Epinastine - CAS 80012-43-7
Catalog number: 80012-43-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C16H15N3
Molecular Weight:
249.31
COA:
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Targets:
Histamine Receptor
Description:
Epinastine is a second-generation antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. It is highly selective for the H1 receptor and does not cross the blood-brain-barrier. It shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. It inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. It is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. It antagonises octopamine-induced cAMP formation in the insect brain. It is effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance. It is produced by Allergan and marketed by Inspire in the United States.
Purity:
>98%
Appearance:
White to yellow crystalline powder
Synonyms:
9,13b-Dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3- amine;3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine;Apinastine Base;WAL 801
Solubility:
DMSO 57 mg/mL; Water 57 mg/mL
Storage:
-20°C Freezer
MSDS:
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Application:
Epinastine is used in eye drops to treat allergic conjunctivitis. It is highly selective for the H1 receptor and does not cross the blood-brain-barrier.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
428.0±55.0 °C | Condition: Press: 760 Torr
Melting Point:
205-208 °C
Density:
1.32±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
WHWZLSFABNNENI-UHFFFAOYSA-N
InChI:
InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
Canonical SMILES:
C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N
Current Developer:
Epinastine is produced by Allergan and marketed by Inspire in the United States.
1.Efficacy of epinastine hydrochloride ophthalmic solution in allergic conjunctivitis by conjunctival cedar pollen allergen challenge.
Fujishima H1, Ohashi Y2, Takamura E3. Ann Allergy Asthma Immunol. 2014 Oct;113(4):476-81. doi: 10.1016/j.anai.2014.07.007. Epub 2014 Aug 20.
BACKGROUND: Epinastine hydrochloride is a selective histamine H1 receptor antagonist that also inhibits IgE receptor-mediated histamine release from mast cells.
2.Efficacy of olopatadine versus epinastine for treating allergic conjunctivitis caused by Japanese cedar pollen: a double-blind randomized controlled trial.
Fukushima A1, Ebihara N. Adv Ther. 2014 Oct;31(10):1045-58. doi: 10.1007/s12325-014-0156-2. Epub 2014 Oct 1.
INTRODUCTION: The objective of this study was to compare the efficacy and safety of olopatadine versus epinastine in healthy Japanese adults with a history of allergic conjunctivitis to Japanese cedar pollen.
3.Study of fluorescence interaction and conformational changes of bovine serum albumin with histamine H₁ -receptor--drug epinastine hydrochloride by spectroscopic and time-resolved fluorescence methods.
Ariga GG1, Naik PN1, Nandibewoor ST1, Chimatadar SA1. Biopolymers. 2015 Nov;103(11):646-57. doi: 10.1002/bip.22707.
The fluorescence, ultraviolet (UV) absorption, time resolved techniques, circular dichroism (CD), and infrared spectral methods were explored as tools to investigate the interaction between histamine H1 drug, epinastine hydrochloride (EPN), and bovine serum albumin (BSA) under simulated physiological conditions. The experimental results showed that the quenching of the BSA by EPN was static quenching mechanism and also confirmed by lifetime measurements. The value of n close to unity indicated that one molecule of EPN was bound to protein molecule. The binding constants (K) at three different temperatures were calculated (7.1 × 10(4), 5.5 × 10(4), and 3.9 × 10(4) M(-1)). Based on the thermodynamic parameters (ΔH(0), ΔG(0), and ΔS(0)), the nature of binding forces operating between drug and protein was proposed. The site of binding of EPN in the protein was proposed to be Sudlow's site I based on displacement experiments using site markers viz, warfarin, ibuprofen, and digitoxin.
4.The enantioselective synthesis of (S)-(+)-mianserin and (S)-(+)-epinastine.
Roszkowski P1, Maurin JK2, Czarnocki Z1. Beilstein J Org Chem. 2015 Aug 28;11:1509-13. doi: 10.3762/bjoc.11.164. eCollection 2015.
A simple enantioselective synthetic procedure for the preparation of mianserin and epinastine in optically pure form is described. The key step in the synthetic pathway is the asymmetric reduction of the cyclic imine using asymmetric transfer hydrogenation conditions.
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CAS 80012-43-7 Epinastine

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