Month: November 2022

Vyas, Bhavesh M.; Singh, Adarsh J.; Dhattiwala, Abdulkadir S.; Mansuri, Sabera M.; Patel, Varsha J. published an article in 2014, the title of the article was Comparative CNS activities of clinically employed antihistamines (H1 antagonist).SDS of cas: 132-20-7 And the article contains the following content:

Aim: H1 Antihistamines are classified into first generation and second generation agents. The main differences between the first and second generations of drugs are their propensity to cause central nervous system (CNS) side effects. Therefore, present study was aimed to analyze the effects of different H1 antihistamines (first and second generation) on CNS using different animal exptl. models. Materials & methods: H1 antihistamines such as pheniramine maleate (3 mg/kg, 6 mg/kg), cetirizine (0.6 mg/kg, 1.2 mg/kg), levocetirizine (0.6mg/kg, 1.2 mg/kg), loratadine (1 mg/kg, 2 mg/kg) and desloratidine (0.6 mg/kg, 1.2 mg/kg) are evaluated and compared for their effects on CNS using exptl. animal model (Pentobarbitone sleeping time, spontaneous motor activity, motor co-ordination) in Swiss albino mice. Results & Discussion: Desloratadine (0.6mg/kg, 1.2 mg/kg) and loratadine (1 mg/kg, 2 mg/kg) did not produce significant (P < 0.05) effect on sleeping time when compared to control. At 120 min time interval after treatment with cetirizine (1.2 mg/kg) and levocetirizine (1.2 mg/kg) was shown reduction in locomotor activity and remaining three drugs such as pheniramine (6 mg/kg), loratadine (2 mg/kg) and desloratadine did produced any effect on locomotor activity. Treatment with higher dose of pheniramine (6 mg/kg) and cetirizine (1.2 mg/kg) was shown significant (P<0.05) motor coordination while other drugs did not induce any motor in-coordination. First generation antihistamines were shown significant effect on CNS activity at low and high dose while only some second generation antihistamines showed significant effect on CNS at high dose. Conclusion: Numerous well-performed, sensitive measures of psychomotor and cognitive performances are needed to study to compare the effect of first generation and second generation antihistamines on CNS to avoid serious impairment of CNS function. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).SDS of cas: 132-20-7

The Article related to pheniramine maleate cetirizine antihistamine motor activity coordination, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.SDS of cas: 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 31, 2011, Balhara, Yatan Pal Singh; Jain, Raka; Dhawan, Anju; Mehta, Manju published an article.Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate The title of the article was A comparative study of pheniramine and lorazepam for physiological and cognitive/psychomotor task impairment. And the article contained the following:

Context: Pheniramine is being used harmfully in combination with opiates and benzodiazepines through injecting route. Aims: The present study is an attempt to compare the physiol. and psychomotor/cognitive task performance on pheniramine and lorazepam. Settings and Design: The study used a double blind randomly allotted cross-over design. Materials and Methods: The doses of the drugs used were placebo (normal saline) – 2 mL, Pheniramine maleate – 45.5 mg, Lorazepam – 2 mg. The assessments were made at base line and then at 15 min, 120 min and 240 min. The subjects were assessed for the socio-demog. profile, drug use history, physiol. parameters (pulse rate, BP, respiratory rate), and psychomotor/cognitive tasks. Statistical Anal. Used: Anal. was carried out using SPSS ver 10.0. In between, drug comparisons were done using one-way ANOVA (multiple comparisons). Results: Physiol. and cognitive/psychomotor tasks performance did not show any significant difference between pheniramine, lorazepam and placebo. Conclusions: The findings suggest the pheniramine and lorazepam have comparable impairment on physiol. and cognitive/psychomotor task performance. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

The Article related to pheniramine maleate lorazepam cognition psychomotor impairment drug addiction, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shravani, Bezawada; Anuradha, H. V.; Shivamurthy, M. C. published an article in 2017, the title of the article was Tramadol induced partial seizure: a rare adverse drug reaction – case report.Synthetic Route of 132-20-7 And the article contains the following content:

