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Loratadine

Loratadine

CAS: 79794-75-5

Molecular Formula: C22H23ClN2O2

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Loratadine - Names and Identifiers

Name Loratadine
Synonyms CLARITIN
CLARATYNE
Loratidine
Loratadine
LORATIDINE
LORATADINE
LORATADINE-D5
ethyl 4-(8-chloro-5,6-dihydro-11h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate
Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate
4-(8-Chloro-10,11-dihydro-4-aza-5H-dibenzo[a,d]cycloheptene-5-ylidene)piperidine-1-carboxylic acid ethyl ester
4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acid ethyl ester
4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridine-11-ylidene)piperidine-1-carboxylic acid ethyl ester
CAS 79794-75-5
EINECS 1308068-626-2
InChI InChI=1/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
InChIKey JCCNYMKQOSZNPW-UHFFFAOYSA-N

Loratadine - Physico-chemical Properties

Molecular FormulaC22H23ClN2O2
Molar Mass382.88
Density1.261±0.06 g/cm3(Predicted)
Melting Point134-136°C
Boling Point531.3±50.0 °C(Predicted)
Water SolubilityIt is soluble in DMSO (50 mg/ml), ethanol (77 mg/ml at 25°C), water (<1 mg/ml at 25°C), chloroform, and methanol.
Solubility DMSO: 26mg/mL, soluble
Appearancepowder
Colorwhite
Merck14,5578
pKa4.27±0.20(Predicted)
Storage Condition2-8°C
StabilityStable, but may be heat sensitive - refrigerate. Incompatible with strong oxidizing agents.
MDLMFCD00672869
Physical and Chemical PropertiesCrystallization from acetonitrile, melting point 134-136 °c.
UseNew national Class II anti-allergic drug for the relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and the relief of chronic urticaria
In vitro studyLoratadine was identified as a selective inhibitor of B(0)AT 2, with an IC 50 of 4 μm, with low or no activity against several other members of the SLC6 family. In Der p 1 and or anti-Fc small RI pre-cultured human Fc small RI cells, Loratadine concentration-dependent inhibition of histamine and leukotriene C4 release. Loratadine(0.1 mM) also inhibited the release of histamine, leukotriene C4, and PGD2 in purified HLMC activated by a small amount of RI against FCR. Loratadine concentration-dependently inhibited the release of histamine, tryptase, LTC4, and PGD 2 in purified HSMC stimulated against a small amount of RI. In Human Umbilical vein endothelial cells, Loratadine significantly inhibited histamine-induced IL-6 and IL-8 secretion. In human Ltk-cells transfected with the hKv1.5 channel gene, Loratadineh blocked the Kv1.5 channel in a concentration-, voltage-, time-and use-dependent manner at concentrations above therapeutic plasma levels. Loratadineh inhibited rhinovirus-induced upregulation of ICAM-1 in the main bronchus or transformed (A549) respiratory epithelial cells. Loratadineh also inhibited rhinovirus infection-induced ICAM-1 mRNA in a dose-dependent manner, and they completely inhibited rhinovirus-induced activation of the ICAM-1 promoter.

Loratadine - Risk and Safety

Hazard SymbolsXi - Irritant
Irritant
Risk Codes36/37/38 - Irritating to eyes, respiratory system and skin.
Safety DescriptionS22 - Do not breathe dust.
S24/25 - Avoid contact with skin and eyes.
S36 - Wear suitable protective clothing.
S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
UN IDs3077
WGK Germany2
RTECSTM6129200
HS Code29333990

Loratadine - Nature

Open Data Verified Data

White or almost white crystalline powder, odorless and tasteless. The melting point was 134-136 °c. Soluble in methanol or chloroform.

Last Update:2025-06-10 22:55:16

Loratadine - Preparation Method

Open Data Verified Data

4-(8 monochloro -5, 6-amino-11h-benzo [5.6] cycloheptano [1,2-b] pyridine-11-subunit)-1-methylpiperidine is dissolved in toluene, ethyl chloroformate is added dropwise, the reaction is finished, water is added, benzene layer is separated, washed with water, dried and concentrated under reduced pressure to obtain oily substance, after being impregnated with ether, after recrystallization, desloratadine was obtained.

Last Update:2025-06-10 22:55:16

Loratadine - Application

Open Data Verified Data

developed by the company in S-Plogh. Antihistamine drugs, peripheral nerve Hi receptor has a high degree of selectivity, strong effect, long time. It is a long-acting tricyclic antihistamine, which competitively inhibits histamine Hi receptor and inhibits allergic symptoms caused by histamine. There was no obvious anticholinergic and central inhibitory effect. For the relief of symptoms associated with allergic rhinitis, as well as the relief of symptoms of chronic urticaria and other allergic skin diseases.

Last Update:2025-08-19 16:24:40
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