108929-04-0 | Epinastine HCl

Packsize	Purity	Availability	Price	Discounted Price
10mg	98%	in stock	$43.00	$30.00
250mg	98%	in stock	$62.00	$44.00
1g	98%	in stock	$137.00	$96.00
5g	98%	in stock	$386.00	$270.00
10g	98%	in stock	$603.00	$422.00

Description

• Catalog Number: AB73378
• Chemical Name: Epinastine HCl
• CAS Number: 108929-04-0
• Molecular Formula: C16H16ClN3
• Molecular Weight: 285.7713
• MDL Number: MFCD00933434
• SMILES: NC1=NCC2N1c1ccccc1Cc1c2cccc1.Cl

Computed Properties

• Complexity: 378
• Covalently-Bonded Unit Count: 2
• Heavy Atom Count: 20
• Hydrogen Bond Acceptor Count: 1
• Hydrogen Bond Donor Count: 2
• Undefined Atom Stereocenter Count: 1

Upstream Synthesis Route

Epinastine Hydrochloride, a potent antihistamine, finds vital application in chemical synthesis due to its remarkable properties. As a selective histamine H1 receptor antagonist, Epinastine Hydrochloride is commonly utilized in the pharmaceutical industry for the development of medications aimed at alleviating allergic symptoms. Its presence in chemical synthesis enables the creation of novel drug compounds designed to combat various allergic conditions effectively. By incorporating Epinastine Hydrochloride into the synthesis process, chemists can produce advanced pharmaceutical products that target specific histamine receptors for enhanced therapeutic outcomes. This compound serves as a crucial building block in the synthesis of medications that cater to individuals suffering from allergies, providing a valuable tool for pharmaceutical researchers and developers. Through its strategic use in chemical synthesis, Epinastine Hydrochloride continues to drive innovation in the field of pharmaceuticals, offering new possibilities for the treatment of allergic disorders.

Literature

• Efficacy of epinastine hydrochloride for antigen-provoked nasal symptoms in subjects with orchard grass pollinosis.

  Allergology international : official journal of the Japanese Society of Allergology 20110301

• An H1-histamine receptor antagonist decreases serum interleukin-31 levels in patients with atopic dermatitis.

  The British journal of dermatology 20110201

• [Cautions in usage of generic epinastine].

  Arerugi = [Allergy] 20110101

• Prophylactic effects of the histamine H1 receptor antagonist epinastine and the dual thromboxane A2 receptor and chemoattractant receptor-homologous molecule expressed on Th2 cells antagonist ramatroban on allergic rhinitis model in mice.

  Biological & pharmaceutical bulletin 20110101

• Honey bee dopamine and octopamine receptors linked to intracellular calcium signaling have a close phylogenetic and pharmacological relationship.

  PloS one 20110101

• The effect of a selective octopamine antagonist, epinastine, on pharyngeal pumping in Caenorhabditis elegans.

  Invertebrate neuroscience : IN 20101101

• Antihistamine effects on prefrontal cortex activity during working memory process in preschool children: a near-infrared spectroscopy (NIRS) study.

  Neuroscience research 20100501

• Effect of epinastine hydrochloride on murine self-scratching behavior after skin-scratching stimulation.

  Archives of dermatological research 20100101

• Treatment of allergic conjunctivitis: results of a 1-month, single-masked randomized study.

  European journal of ophthalmology 20100101

• Effects of sedative and nonsedative antihistamines on prefrontal activity during verbal fluency task in young children: a near-infrared spectroscopy (NIRS) study.

  Psychopharmacology 20091101

• Multiple action agents and the eye: do they really stabilize mast cells?

  Current opinion in allergy and clinical immunology 20091001

• Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects.

  Expert opinion on drug metabolism & toxicology 20090901

• Efficacy of olopatadine HCI 0.1%, ketotifen fumarate 0.025%, epinastine HCI 0.05%, emedastine 0.05% and fluorometholone acetate 0.1% ophthalmic solutions for seasonal allergic conjunctivitis: a placebo-controlled environmental trial.

  Acta ophthalmologica 20090801

• Suppression of histamine- and allergen-induced skin reactions: comparison of first- and second-generation antihistamines.

  Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology 20090601

• Differential effects of octopamine and tyramine on the central pattern generator for Manduca flight.

  Journal of comparative physiology. A, Neuroethology, sensory, neural, and behavioral physiology 20090301

• Epinastine 0.05% ophthalmic solution in contact lens-wearing subjects with a history of allergic conjunctivitis.

  Eye & contact lens 20090101

• Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo.

  Mediators of inflammation 20090101

• Repeated pre-treatment with antihistamines suppresses [corrected] transcriptional up-regulations of histamine H(1) receptor and interleukin-4 genes in toluene-2,4-diisocyanate-sensitized rats.

  Journal of pharmacological sciences 20081201

• Development and characterisation of a novel and rapid lung eosinophil influx model in the rat.

  Pulmonary pharmacology & therapeutics 20080801

• Arousal facilitates collision avoidance mediated by a looming sensitive visual neuron in a flying locust.

  Journal of neurophysiology 20080801

• Ocular comfort and drying effects of three topical antihistamine/mast cell stabilizers in adults with allergic conjunctivitis: a randomized, double-masked crossover study.

  Clinical therapeutics 20080701

• Analysis of disease-dependent sedative profiles of H(1)-antihistamines by large-scale surveillance using the visual analog scale.

  Methods and findings in experimental and clinical pharmacology 20080401

• Suppressive activity of epinastine hydrochloride on eosinophil activation in vitro.

  In vivo (Athens, Greece) 20080101

• Inhibition of angiogenic factor production from murine mast cells by an antiallergic agent (epinastine hydrochloride) in vitro.

  Mediators of inflammation 20080101

• Modulation of eosinophil survival by epinastine hydrochloride, an H1 receptor antagonist, in vitro.

  In vivo (Athens, Greece) 20080101

• Octopamine partially restores walking in hypokinetic cockroaches stung by the parasitoid wasp Ampulex compressa.

  The Journal of experimental biology 20071201

• Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo.

  Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology 20071101

• Effects of sedative and non-sedative H1 antagonists on cognitive tasks: behavioral and near-infrared spectroscopy (NIRS) examinations.

  Psychopharmacology 20070901

• Duration of action of topical antiallergy drugs in a Guinea pig model of histamine-induced conjunctival vascular permeability.

  Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics 20070801

• Simultaneous multiresponse optimization applied to epinastine determination in human serum by using capillary electrophoresis.

  Analytica chimica acta 20070709

• Inhibition of IgE-mediated phosphorylation of FcepsilonRIgamma protein by antiallergic drugs in rat basophilic leukemia (RBL-2H3) cells: a novel action of antiallergic drugs.

  International immunopharmacology 20070701

• Efficacy and comfort of olopatadine 0.2% versus epinastine 0.05% ophthalmic solution for treating itching and redness induced by conjunctival allergen challenge.

  Current medical research and opinion 20070601

• An open-label, investigator-masked, crossover study of the ocular drying effects of two antihistamines, topical epinastine and systemic loratadine, in adult volunteers with seasonal allergic conjunctivitis.

  Clinical therapeutics 20070401

• Influences of histamine H1 receptor antagonists on maximal electroshock seizure in infant rats.

  Biological & pharmaceutical bulletin 20070301

• Inhibitory effects of epinastine on chemokine production and MHC class II/CD54 expression in keratinocytes.

  Journal of dermatological science 20070201

• Effect of topical olopatadine and epinastine in the botulinum toxin B-induced mouse model of dry eye.

  Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics 20070201

• Distribution to the skin of epinastine hydrochloride in atopic dermatitis patients.

  European journal of dermatology : EJD 20070101

• Development and validation of liquid chromatographic and ultraviolet derivative spectrophotometric methods for determination of epinastine hydrochloride in coated tablets.

  Journal of AOAC International 20070101

• Octopamine boosts snail locomotion: behavioural and cellular analysis.

  Invertebrate neuroscience : IN 20061201

• Effect of topical ophthalmic epinastine and olopatadine on tear volume in mice.

  Eye & contact lens 20061201

• Antiallergic drugs, azelastine hydrochloride and epinastine hydrochloride, inhibit ongoing IgE secretion of rat IgE-producing hybridoma FE-3 cells.

  European journal of pharmacology 20061010

• Roles of octopaminergic and dopaminergic neurons in mediating reward and punishment signals in insect visual learning.

  The European journal of neuroscience 20061001

• Efficacy and response with olopatadine versus epinastine in ocular allergic symptoms: a post hoc analysis of data from a conjunctival allergen challenge study.

  Clinical therapeutics 20061001

• Nasal congestion model in Brown Norway rats and the effects of some H1-antagonists.

  International immunopharmacology 20060501

• Role of substance P in allergic nasal symptoms in rats.

