heart failure 54	Primary		Approved 8,583	AMRINONE LACTATE

C_max

Value	Dose	Co-administered	Analyte	Population
5.2 μg/mL	0.75 mg/kg 3 times / day steady-state, intravenous		INAMRINONE plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
245 μg × h/mL	0.75 mg/kg 3 times / day steady-state, intravenous		INAMRINONE plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
5.4 h	0.75 mg/kg 3 times / day steady-state, intravenous		INAMRINONE plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
198 ug/kg/min 1 times / day single, intravenous Overdose	unhealthy, 0.208333333333333	Other AEs: Death...
198 ug/kg/min 1 times / day single, intravenous Overdose	unhealthy, 0.208333333333333	Other AEs: Cardiac arrest...
100 mg 3 times / day multiple, oral Recommended	unhealthy, 49	Disc. AE: Pulmonary edema, Cardiac arrest...
200 mg 3 times / day multiple, oral Highest studied dose	unhealthy, 53	Disc. AE: Diarrhea, Thrombocytopenia...
5.8 mg/kg/day 1 times / day multiple, intravenous Recommended	unhealthy, 59.4 (37-81)	Disc. AE: Thrombocytopenia...

Showing 1 to 5 of 6 entries

Previous1 2Next

AEs

Show entries

AE	Significance	Dose	Population
Death	grade 5	198 ug/kg/min 1 times / day single, intravenous Overdose	unhealthy, 0.208333333333333
Cardiac arrest		198 ug/kg/min 1 times / day single, intravenous Overdose	unhealthy, 0.208333333333333
Cardiac arrest	Disc. AE	100 mg 3 times / day multiple, oral Recommended	unhealthy, 49
Chest pain	Disc. AE	100 mg 3 times / day multiple, oral Recommended	unhealthy, 49
Palpitations	Disc. AE	100 mg 3 times / day multiple, oral Recommended	unhealthy, 49

Showing 1 to 5 of 11 entries

Previous1 2 3Next

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B1-00216	http://www.3bsc.com/index/pro_info.php?id=20428
3B Scientific (Wuhan) Corp	3B2-0633	http://www.3bsc.com/index/pro_info.php?id=19989
Acadechem	ACDS-033154	http://www.acadechemical.com/product/107853
Achemo Scientific Limited	AC-16677	http://www.achemo.com/search/?Keyword= 60719-84-8
Achemtek	0104-017105	http://www.achemtek.com/60719-84-8

Showing 1 to 5 of 47 entries

Previous1 2 3 4 5…10Next

PubMed

Show entries

Title	Date	PubMed
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.	2000 Feb 15	10644042
Adenylate cyclase/protein kinase A signaling pathway enhances angiogenesis through induction of vascular endothelial growth factor in vivo.	2001 Nov	11885966
Role of cyclic nucleotides in ischemia and reperfusion injury of canine livers.	2002 Apr 15	11965029
The effectiveness and relative effectiveness of intravenous inotropic drugs acting through the adrenergic pathway in patients with heart failure-a meta-regression analysis.	2002 Aug	12167393
Intraoperative insulin therapy does not reduce the need for inotropic or antiarrhythmic therapy after cardiopulmonary bypass.	2002 Aug	12154416

Showing 1 to 5 of 46 entries

Previous1 2 3 4 5…10Next

Patents

Sample Use Guides

In Vivo Use Guide

Congestive heart failure IV Initially, 0.75 mg/kg as a slow (over 2–3 minutes) direct injection; if warranted, may administer a supplemental direct IV dose of 0.75 mg/kg 30 minutes after the initial dose.1 60 Direct IV injection is followed by an IV infusion of 5–10 mcg/kg per minute. Duration of therapy determined by clinical response and tolerance to adverse effects.

Route of Administration: Intravenous

In Vitro Use Guide

Inamrinone inhibited human platelet aggregation at 10,800 s(-1) in a dose-dependent manner with the IC(50) value of 61 +/- 8 uM (mean +/- S.D.), Inamrinone significantly inhibited platelet aggregation at 1200 s(-1) only at highest concentration tested (100 uM)