Tramadol is a synthetic codeine analog, acts at μ-opioid receptors (MOR) receptor and used to treat moderate pain with its onset of action being 10-15 min to 1 h and duration lasting upto 4-6 h. It inhibits uptake of norepinephrine and serotonin. It commonly causes vomiting, dry mouth sedation, very rarely seizures. Risk of seizure is more when used at high doses, abused for long time, used concomitantly with certain serotonergic or monoaminergic drugs and in patients with history of epilepsy. A 23 yr young unmarried female patient diagnosed as a case of Acute Pancreatitis and Systemic lupus erythematosis complained of severe low back pain and was prescribed one dose of Inj. Tramadol 50mg i.v. She developed jerky movements of the upper portion of her body involving the left arm and shoulder and uprolling of eye balls to one side after 10 min. This single episode lasted for about a minute and subsided thereafter immediately. Patient was conscious during the episode. No further such episodes noticed. No previous history of drug allergy or past and family history of seizures. No history of smoking, alc., drug abuse. No significant drug interactions were noted with inj. tramadol. This case illustrates that tramadol when used at low doses and without any predisposing risk factors as explained has the propensity to cause seizure. This reaction could be an idiosyncratic reaction. It alarms one to be more vigilant and monitor adverse reaction while prescribing various dose ranges of Tramadol. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Synthetic Route of 132-20-7

The Article related to partial seizure acute pancreatitis systemic lupus erythematosis tramadol delivery, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Synthetic Route of 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 31, 2013, Beraki, Simret; Litrus, Lily; Soriano, Liza; Monbureau, Marie; To, Lillian K.; Braithwaite, Steven P.; Nikolich, Karoly; Urfer, Roman; Oksenberg, Donna; Shamloo, Mehrdad published an article.COA of Formula: C20H24N2O4 The title of the article was A pharmacological screening approach for discovery of neuroprotective compounds in ischemic stroke. And the article contained the following:

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. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).COA of Formula: C20H24N2O4

The Article related to ischemic stroke drug discovery screening neuroprotectant carbenoxolone brain injury, beta hydroxysteroid dehydrogenase, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.COA of Formula: C20H24N2O4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 15, 2018, Moustani, Chrysavgi; Anagnostopoulou, Eleni; Krommyda, Kalliopi; Panopoulou, Christina; Koukoulakis, Konstantinos G.; Bakeas, Evangelos B.; Papadogianakis, Georgios published an article.Product Details of 636-73-7 The title of the article was Novel aqueous-phase hydrogenation reaction of the key biorefinery platform chemical levulinic acid into γ-valerolactone employing highly active, selective and stable water-soluble ruthenium catalysts modified with nitrogen-containing ligands. And the article contained the following:

High catalytic activities (TO = 000 -1) have been achieved by novel water-soluble ruthenium catalysts modified with nitrogen-containing ligands such as the bathophenanthrolinedisulfonic acid disodium salt (BPhDS) in the hydrogenation reaction of the renewable polar platform chem. levulinic acid (LA) which possesses a central relevance in the development of biorefineries of the future in a sustainable way to produce with essentially quant. selectivity of 99.9 mol% γ-valerolactone (GVL) in aqueous media. The apparent activation energy of the Ru/BPhDS catalyst was calculated and amounts a relative low value of 53.3 J/mol when one considers that in the LA hydrogenation reaction this catalyst reduces a less reactive keto group into alc. functionality. A recycling experiment of the Ru/BPhDS catalyst by extraction after addition of di-Et ether has shown that the catalyst is stable without loss of activity and selectivity in a consecutive run. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Product Details of 636-73-7

The Article related to hydrogenation m levulinate gamma valerolactone catalyst, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Product Details of 636-73-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 10, 2008, Minter, Aaron; Stokes, Berlin published a patent.HPLC of Formula: 51566-22-4 The title of the patent was Preparation of diaminopyridines from glutarimidines. And the patent contained the following:

I is prepared by contacting II with a chem. oxidant and/or a dehydrogenation catalyst in liquid ammonia neat, or in a mixture of liquid ammonia and a polar, aprotic solvent, to form a reaction mixture; and heating the reaction mixture to produce I; wherein R1 and R2 are each independently selected from (a) H; (b) a hydrocarbyl group; (c) NR3R4 wherein R3 and R4 are each independently selected from H and a hydrocarbyl group; (d) -CO-R5wherein R5 is a hydrocarbyl group; and (e) YR6 wherein Y is selected from O and S and R6 is selected from H , a hydrocarbyl group, and -COR5 wherein R5 is a hydrocarbyl group. Thus, glutarimidine (111 mg, 0.99 mmol) was combined with Pd-C (100 mg, 0.10 mmol, 10 mol% of 10% Pd on carbon), and then mixed with liquidNH3 (1.0 g, 58.7 mmol) then heated at 200° for 45 h to give 0.14 mmol of 2,6-diaminopyridine in yield 13.7%. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).HPLC of Formula: 51566-22-4

