Day: December 6, 2022

Shankpal, Pramod published the artcileEvaluation of anti-anxiety effect of nifedipine compared to diazepam in swiss albino mice using behavioural models, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is nifedipine diazepam anxiolytic dihydropyridines elevated plus maze behavioral model.

The present study was undertaken to evaluate the acute and chronic anxiolytic effects of nifedipine in comparison to diazepam using in Swiss Albino mice using two behavioral models. 30 Swiss albino mice were divided into 5 groups with 6 mice in each group. The study was conducted in two phases to evaluate acute and chronic effects. The groups consisted of diazepam (1 mg/kg), 3 doses of nifedipine (2.6 mg/kg, 5.2 mg/kg and 10.4 mg/kg) and vehicle control. The Elevated Plus Maze (EPM) and Light and Dark box were used to evaluate the anti-anxiety effects. The number of entries and time spent in the open arm of the elevated plus-maze and in the light area of light and dark box model were noted and compared among the 5 groups. Observations were analyzed using ANOVA and post hoc Tukey’s test. Nifedipine (5.2 mg/kg and 10.4 mg/kg) significantly increased the number of entries and time spent in the open arm compared to vehicle control in the EPM test (p < 0.001). Similarly, in the light and dark box test, nifedipine (5.2 mg/kg and 10.4 mg/kg) increased the number of entries and time spent in the light area compared to vehicle control (p < 0.05). However, the low dose of nifedipine (2.6 mg/kg) did not exhibit significant findings. Two doses of nifedipine (5.2 mg/kg and 10.4 mg/kg) possess anti-anxiety effects both on acute and chronic administration in both elevated plus maze and light and dark box model. International Journal of Pharmacy and Pharmaceutical Sciences published new progress about Amygdala. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ishida, Yoshiyuki published the artcileSequence selective dual-emission detection of (i, i + 1) bis-phosphorylated peptide using diazastilbene-type Zn(ii)-Dpa chemosensor, COA of Formula: C7H6ClNO2, the main research area is sequence selective dual emission bisphosphorylated peptide diazastilbene zinc chemosensor.

This paper describes a new fluorescent chemosensor for phosphorylated peptide, which comprises a rigid trans-4,4′-diazastilbene and two Zn(II)-Dpa (2,2′-dipicolylamine) units; this chemosensor sequence-selectively binds to a (i, i + 1) bis-phosphorylated peptide and displays a dual-emission fluorescence change.

Chemical Communications (Cambridge, United Kingdom) published new progress about Affinity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, COA of Formula: C7H6ClNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fagerberg, Jonas Henrik published the artcileAffinity of Lipophilic Drugs to Mixed Lipid Aggregates in Simulated Gastrointestinal Fluids, Computed Properties of 72509-76-3, the main research area is sodium taurocholate affinity lipophilic lipid aggregate simulated gastrointestinal fluid; Affinity; Biorelevant dissolution media; Drug lipophilicity; Ionization; Mixed lipid aggregates; Solubilization.

Mixed lipid aggregates, comprising of bile salts and phospholipids, present in the small intestine assist in drug solubilization and subsequent drug dissolution and absorption through the intestinal epithelium. The increased variability in their levels, observed physiol., may create challenges not only for in vivo bioavailability and bioequivalence studies, but also for in vitro bio-predictive studies as correlations between in vitro and in vivo data are not always successful. The current study investigated the impact of biorelevant dissolution media, with physiol. relevant sodium taurocholate and lecithin levels, on the apparent solubility and affinity of lipophilic compounds with a wide range of physicochem. properties (drug ionization, drug lipophilicity, mol. weight) to mixed lipid aggregates. Apparent solubility data in biorelevant dissolution media for the studied neutral drugs, weak bases and weak acids were compared against a phosphate buffer pH 6.5 in the absence of these lipidic components. Presence of mixed lipid aggregates enhanced the apparent solubility of the majority of compounds and the use of multivariate data anal. identified the significant parameters affecting drug affinity to mixed lipid aggregates based on the chem. class of the drug. For neutral drugs, increasing bile salt concentrations and/or drug lipophilicity resulted in greater enhancement in apparent solubility at 24-h. For weak bases and weak acids, the effect of increasing bile salt levels on apparent solubility depended mostly on an interplay between drug lipophilicity and drug ionization.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Affinity. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mishra, Abhishek Kumar published the artcileFunctional insights into voltage gated proton channel (Hv1) in bull spermatozoa, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is cAMP PKA voltage gated proton channel biomarker spermatozoa; Capacitation, 2-GBI, zinc, AEA, bull, spermatozoa; Catsper; Hv1; PKA; Sperm motility; sAC.

