Tag: M.W=300-350

Abd-Elbary, A. published the artcileInteraction of carbopol 934 with certain antihistaminic drugs, HPLC of Formula: 2508-72-7, the publication is Pharmazie (1981), 36(5), 356-8, database is CAplus.

Increases in Carbopol 934 [9007-16-3] concentration and pH of the buffer solutions resulted in an increased interaction of antazoline-HCl (I-HCl) [2508-72-7] and cyproheptadine-HCl (II-HCl) [969-33-5] with Carbopol 934 while increases in I-HCl or II-HCl concentrations or the presence of NaCl resulted in a decreased interaction. IR spectrum anal. showed that I-HCl reaction was chem., while II-HCl reaction with Carbopol 934 was probably phys. in nature.

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, HPLC of Formula: 2508-72-7.

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

Kaliszan, Roman published the artcileSuppression of deleterious effects of free silanols in liquid chromatography by imidazolium tetrafluoroborate ionic liquids, Formula: C17H20ClN3, the publication is Journal of Chromatography A (2004), 1030(1-2), 263-271, database is CAplus and MEDLINE.

Silica-based stationary phases are commonly used in liquid chromatog., but their surface acidity causes known problems, especially when separating basic compounds Deleterious effects of free silanols are not fully removed by standard prevention procedures consisting in adding alkylamines or other amino quenchers to the eluents. Ionic liquids of the imidazolium tetrafluoroborate class, added to mobile phases at concentrations of 0.5-1.5% (volume/volume), blocked silanols and provided excellent thin-layer chromatog. separations of strongly basic drugs which were otherwise not eluted, even with neat acetonitrile as the mobile phase. The silanol suppressing potency of imidazolium tetrafluoroborates was demonstrated to markedly exceed that of the standard mobile phase additives, like triethylamine, dimethyloctylamine and ammonia. The proposed new mobile phase additives also provide reliable lipophilicity parameters of base drug analytes as determined by gradient mode of HPLC. By applying the readily available and environmentally friendly imidazolium tetrafluoroborate ionic liquids, simple and efficient means of improvement of liquid chromatog. anal. of organic bases were elaborated.

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 C17H20ClN3, Formula: C17H20ClN3.

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

Liu, Zhen-zhen published the artcileIdentification of pimavanserin tartrate as a potent Ca²⁺-calcineurin-NFAT pathway inhibitor for glioblastoma therapy, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Acta Pharmacologica Sinica (2021), 42(11), 1860-1874, database is CAplus and MEDLINE.

Glioblastoma multiforme (GBM) is the most common and malignant type of primary brain tumor, and 95% of patients die within 2 years after diagnosis. In this study, aiming to overcome chemoresistance to the first-line drug temozolomide (TMZ), we carried out research to discover a novel alternative drug targeting the oncogenic NFAT signaling pathway for GBM therapy. To accelerate the drug′s clin. application, we took advantage of a drug repurposing strategy to identify novel NFAT signaling pathway inhibitors. After screening a set of 93 FDA-approved drugs with simple structures, we identified pimavanserin tartrate (PIM), an effective 5-HT_2A receptor inverse agonist used for the treatment of Parkinson′s disease-associated psychiatric symptoms, as having the most potent inhibitory activity against the NFAT signaling pathway. Further study revealed that PIM suppressed STIM1 puncta formation to inhibit store-operated calcium entry (SOCE) and subsequent NFAT activity. In cellula, PIM significantly suppressed the proliferation, migration, division, and motility of U87 glioblastoma cells, induced G1/S phase arrest and promoted apoptosis. In vivo, the growth of s.c. and orthotopic glioblastoma xenografts was markedly suppressed by PIM. Unbiased omics studies revealed the novel mol. mechanism of PIM′s antitumor activity, which included suppression of the ATR/CDK2/E2F axis, MYC, and AuroraA/B signaling. Interestingly, the genes upregulated by PIM were largely associated with cholesterol homeostasis, which may contribute to PIM′s side effects and should be given more attention. Our study identified store-operated calcium channels as novel targets of PIM and was the first to systematically highlight the therapeutic potential of pimavanserin tartrate for glioblastoma.

Acta Pharmacologica Sinica 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, 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

Beraki, Simret published the artcileA pharmacological screening approach for discovery of neuroprotective compounds in ischemic stroke, Related Products of imidazoles-derivatives, the publication is PLoS One (2013), 8(7), e69233, database is CAplus and MEDLINE.

With the availability and ease of small mol. production and design continuing to improve, robust, high-throughput methods for screening are increasingly necessary to find pharmacol. relevant compounds amongst the masses of potential candidates. Here, we demonstrate that a primary oxygen glucose deprivation assay in primary cortical neurons followed by secondary assays (i.e. post-treatment protocol in organotypic hippocampal slice cultures and cortical neurons) can be used as a robust screen to identify neuroprotective compounds with potential therapeutic efficacy. In our screen about 50% of the compounds in a library of pharmacol. active compounds displayed some degree of neuroprotective activity if tested in a pre-treatment toxicity assay but just a few of these compounds, including Carbenoxolone, remained active when tested in a post-treatment protocol. When further examined, Carbenoxolone also led to a significant reduction in infarction size and neuronal damage in the ischemic penumbra when administered six hours post middle cerebral artery occlusion in rats. Pharmacol. testing of Carbenoxolone-related compounds, acting by inhibition of 11-β-hydroxysteroid dehydrogenase-1 (11β-HSD1), gave rise to similarly potent in vivo neuroprotection. This indicates that the increase of intracellular glucocorticoid levels mediated by 11β-HSD1 may be involved in the mechanism that exacerbates ischemic neuronal cell death and inhibiting this enzyme could have potential therapeutic value for neuroprotective therapies in ischemic stroke and other neurodegenerative disorders associated with neuronal injury.

