Category: 2508-72-7

Yanni, John M. published the artcileInhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Archives of Ophthalmology (Chicago) (1999), 117(5), 643-647, database is CAplus and MEDLINE.

To evaluate the effects of topical ocular drugs with histamine H₁-antagonist activity on histamine-stimulated phosphatidylinositol turnover and interleukin (IL) 6 and IL-8 secretion from human conjunctival epithelial cells. Primary human conjunctival epithelial cell cultures were stimulated with histamine in the presence or absence of test drugs. Phosphatidylinositol turnover was quantified by ion exchange chromatog. and cytokine content of supernatants by ELISA. Antazoline hydrochloride, emedastine difumarate, levocabastine hydrochloride, olopatadine hydrochloride, and pheniramine maleate attenuated histamine-stimulated phosphatidylinositol turnover and IL-6 and IL-8 secretion. Emedastine was the most potent in ligand binding, phosphatidylinositol turnover, and IL-6 secretion, with dissociation constant and 50% inhibitory concentrations of 1-3 nmol/L. Olopatadine, antazoline, and pheniramine exhibited similar H₁-binding affinities (32-39 nmol/L). However, olopatadine was approx. 10-fold more potent as an inhibitor of cytokine secretion (50% inhibitory concentration, 1.7-5.5 nmol/L) than predicted from binding data, while antazoline and pheniramine were far less potent (20- to 140-fold) in functional assays. Levocabastine (dissociation constant, 52.6 nmol/L) exhibited greater functional activity (50% inhibitory concentration, 8-25 nmol/L) than either antazoline or pheniramine. Histamine-stimulated phosphatidylinositol turnover and cytokine secretion by human conjunctival epithelial cells are attenuated by compounds with H₁-antagonist activity. However, antihistaminic potency alone does not predict anti-inflammatory potential. Olopatadine, emedastine, and levocabastine were notably more potent than pheniramine and antazoline. Selected topical ocular drugs with antihistaminic activity may offer therapeutic advantages to patients with allergic conjunctivitis by inhibiting proinflammatory cytokine secretion from human conjunctival epithelial cells.

Archives of Ophthalmology (Chicago) published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C20H28B2O4S2, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Maling, Harriet M. published the artcileInflammation induced by histamine, serotonin, bradykinin, and compound 48/80 in the rat. Antagonists and mechanisms of action, SDS of cas: 2508-72-7, the publication is Journal of Pharmacology and Experimental Therapeutics (1974), 191(2), 300-10, database is CAplus and MEDLINE.

A number of antagonists were tested for their ability to inhibit the inflammation induced by subplantar injection into the rat hindpaw of histamine-2HCl [56-92-8], serotonin creatinine sulfate [971-74-4], bradykinin [58-82-2],or compound 48-80. Triprolidine [486-12-4] and chlorpheniramine maleate [113-92-8] specifically inhibited histamine-induced edema. D-2-bromolysergic acid diethylamide [478-84-2] and methysergide [361-37-5] specifically inhibited serotonin-induced edema. Tripelennamine-HCl [22306-05-4], pyrilamine maleate [59-33-6], promethazine-HCl [58-33-3], antazoline-HCl [2508-72-7] diphenylhydramine-HCl [147-24-0], phenindamine tartrate [569-59-5], chlorcyclizine-HCl [14362-31-3] and l-isoproterenol-HCl [5984-95-2] inhibited the edemas induced by either serotonin or histamine. Promethazine, antazoline, diphenhydramine and l-isoproterenol also partially blocked the edema induced by bradykinin. Cyproheptadine-HCl [969-33-5] inhibited the edemas induced by both serotonin and bradykinin. By means of specific antagonists, the edema induced by compound 48/80 was shown to be due to the release of serotonin (65%) and histamine (30%). Kinins are probably not involved. In doses as low as 0.005 μmol/kg s.c., l-isoproterenol inhibited compound 48/80-induced edema. Some antihistamines, especially tripelennamine, inhibited compound 48/80 edema more effectively than could be explained by their inhibition of either histamine or serotonin. Their effectiveness was correlated with their abilities to inhibit the release of mediators from isolated rat peritoneal mast cells.

Journal of Pharmacology and Experimental Therapeutics published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, SDS of cas: 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Pini, J. J. P. B. published the artcileDegranulation of rat mesentery mast cells by antihistamines: influence of ionization, Application In Synthesis of 2508-72-7, the publication is Agents and Actions (1978), 8(5), 491-6, database is CAplus and MEDLINE.