Acid extrusion and intracellular alkalisation are the key events during sperm capacitation and these are mediated through proton gated channels (Hv1). Role of Hv1 in regulating sperm motility, capacitation and acrosome reaction has been documented in human spermatozoa; but no such data is available in bull spermatozoa; therefore, the present study was undertaken in Hariana bull spermatozoa. Sixty four ejaculates were collected from four Hariana bulls to investigate the functional involvement of Hv1 in regulation of sperm motility, capacitation and acrosome reaction in bull spermatozoa. Immunoblotting revealed the presence of a single band of 31.8 kDa corresponding to Hv1 in Hariana bull spermatozoa and immunofluorescence confirmed the pos. immune-reactivity at principal piece of spermatozoa for Hv1. Functional study was carried out using 200μM 2- Guadinobenzimidazole (2-GBI,selective Hv1 blocker) and 1 mM zinc chloride (potent Hv1 blocker), and 0.3μM Anandamide (AEA), an activator of Hv1. Blocking as well as activation of Hv1 resulted in significant (P < 0.05) reduction in sperm livability, spermatozoa having intact membrane, intact acrosome, and high mitochondrial transmembrane potential (MTP). Further studies are required to find out the possible relationship between Hv1 channels and other channels in regulating spermatozoa functions. Theriogenology published new progress about Acrosome. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hong, Ji Young published the artcileAntenatal magnesium sulfate treatment and risk of necrotizing enterocolitis in preterm infants born at less than 32 weeks of gestation, Product Details of C17H18N2O6, the main research area is necrotizing enterocolitis gestation magnesium sulfate.

Abstract: Antenatal magnesium sulfate (MgSO4) treatment is widely used for fetal neuroprotection in women at risk of preterm delivery. However, some studies have recently suggested that in utero MgSO4 exposure is associated with an increased risk of necrotizing enterocolitis (NEC). This study aimed to investigate the association between antenatal MgSO4 treatment and risk of NEC. This retrospective cohort study included 756 infants born at 24-31 wk gestation. Subjects were classified into three groups: period 1, when MgSO4 treatment protocol for fetal neuroprotection was not adopted (n = 267); period 2, when the protocol was adopted (n = 261); and period 3, when the protocol was withdrawn because of concern of risk of NEC (n = 228). Rates of NEC (�stage 2b) were analyzed according to time period and exposure to antenatal MgSO4. Significant difference in the rate of NEC was not found across the three time periods (2.6% vs. 6.5% vs. 4.8% in periods 1, 2 and 3, resp., p = 0.103). The rate of NEC was comparable between the infants exposed and unexposed to antenatal MgSO4 (5.1% vs. 3.6%, p = 0.369). These results showed that antenatal MgSO4 treatment was not associated with risk of NEC in our study population.

Scientific Reports published new progress about Acidosis. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shen, Hsuan-Shu published the artcileChinese herbal medicines have potentially beneficial effects on the perinatal outcomes of pregnant women, HPLC of Formula: 21829-25-4, the main research area is chinese herbal medicine premature birth miscarriage population; Chinese herbal products; National health insurance research database; preterm labor; threatened miscarriage; tocolytic treatment.

