Loratadine - CAS 79794-75-5
Catalog number: B0084-302300
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C22H23ClN2O2
Molecular Weight:
382.88
COA:
Inquire
Targets:
Histamine Receptor
Description:
Loratadine is a histamine H1 receptor antagonist, used to treat allergies. It also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-302300 2.5 g $195 In stock
Bulk Inquiry
Brife Description:
histamine H1 receptor antagonist, allergies
Purity:
>98%
Synonyms:
Loratadine; Claritin; Loratidine; Clarityn; Alavert; Loratadine Wyeth Brand; Sch 29851; Sch-29851; Sch29851; Wyeth Brand of Loratadine;
Solubility:
Water: 0.000011 mg/ml
MSDS:
Inquire
Application:
the treatment of allergies
Melting Point:
134-136 °C
InChIKey:
JCCNYMKQOSZNPW-UHFFFAOYSA-N
InChI:
InChI=1S/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
Canonical SMILES:
CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
1.Effects of Prednisolone on the Pharmacokinetics of Loratadine after Oral and Intravenous Administration of Loratadine in Rats
Cheng Li, Minhee Kim, and Jun-Shik Choi. Arch Pharm Res Vol 33, No 9, 1395-1400, 2010
Loratadine undergoes extensive first-pass metabolism in the liver to form its major metabolite desloratadine, which also possesses antihistamine activity and is subject to further metabolism (Hilbert et al., 1987; Kreutner et al., 2000; Henz, 2001). CYP3A4 and CYP2D6 enzymes are responsible for the metabolism of loratadine to desloratadine (Yumibe et al., 1996). Loratadine is also a substrate of P-glycoprotein (P-gp) (Bradley et al., 1987). Since P-gp is co-localized with CYP3A4 in the small intestine, P-gp and CYP3A4 may act synergistically in absorption and first-pass metabolism of drugs, respectively (Pichard et al., 1990; Wacher et al., 1998; Ito et al., 1999).
2.Physicochemical characterization and dissolution enhancement of loratadine by solid dispersion technique
Suresh Bandari, Subash Jadav, Basanth Babu Eedara. Korean J. Chem. Eng., 30(1), 238-244 (2013)
In-vitro dissolution studies of pure loratadine, physical mixture, solid dispersions and tablets were done by using USP XXIV type II apparatus (Electrolab, Mumbai, India). Samples equivalent to 10 mg of loratadine were added to the 900 ml distilled water containing 0.1% w/v sodium lauryl sulfate at 37±0.5 ℃ and stirred at 50 rpm. An aliquot of 5 ml was withdrawn at predetermined time intervals and filtered through 0.45 μm filter using a syringe filter. The withdrawn volume was replenished immediately with the same volume of fresh dissolution medium in order to keep the total volume constant. The filtered samples were diluted suitably and assayed for loratadine content with a UV spectrophotometer at 280 nm. The mean of at least three determinations was used to calculate the drug release.
3.Plasma histamine levels (H) during adjunctive H1-receptor antagonist treatment with loratadine in patients with active Inflammatory Bowel disease (IBD)
M. Raithel • A. Nagel • Y. Zopf • Th. deRossi, Inflamm. Res. (2010) 59 (Suppl 2):S257–S258
The cumulative decrease of histamine values during the trial with or without loratadine was 0.30 and 0.13 ng histamine/ml 9 m2 BSA in Crohn’s disease (n.s.). Plasma histamine values in loratadine treated and untreated patients with ulcerative colitis decreased by 0.03 and 0.20 ng histamine/ml 9 m2 BSA (n.s.). Loratadine tended to decrease plasma histamine values more efficiently in Crohn’s disease than in ulcerative colitis. However, the dosage used was very low as originally described for allergic rhinoconjunctivitis. Considering the greater mucosal surface area in the gastrointestinal tract; future trials should consider higher doses to adequately block all intestinal H1-receptors and produce significant reductions in plasma histamine levels in IBD.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Histamine Receptor Products


CAS 1039399-17-1 PF-03654746 Tosylate

PF-03654746 Tosylate
(CAS: 1039399-17-1)

PF-03654746 Tosylate is a histamine H3 receptor antagonist undergoing a clinical trial for attention-deficit hyperactivity disorder (ADHD) therapy.

CAS 869497-75-6 JNJ 10191584 maleate

JNJ 10191584 maleate
(CAS: 869497-75-6)

The maleate salt form of JNJ 10191584, which has been found to be a selective histamine H4 receptor silent antagonist and could restrain mast cell and eosinophi...

CAS 73903-17-0 JNJ-10191584

JNJ-10191584
(CAS: 73903-17-0)

JNJ-10191584 is a selective histamine H4 receptor antagonist. It inhibits mast cell in vitro with IC50 value of 138nM. JNJ-10191584 has antiinflammatory and ana...

CAS 482-15-5 Isothipendyl

Isothipendyl
(CAS: 482-15-5)

Isothipendyl is a first-generation histamine H1 antagonist with anticholinergic activity. It has been used as an antipruritic.

CAS 5053-06-5 Fenspiride

Fenspiride
(CAS: 5053-06-5)

Fenspiride is an α adrenergic and H1 histamine receptor antagonist. It is an oxazolidinone spiro compound. It is used as a drug in the treatment of certain resp...

CAS 7456-24-8 Fonazine

Fonazine
(CAS: 7456-24-8)

Dimetotiazine is a histamine H1 receptor antagonist. It is a phenothiazine drug used for the treatment of migraine.

CAS 145196-87-8 Iodophenpropit dihydrobromide

Iodophenpropit dihydrobromide
(CAS: 145196-87-8)

Iodophenpropit dihydrobromide is a selective and high affinity histamine H3 antagonist (KD = 0.3 nM).

CAS 100643-71-8 Desloratadine

Desloratadine
(CAS: 100643-71-8)

Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

Chemical Structure

CAS 79794-75-5 Loratadine

Quick Inquiry

Verification code

Featured Items