Classical antihistamines were potent rat mast cell degranulators active in the range of 0.1 to 2.0 mM at pH 8.4. No relation between their potency as mast cell degranulators and their chem. structure or their activity as inhibitors of peripheral H₁ histamine receptors could be established. Halogenation of diphenhydramine-HCl [147-24-0] and cyclizine-HCl [303-25-3], but not of promethazine [60-87-7], increased their activity. The alkylamino side chain of phenothiazine does not seem to be essential for degranulation since toluidine blue [92-31-9] and methylene blue [61-73-4], which lack it, were also active. Thionin [581-64-6], whose amino groups in the phenothiazine ring are not methylated, was inactive. The action of antihistamines on mast cells increased with an increase of pH, suggesting that activity can mainly be attributed to the uncharged base. However, the ionized mol. must be active at lower pH too. Above certain concentrations, antihistamines became inactive both at pH 7.0 and 8.4. At these higher concentrations, promethazine inhibited degranulation induced by chlorcyclizine or compound 48/80, an action not reversed by glucose. Thus, mast cell degranulation by antihistamines does not seem to be caused by the ionized base acting inside the cell following penetration of the cell membrane by the lipid soluble uncharged mol.

Agents and Actions published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Application In Synthesis of 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Melis-Decerf, C. published the artcileAn in vitro method simulating drug release from viscous eye drops in rabbit and man, Category: imidazoles-derivatives, the publication is Journal of Pharmacy and Pharmacology (1979), 31(1), 12-15, database is CAplus and MEDLINE.

The release of drugs from viscous solutions under conditions simulating the blinking movements in the rabbit and human eye was determined using a rotatable diffusion cell. For the solutions at rest, corresponding with the conditions at the surface of the rabbit cornea, the diffusion velocity decreased with increasing viscosity. When the solution was moved at a velocity corresponding to that of lacrimal fluid at the surface of the human eye, the influence of viscosity may be neglected.

Journal of Pharmacy and Pharmacology published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Van Gyseghem, E. published the artcileDetermining orthogonal chromatographic systems prior to the development of methods to characterise impurities in drug substances, Product Details of C17H20ClN3, the publication is Journal of Chromatography, A (2003), 988(1), 77-93, database is CAplus and MEDLINE.

To define starting conditions for the development of methods to sep. impurities from the active substance and from each other in drugs with an unknown impurity profile, the parallel application of generic orthogonal chromatog. systems could be useful. The possibilities to define orthogonal chromatog. systems were examined by calculation of the correlation coefficients between retention factors k for a set of 68 drugs on 11 systems, by visual evaluation of the selectivity differences, by principal component anal., by drawing color maps, and evaluating dendrograms. A zirconia-based stationary phase coated with a polybutadiene (PBD) polymer and 3 silica-based phases (base-deactivated, polar-embedded and monolithic) were used. Besides the stationary phase, the influence of pH and of organic modifier, on the selectivity of a system were evaluated. The dendrograms of hierarchical clusters were found good aids to assess orthogonality of chromatog. systems. The PBD-zirconia phase/methanol/pH 2.5 system is found most orthogonal towards several silica-based systems, e.g. a base-deactivated C₁₆-amide silica/methanol/pH 2.5 system. The orthogonality was validated using cross-validation, and 2 other validation sets, i.e. a set of non-ionizable solutes and a mixture of a drug and its impurities.

Journal of Chromatography, A published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C7H16Cl2Si, Product Details of C17H20ClN3.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Pohjala, Leena published the artcileInhibitors of alphavirus entry and replication identified with a stable Chikungunya replicon cell line and virus-based assays, Synthetic Route of 2508-72-7, the publication is PLoS One (2011), 6(12), e28923, database is CAplus and MEDLINE.

