Detail of "113806-05-6"

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Azelastine is more potent than olopatadine in inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells

Azelastine is more potent than olopatadine in inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Kempuraj, Duraisamy; Huang, Man; Kandere, Kristiana; Boucher, William; Letourneau, Richard; Jeudy, Sheila; Fitzgerald, Kim; Spear, Kathleen; Athanasiou, Achilles; Theoharides, Theoharis C. ( Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, MA, USA).In this study， 113806-05-6 and 51-45-6 are also used. Annals of Allergy, Asthma, & Immunology, 88(5), 501-506 (English) 2002 American College of Allergy, Asthma, & Immunology. CODEN: ALAIF6. ISSN: 1081-1206. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 15 Background: Mast cells are involved in early- and late-phase reactions by releasing vasoactive mols., proteases, and cytokines. Certain histamine-1 receptor antagonists and other antiallergic drugs seem to inhibit the release of mediators from rat and human mast cells. Objective: Azelastine and olopatadine are antiallergic agents present in the ophthalmic solns. azelastine hydrochloride (Optivar, Asta Medica/Muro Pharmaceuticals, Tewksbury, MA), and olopatadine hydrochloride (Patanol, Alcon Labs., Fort Worth, TX), resp. The authors investigated the effect of these drugs on interleukin-6 (IL-6), tryptase, and histamine release from cultured human mast cells (CHMCs). Methods: CHMCs were grown from human umbilical cord blood-derived CD34+ cells in the presence of stem cell factor and IL-6 for 14 to 16 wk. Sensitized CHMCs were pretreated with various concns. of azelastine or olopatadine for 5 min. CHMCs were then challenged with anti-IgE, and the released mediators were quantitated. Results: The greatest inhibition of mediator release was seen with 24 mM azelastine; this level of inhibition was matched with the use of 133 mM olopatadine. At this concn., these drugs inhibited IL-6 release by 83% and 74%, tryptase release by 55% and 79%, and histamine release by 41% and 45%, resp. Activated CHMCs were characterized by numerous filopodia that were inhibited by both drugs as shown by electron microscopy. Conclusions: These results indicate that azelastine and olopatadine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine. .

A comparison of the efficacy and tolerability of olopatadine hydrochloride 0

A comparison of the efficacy and tolerability of olopatadine hydrochloride 0.1% ophthalmic solution and cromolyn sodium 2% ophthalmic solution in seasonal allergic conjunctivitis. Katelaris, Constance H.; Ciprandi, Giorgio; Missotten, Luc; Turner, F. Darell; Bertin, Donata; Berdeaux, Gilles; Czarny, Daniel; Hall, John H.; McCurrach, Fiona E.; Mitchell, Paul; Stawell, Richard J.; Thomson, George; Weiner, John; West, Robert H.; Goes, Frank M. R.; Marechal-Courtois, Christiane; Missotten, Luc; Pourjavan, Sayeh B.; Riviere, Agnes; Bremond, Dominique; Verin, Philippe; Collum, Amanda; Collum, Luis M. T.; Hurley, Colin; Kearney, Joanne; Khurana, Kavita P.; Ooi, Yeok-See; Cerqueti, Piera M.; Ciprandi, Giorgio; Leonardi, Andrea; Orsoni, Gabriella J.; Secchi, Antonio; de Smet, Marc; Meijer, Frans; Odenthal, T. P.; Reinders, Erik; Dominguez, Dolores S.; Iruzubieta, Jesus M.; Lapuente, Carlos R.; Lopez, Esther C.; Palmer, Ana M.; Parra, Juan C.; Peiro, Jose F.; Sans, Mariano, R.; Pigache, Robert (Department of Clinical Immunology and Allergy, Westmead Hospital, Sydney, Australia). Clinical Therapeutics, 24(10), 1561-1575 (English) 2002 Excerpta Medica, Inc. CODEN: CLTHDG. ISSN: 0149-2918. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 63 Treatments for allergic conjunctivitis have various mechanisms of action. Cromolyn sodium stabilizes conjunctival mast cells by preventing calcium influx across the cell membrane, whereas olopatadine hydrochloride is both an antihistamine and a mast cell stabilizer. This study compared the efficacy and tolerability of olopatadine and cromolyn in controlling the ocular signs and symptoms of seasonal allergic conjunctivitis. This was a multicenter, randomized, double-masked, parallel-group trial. One group instilled olopatadine 0.1% ophthalmic soln. and placebo BID, and the other instilled cromolyn 2% ophthalmic soln. QID, both for 6 wk.Several substances with their cas registry numbers 113806-05-6 and 140462-76-6 may be metioned in this study. The formulation of cromolyn used in this study is currently available only in Europe and Australia. The intent-to-treat efficacy and safety analyses included 185 patients, 91 in the olopatadine group and 94 in the cromolyn group. At 30 min after the first instillation, resp. decreases of ~30% and ~20% were reported in self-rated ocular itching and redness with both treatments; by 4 h, itching had decreased by ~38% in both groups. Differences between treatments were not statistically significant. At 4 h, redness had decreased by ~38% and ~26% in the resp. treatment groups. By day 42, both treatments had produced significant redns. from baseline in ocular signs and symptoms; however, the redns. in itching and redness were significantly greater with olopatadine compared with cromolyn (both variables, P < 0.05). The difference in physicians' impression of overall improvement on days 30 and 42 significantly favored olopatadine over cromolyn (both days, P < 0.05). Most patients (62.2%) had reacted pos. to grass pollen at baseline. The regression slopes correlating itching and redness with pollen count were 5 times lower for olopatadine compared with cromolyn (P = 0.002 and P = 0.016, resp.), indicating that olopatadine's efficacy increased as the pollen count increased. Six weeks' instillation of olopatadine 0.1 % ophthalmic soln. BID had a significantly greater effect on the ocular signs and symptoms of allergic conjunctivitis compared with 6 wk' instillation of cromolyn 2% ophthalmic soln. QID. Both treatments were well tolerated by patients in all age groups; however, olopatadine appeared to have better local tolerability in children aged <11 yr. .