  European journal of pharmacology 20060217

• Effects of histamine H(1) receptor antagonists on depressive-like behavior in diabetic mice.

  Pharmacology, biochemistry, and behavior 20060201

• [Pharmacological and clinical profile of epinastine hydrochloride (Alesion Dry Syrup 1%)].

  Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20060101

• Epinastine hydrochloride antagonism against interleukin-4-mediated T cell cytokine imbalance in vitro.

  International archives of allergy and immunology 20060101

• Epinastine in the management of ocular allergic disease.

  International ophthalmology clinics 20060101

• Elestat (epinastine HCl ophthalmic solution 0.05%) as a therapeutic for allergic conjunctivitis.

  International ophthalmology clinics 20060101

• The various effects of four H1-antagonists on serum substance P levels in patients with atopic dermatitis.

  The Journal of dermatology 20051001

• Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro.

  The Journal of pharmacy and pharmacology 20050801

• Exacerbation of palmoplantar pustulosis by granulocyte colony-stimulating factor.

  International journal of dermatology 20050601

• Octopamine and experience-dependent modulation of aggression in crickets.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20050209

• Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children.

  British journal of clinical pharmacology 20050101

• Clinical efficacy of olopatadine vs epinastine ophthalmic solution in the conjunctival allergen challenge model.

  Current medical research and opinion 20040801

• Epinastine hydrochloride for atopic disease.

  Drugs of today (Barcelona, Spain : 1998) 20040801

• Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier.

  Drug metabolism and disposition: the biological fate of chemicals 20040501

• Epinastine ophthalmic solution (Elestat).

  The Medical letter on drugs and therapeutics 20040426

• Efficacy and tolerability of ophthalmic epinastine: a randomized, double-masked, parallel-group, active- and vehicle-controlled environmental trial in patients with seasonal allergic conjunctivitis.

  Clinical therapeutics 20040101

• Efficacy and tolerability of ophthalmic epinastine assessed using the conjunctival antigen challenge model in patients with a history of allergic conjunctivitis.

  Clinical therapeutics 20040101

• [Assessment of the clinical efficacy and safety of epinastine plus pseudoephedrine vs loratadine plus pseudoephedrine in perennial allergic rhinitis].

  Revista alergia Mexico (Tecamachalco, Puebla, Mexico : 1993) 20040101

• Antitussive effects of the H1-receptor antagonist epinastine in patients with atopic cough (eosinophilic bronchitis).

  Arzneimittel-Forschung 20040101

• Anti-glomerular basement membrane antibody-induced glomerulonephritis with periglomerular granulomatous reaction and massive renal eosinophilic infiltration.

  American journal of kidney diseases : the official journal of the National Kidney Foundation 20030901

• A new histamine measurement system employing a confocal laser microscope and cultured human dermal microvascular endothelial cells.

  Journal of dermatological science 20030901

• A case of type IV solar urticaria identified by reverse in vitro serum test.

  The Tokai journal of experimental and clinical medicine 20030701

• Hygienic behavior in the honey bee (Apis mellifera L.) and the modulatory role of octopamine.

  Journal of neurobiology 20030601

• [Efficacy of combined drug therapy using a macrolide antibiotic and an antihistamine for adult patients with chronic paranasal sinusitis].

  The Japanese journal of antibiotics 20030401

• Epinastine inhibits eosinophil chemotaxis and adhesion molecules in atopic dermatitis.

  Skin pharmacology and applied skin physiology 20030101

• Dermal objective pharmacodynamic profile of cetirizine and epinastine: two controlled, randomised, double-blind, crossover studies.

  International journal of clinical practice 20021001

• Pharmacokinetics of epinastine and a possible mechanism for double peaks in oral plasma concentration profiles.

  Biological & pharmaceutical bulletin 20010701

• Effect of H1-antagonists on spatial memory deficit evaluated by 8-arm radial maze in rats.

  Acta pharmacologica Sinica 20010701

• Effects of cetirizine and epinastine on the skin response to histamine iontophoresis.

  Journal of dermatological science 20010101

• A new model of allergic rhinitis in rats by topical sensitization and evaluation of H(1)-receptor antagonists.

  Immunopharmacology 20000601

• Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel.

  European journal of pharmacology 19990625

• A comparative pharmacokinetic-pharmacodynamic study of the electrocardiographic effects of epinastine and terfenadine in rats.

  The Journal of pharmacy and pharmacology 19970401

• Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers.

  International journal of clinical pharmacology, therapy, and toxicology 19901201

• New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine.

  Arzneimittel-Forschung 19900401