Chikungunya virus (CHIKV), an alphavirus, has recently caused epidemic outbreaks and is therefore considered a re-emerging pathogen for which no effective treatment is available. In this study, a CHIKV replicon containing the virus replicase proteins together with puromycin acetyltransferase, EGFP and Renilla luciferase marker genes was constructed. The replicon was transfected into BHK cells to yield a stable cell line. A non-cytopathic phenotype was achieved by a Pro718 to Gly substitution and a five amino acid insertion within non-structural protein 2 (nsP2), obtained through selection for stable growth. Characterization of the replicon cell line by Northern blotting anal. revealed reduced levels of viral RNA synthesis. The CHIKV replicon cell line was validated for antiviral screening in 96-well format and used for a focused screen of 356 compounds (natural compounds and clin. approved drugs). The 5,7-dihydroxyflavones apigenin, chrysin, naringenin and silybin were found to suppress activities of EGFP and Rluc marker genes expressed by the CHIKV replicon. In a concomitant screen against Semliki Forest virus (SFV), their anti-alphaviral activity was confirmed and several addnl. inhibitors of SFV with IC₅₀ values between 0.4 and 24 μM were identified. Chlorpromazine and five other compounds with a 10H-phenothiazinyl structure were shown to inhibit SFV entry using a novel entry assay based on a temperature-sensitive SFV mutant. These compounds also reduced SFV and Sindbis virus-induced cytopathic effect and inhibited SFV virion production in virus yield experiments Finally, antiviral effects of selected compounds were confirmed using infectious CHIKV. In summary, the presented approach for discovering alphaviral inhibitors enabled us to identify potential lead structures for the development of alphavirus entry and replication phase inhibitors as well as demonstrated the usefulness of CHIKV replicon and SFV as biosafe surrogate models for anti-CHIKV screening.

PLoS One published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Synthetic Route of 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Amer, M. M. published the artcileColorimetric determination of antazoline in pharmaceutical preparations with sodium nitrite, COA of Formula: C17H20ClN3, the publication is Analyst (Cambridge, United Kingdom) (1974), 99(1181), 487-90, database is CAplus and MEDLINE.

Pharmaceutical preparations containing antazoline-HCl [2508-72-7] were analyzed by solution in aqueous HCl and addition of NaNO2 solution at <10°, giving a yellow color which was stabilized by the addition of iso-PrOH, and solution absorbance determined at 410 nm. Beer’s law was obeyed between 20-120 μg of antazoline-HCl and 20-140 μg of the methanesulfonate [3131-32-6].

Analyst (Cambridge, United Kingdom) published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, COA of Formula: C17H20ClN3.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Amer, M. M. published the artcileColorimetric determination of antazoline, Formula: C17H20ClN3, the publication is Australian Journal of Pharmaceutical Sciences (1974), 3(2), 58-60, database is CAplus.

The color reaction between antazoline-HCl (I) [2508-72-7] and Ce(SO4)2 yielded maximum absorption at 500 nm, and was used in the anal. of I in pharmaceutical preparations Fifty mg I in a final concentration of 50% H2SO4 and 2 mg ceric ammonium sulfate reached maximum intensity in 10 min and remained stable for an addnl. 30 min when kept cool. The color followed Beer’s Law at concentrations of 2-10 μgm/ml, and was due to the oxidation of I.

Australian Journal of Pharmaceutical Sciences published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Formula: C17H20ClN3.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Amer, M. M. published the artcileModified nitroprusside colorimetric determination of antazoline salts in some pharmaceutical preparation, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Pharmazie (1974), 29(5), 354-5, database is CAplus and MEDLINE.

The nitroprusside method of Slack and Mader (1957) was improved by using 80 mg H3BO3 in place of NaHCO3 (to alter pH) and adding 4 ml EtOH to give a red color instead of the violet, measurable at 540 nm, the color being maximum at 1 min and stable for 12 hr. The method is superior to that of BP 1968 and USP XV, since ephedrine and 19 other substances tested did not interfere with the reaction but naphazoline, Zn2+, and phentolamine did,. Recovery by this method ranged between 100.6.+-.0.23% to 102.3.+-.1.2%. Determinations were made against a standard curve for 0.1-1. mg of the corresponding antazoline salt.

Pharmazie published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Khristova, M. published the artcileDetermination of naphazoline hydrochloride in the presence of antazoline hydrochloride, Application of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Farmatsiya (Sofia, Bulgaria) (1980), 30(6), 18-20, database is CAplus.

Naphazoline-HCl (I-HCl) [550-99-2] was determined in the presence of antazoline-HCl [2508-72-7] by mixing with H₂CO-H₂SO₄, extracting the colored product with CHCl₃ to remove the interference of SO₄^2-, and measuring the absorbance at 665 nm. Absorbance was linear with concentration for 20-100 μg/mL, and the error was 4.8%.

Farmatsiya (Sofia, Bulgaria) published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Application of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem