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Details

Stereochemistry RACEMIC
Molecular Formula C8H19NO.ClH
Molecular Weight 181.703
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of HEPTAMINOL HYDROCHLORIDE

SMILES

Cl.CC(N)CCCC(C)(C)O

InChI

InChIKey=JZNBMCOSOXIZJB-UHFFFAOYSA-N
InChI=1S/C8H19NO.ClH/c1-7(9)5-4-6-8(2,3)10;/h7,10H,4-6,9H2,1-3H3;1H

HIDE SMILES / InChI

Molecular Formula C8H19NO
Molecular Weight 145.2426
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula ClH
Molecular Weight 36.461
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

Heptaminol is an amino alcohol that has been used as a myocardial stimulant and vasodilator and to relieve bronchospasm. Its most common therapeutic use is in orthostatic hypotension. The mechanism of heptaminol's therapeutic actions is not well understood although it has been suggested to affect catecholamine release or calcium metabolism.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
15.3 µM [IC50]
60.0 µM [Ki]
650.0 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Corasore

Cmax

ValueDoseCo-administeredAnalytePopulation
2.19 μg/mL
0.47 g single, oral
HEPTAMINOL plasma
Homo sapiens
1.6 mg/L
300 mg single, oral
HEPTAMINOL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
2.1 h
0.47 g single, oral
HEPTAMINOL plasma
Homo sapiens
2.7 h
300 mg single, oral
HEPTAMINOL plasma
Homo sapiens

Doses

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Infants & children under 12 years: 4-16 drops (25 -100 mg) depending on age, 2 – 4 times daily, up to 6 times daily if necessary, or as directed by the physician. Adults & children over 12 years: One tablet or 25 drops, (150 mg) 2-4 times daily, up to 6 times daily.
Route of Administration: Oral
In Vitro Use Guide
1. The effects of heptaminol on calcium current amplitude and characteristics were studied in single ventricular myocytes of guinea-pig by use of the whole cell configuration of the patch clamp technique. 2. A concentration-dependent decrease in ICa amplitude was observed. At heptaminol concentration as low as 10(-6) M, this effect was observed in only two cells (n = 6). At 10(-5) M the reduction of ICa was of 30 +/- 15% (n = 11). Both at -40 mV and -80 mV HP, heptaminol (10(-5) M) significantly increased the steady state inactivation of ICa.
Substance Class Chemical
Record UNII
XB3RM40HIR
Record Status Validated (UNII)
Record Version