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, Related Products of imidazoles-derivatives.

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

Garcia Rodriguez, Miguel published the artcileAction of iproniazid and some antihistamines on the adrenergic neuron blockade produced by bretylium, HPLC of Formula: 2508-72-7, the publication is Revista Cubana de Farmacia (1974), 8(2), 183-5, database is CAplus.

Systral (chlorphenoxamine-HCl)(I) [562-09-4], gravinol (dimenhydrinate) [523-87-5], suprastin (chloropyramine) [59-32-5], and antistina (antazoline-HCl) [2508-72-7] (each at 15 μg/ml for 15 min) blocked the bretylium [59-41-6]-induced sympatholytic activity in isolated rat vas deferens, whereas iproniazid-HCl [6011-62-7] had no effect. Patients under prolonged treatment with antihistamines who show signs and symptoms of hypertension probably should not be subjected to simultaneous treatment with adrenergic blocking agents.

Revista Cubana de Farmacia 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, HPLC of Formula: 2508-72-7.

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

Guedes, Maria Fernanda published the artcileEffectiveness of preservatives in multidose ocular and nasal formulations. II. Contamination of nasal products, COA of Formula: C17H20ClN3, the publication is Revista Portuguesa de Farmacia (1986), 36(1), 29-33, database is CAplus.

In sulfacetamide  [144-80-9] nasal solutions, chlorobutanol  [57-15-8] was ineffective with the solution turning brown-yellow possibly due to absorption of chlorobutanol by the plastic dropper and oxidation Chlorocresol  [1321-10-4] was more effective in the formulations. The permeability of polyethylene  [9002-88-4] to water, steam, and gases was also studied.

Revista Portuguesa de Farmacia 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

Ismaiel, Saad A. published the artcileVolumetric determination of antazoline, diphenhydramine, and ephedrine in some pharmaceutical preparations, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Pharmazie (1975), 30(1), 58, database is CAplus and MEDLINE.

Antazoline-HCl (I) [2508-72-7] or diphenhydramine-HCl (II) [147-24-0] can be determined in the presence of ephedrine-HCl (III) [50-98-6] by a modification of the nonaqueous titrimetric method of BP 1973, i.e., by the prior addition of pure NaHCO3 and cooling to <15° (to prevent decomposition of NaHCO3 → Na2CO3), extraction of the liberated I and(or) II with CHCl3, the addition of NaOH to the separated aqueous layer and extraction of the liberated III with CHCl3. The CHCl3 solutions were evaporated and the residues titrated with HClO4 (crystal violet, indicator). The method compares favorably with that of Ismaiel (ibid. 1974).

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

Omar, Nabil M. published the artcileImproved spectrophotometric determination of antazoline, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Journal of Pharmaceutical Sciences (1978), 67(11), 1610-13, database is CAplus and MEDLINE.

A simple, precise, and accurate spectrophotometric determination of antazoline (I) salts was developed by improving the ceric sulfate procedure. Replacement of water with HOAc for the preparation of all assay solutions permitted reproducible measurements of the chromogen that absorbed at 505 nm. An appreciable increase in color stability was attained by the controlled addition of HClO₄ to the ceric reagent prior to interaction with I at room temperature Evidence is provided to account for the oxidation of I at the expense of a complex ceric species. Other 2-imidazolines or phenylephrine did not interfere with the investigated color reaction. In addition to the high value of the chromogen molar absorptivity, ideal adherence of color absorption to Beer’s law permitted accurate and reproducible estimation of I over the 1-10-μg range. The procedure was applied to the anal. of different I dosage forms.

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, 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

Stawowczyk, Adolf published the artcileTriethanolamine stearate compatibility with some drugs in emulsion ointments, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Farmacja Polska (1975), 31(2), 105-9, database is CAplus.

Benzalkanium bromide and Vioform [130-26-7] were the only 2 of the 12 drugs tested which were stable for the whole duration of the exptl. period in the presence of triethanolamine stearate [4568-28-9] in solutions and emulsion ointments. Sulfathiazole [72-14-0] was stable for 30 days in solutions, but became discolored within 20 days in ointment. Ointments of ethacridine lactate [1837-57-6] were stable for at least 6 months, and those of diphenhydramine-HCl [147-24-0], chloropyribenzamine-HCl [6170-42-9], and tripellennamine-HCl [154-69-8] for 30 days.

Farmacja Polska 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 C3H3Br2ClO, 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

Tewari, S. N. published the artcileDetection and determination of psychotropic drugs by thin layer chromatography and its application in toxicological analysis, Related Products of imidazoles-derivatives, the publication is Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriumsdiagnostik (1977), 116(11), 1123-9, database is CAplus.

The detection, identification, and determination of 22 tranquilizers in tissues by thin-layer chromatog. using 18 solvent systems and 6 chromogenic reagents is described. The tissues were homogenized, incubated at 100° in concentrated HCl and ether extracted through an acid-base cycle. Tissue distributions of promazine [58-40-2], chlorpromazine [50-53-3], thioridazine [50-52-2], and imipramine [50-49-7] in cases of human poisoning were determined using 2 solvent systems and chromogenic reagents.

Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriumsdiagnostik 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 C12H23N3S, Related Products of imidazoles-derivatives.

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