The Article related to glutarimidine dehydrogenation diaminopyridine preparation, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.HPLC of Formula: 51566-22-4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 27, 2011, Minter, Aaron; Stokes, Berlin published a patent.Quality Control of 3-Methylpyridine-2,6-diamine The title of the patent was Process for the synthesis of diaminopyridines from glutarimidines. And the patent contained the following:

A liquid-phase process is provided for the synthesis from glutarimidines of diaminopyridines and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a dehydrogenative aromatization process. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).Quality Control of 3-Methylpyridine-2,6-diamine

The Article related to glutarimidine dehydrogenation diaminopyridine preparation, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Quality Control of 3-Methylpyridine-2,6-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 15, 2021, Flohr, Alexander; Eidam, Olive; Fasching, Bernhard; Meniconi, Mirco; Sadok, Amine; Chopra, Rajesh; Zhuai Wang, Hannah; Caldwell, John Jamieson; Collins, Ian; Ryckmans, Thomas published a patent.Recommanded Product: 39919-70-5 The title of the patent was Isoindolinone compounds as cereblon inhibitors and GSPT1 degraders and their preparation. And the patent contained the following:

Disclosed herein is a compound of formula I or pharmaceutically acceptable salts or stereoisomers thereof. Compounds of formula I wherein X1 is (un)branched C1-6 alkyl, C3-6 cycloalkyl, -C1-6 alkyl-C3-6 cycloalkyl, C6-10 aryl, 5- to 10-membered heteroaryl, etc.; X2 is H, C6-10 aryl, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 4- to 8-membered heterocycloalkyl, etc.; n is 0, 1 and 2; and pharmaceutically acceptable salts, and stereoisomers thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their cereblon inhibitory activity and GSPT1 degradation activity. From the assay, it was determined that compound II exhibited IC50 value of 1037 nM and a DC50 value of > 300 nM. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).Recommanded Product: 39919-70-5

The Article related to isoindolinone preparation cereblon inhibitor gspt1 degrader, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 39919-70-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 19, 2002, Owa, Takashi; Yoshino, Hiroshi; Okauchi, Tatsuo; Okabe, Tadashi; Ozawa, Yoichi; Hata Sugi, Naoko; Yoshimatsu, Kentaro; Nagasu, Takeshi; Koyanagi, Nozomu; Kitoh, Kyosuke published an article.Computed Properties of 636-73-7 The title of the article was Synthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents. And the article contained the following:

The synthesis and antitumor activity of E7070 analogs containing a 3-pyridinesulfonamide moiety is reported. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clin. trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogs examined, ER-35745 (I), a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Computed Properties of 636-73-7

The Article related to pyridinesulfonamide indolyl derivative preparation antitumor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 636-73-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 10, 2008, Minter, Aaron; Stokes, Berlin published a patent.Application of 51566-22-4 The title of the patent was Preparation of diaminopyridines from glutaronitriles. And the patent contained the following:

I is prepared by contacting II with a chem. oxidant and/or a dehydrogenation catalyst in liquid ammonia neat, or in a mixture of liquid ammonia and a polar, aprotic solvent, to form a reaction mixture; and heating the reaction mixture to produce I; wherein R1 and R2 are each independently selected from (a) H; (b) a hydrocarbyl group; (c) NR3R4 wherein R3 and R4 are each independently selected from H and a hydrocarbyl group; (d) -CO-R5wherein R5 is a hydrocarbyl group; and (e) YR6 wherein Y is selected from O and S and R6 is selected from H , a hydrocarbyl group, and -COR5 wherein R5 is a hydrocarbyl group. Thus, glutaronitrile (3.0 g, 31.9 mmol) was combined with Pd-C (3.39 g, 3.19 mmol, 10 mol% of 10% Pd on carbon) and mixed with liquid NH3 (1.0 g, 58.7 mmol), then heated at 200° for 45 h and a pressure of approx. 90 psi to give 2.43 mmol of 2,6-diaminopyridine in 7.6 % net yield. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).Application of 51566-22-4

The Article related to glutaronitrile amination dehydrogenation diaminopyridine preparation, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Application of 51566-22-4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem