Olopatadine Hydrochloride

• CAT Number: A000345
• CAS Number: 140462-76-6
• Molecular Formula: C21H23NO3 • HCl
• Molecular Weight: 373.9
• Purity: ≥95%
• Target: Histamine Receptor
• Solubility: Soluble in DMSO > 10 mM
• Storage: 3 years -20C powder
• Related CAS: 113806-05-6(free base)
• IC50: Ki = 16-41.1 nM
• InChIKey: HVRLZEKDTUEKQH-NOILCQHBSA-N
• SMILES: CN(C)CC/C=C1C2=C(C=CC=C2)COC3=CC=C(CC(O)=O)C=C3/1.Cl

Olopatadine Hydrochloride(cas 140462-76-6) is a potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively).


It blocks histamine-induced phosphoinositide turnover in isolated cells (IC50 = 9.5-39.9 nM) and prevents passive cutaneous anaphylaxis in rats (ED50 = 49 μg/kg) and anaphylactic bronchoconstriction in guinea pigs (ID50 = 30 μg/kg).1,2 Olopatadine is effective in treating allergic rhinitis and conjunctivitis.

Reference

1: Torkildsen G, Narvekar A, Bergmann M. Efficacy and safety of olopatadine
hydrochloride 0.77% in patients with allergic conjunctivitis using a conjunctival
allergen-challenge model. Clin Ophthalmol. 2015 Sep 14;9:1703-13. doi:
10.2147/OPTH.S83263. eCollection 2015. PubMed PMID: 26392751; PubMed Central
PMCID: PMC4574803.
2: Satake K, Ikeda J, Tamura T, Amano T, Kobayashi K. Olopatadine hydrochloride
suppresses hot flashes induced by topical treatment with tacrolimus ointment in
rats. Eur J Pharmacol. 2015 Oct 15;765:402-5. doi: 10.1016/j.ejphar.2015.09.008.
Epub 2015 Sep 8. PubMed PMID: 26362749.
3: Matsui S, Murota H, Ono E, Kikuta J, Ishii M, Katayama I. Olopatadine
hydrochloride restores histamine-induced impaired sweating. J Dermatol Sci. 2014
Jun;74(3):260-1. doi: 10.1016/j.jdermsci.2014.02.004. Epub 2014 Feb 28. PubMed
PMID: 24667096.
4: Shindo M, Yoshida Y, Yamamoto O. Olopatadine hydrochloride inhibits
capsaicin-induced flare response in humans. Pharmacology. 2011;87(3-4):152-4.
doi: 10.1159/000323868. Epub 2011 Feb 22. PubMed PMID: 21346393.