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Details

Stereochemistry RACEMIC
Molecular Formula C16H19ClN2O
Molecular Weight 290.788
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CARBINOXAMINE

SMILES

CN(C)CCOC(C1=CC=C(Cl)C=C1)C2=CC=CC=N2

InChI

InChIKey=OJFSXZCBGQGRNV-UHFFFAOYSA-N
InChI=1S/C16H19ClN2O/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13/h3-10,16H,11-12H2,1-2H3

HIDE SMILES / InChI

Molecular Formula C16H19ClN2O
Molecular Weight 290.788
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Carbinoxamine is a histamine-H1 receptor blocking agent. It is an antihistamine with anticholinergic (drying) and sedative properties. Carbinoxamine appears to compete with histamine (type H1) for receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract. Carbinoxamine is effective for the symptomatic treatment of seasonal and perennial allergic rhinitis; vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; mild, uncomplicated allergic skin manifestations of urticaria and angioedema; dermatographism; as therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Most common adverse reactions are: sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, and thickening of bronchial secretions. Avoid concomitant use of alcohol and CNS depressants (hypnotics sedatives, tranquilizers, etc.) due to additive adverse effects.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.3 nM [Ki]
25.0 µM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE
Palliative
CARBINOXAMINE MALEATE

Cmax

ValueDoseCo-administeredAnalytePopulation
16.9 ng/mL
8 mg single, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens
4.5 ng/mL
4 mg single, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens
13.5 ng/mL
4 mg 2 times / day multiple, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
14.5 h
8 mg single, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens
30 h
4 mg single, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens
22 h
4 mg 2 times / day multiple, oral
CARBINOXAMINE MALEATE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
31%
unknown, unknown
CARBINOXAMINE MALEATE plasma
Homo sapiens

PubMed

Sample Use Guides

In Vivo Use Guide
Tablets: 1 or 2 tablets (4 to 8 mg) 3 to 4 times daily Oral Solution: 1 or 2 teaspoonfuls (4 to 8 mg) 3 to 4 times daily.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
982A7M02H5
Record Status Validated (UNII)
Record Version