Tocolytic treatment is beneficial to pregnant women with a risk of premature labor or miscarriage. However, previous reports have shown that progestogen might not be effective and ritodrine may increase the risk of maternal vascular-related diseases. Chinese herbal products (CHP) are used as alternative therapies for pregnant women. The goal was to evaluate the efficacy of combined tocolytic therapy and CHP therapy in pregnancy outcomes for pregnant women in Taiwan. We conducted a retrospective cohort study based on the National Health Insurance Research Database. A total of 47,153 pregnantwomen treatedwith tocolytics aged 18-50 years from 2001 to 2015 were selected from two million random samples. According to the medical use of tocolytics and CHP, we divided the users into two groups: westernmedicine (WM) only (n = 40,961) andWM/CHP (n = 6,192) groups. A propensity score (PS)-matched cohort (6,192 pairs) was established based on baseline confounders. All participants were followed up to perinatal outcomes. Conditional logistic regression anal. was used to examine the effects of CHP use on the odds of miscarriage and preterm birth. The adjusted odds ratio (OR) for premature birth in the WM/CHP group (n = 411, 6.64%) was significantly lower than in the WM group (n = 471, 7,61%) (0,86, 95% confidence interval [CI], 0.74-0.99). Further subgroup anal. based on the usage of formulas that activate blood and remove stasis or purgative formulas, the adjusted OR of preterm birth of those using these formulas was significantly lower in theWM/CHP group (n = 215, 6.32%) than that in theWM group (n = 265, 7.77%) (OR: 0.79, 95% CI: 0.65-0.96). We found that the combination of CHP and tocolytics can be beneficial to pregnant women in the prevention of premature birth. Further research is required to investigate causal relationships.

Frontiers in Pharmacology published new progress about Abortion. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Makara, Gergely M. published the artcileSynthesis of Bicyclic Pyrimidine Derivatives as ATP Analogues, Formula: C26H42Br2N2, the main research area is pyrimidine bicyclic derivative solid phase synthesis reduction; ATP analog solid phase synthesis reduction.

A highly efficient and general solid-phase synthesis of bicyclic pyrimidine derivatives that target purine dependent proteins is reported. The synthesis of the key intermediate, 4,6-disubstituted-5-amino-pyrimidine, involved reduction of the corresponding nitro derivatives using 1,1′-dioctyl-viologen in a triphasic milieu. The mild reduction conditions enable the use of any acid labile solid support as well as a wide range of combinatorial substituents, thus enabling the synthesis of large libraries of highly diverse bicyclic pyrimidines. Alternative reduction conditions with tin(II) chloride and structure-reactivity studies are discussed as well.

Journal of Organic Chemistry published new progress about Reduction. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Formula: C26H42Br2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Udumyan, Ruzan published the artcileBeta-blocker use and lung cancer mortality in a nationwide cohort study of patients with primary non-small cell lung cancer, Category: pyridine-derivatives, the main research area is non small cell lung cancer mortality beta blocker.

β-Adrenergic receptor blockers have been associated with improved survival among patients with different types of malignancies, but available data for patients with non-small cell lung cancer are contradictory and limited to small hospital-based studies. We aimed to investigate whether β-blocker use at time of cancer diagnosis is associated with lung cancer mortality in largest general population-based cohort of patients with NSCLC to date. For this retrospectively defined nationwide cohort study, we used prospectively collected data from Swedish population and health registers. Through Swedish Cancer Register, we identified 18,429 patients diagnosed with primary NSCLC between 2006 and 2014 with follow-up to 2015. Cox regression was used to estimate the association between β-blocker use at time of cancer diagnosis ascertained from the Prescribed Drug Register and cancer-specific mortality identified from the Cause of Death Register. Over a median follow-up of 10.2 mo, 14,994 patients died. Compared with nonuse, β-blocker use was not associated with lung cancer mortality [HR (95% confidence interval): 1.01 (0.97-1.06)]. However, the possibility that diverging associations for specific β-blockers and some histopathol. subtypes exist cannot be excluded. In this nationwide cohort of patients with NSCLC, β-blocker use was not associated with lung cancer mortality when assessed in aggregate in the total cohort, but evidence for some β-blockers is less conclusive.

Cancer Epidemiology, Biomarkers & Prevention published new progress about Diagnosis. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cobine, Caroline A. published the artcileRhythmic calcium transients in smooth muscle cells of the mouse internal anal sphincter, Application In Synthesis of 21829-25-4, the main research area is calcium transient smooth muscle cell internal analysis sphincter; gastrointestinal; interstitial cells of Cajal; pacemaker; slow wave; tone.

Ca2+ transients displayed ongoing rhythmic firings at both lengths and were abolished by nifedipine and the KATP channel activator pinacidil indicating their dependence upon CavL. Like SWs, CTs were greatest in frequency and amplitude at the distal extremity and conducted proximally. Removal of the distal IAS reduced but did not abolish CTs. The time constant for clearing cytoplasmic Ca2+ averaged 0.46 s and basal Ca2+ levels were significantly elevated. The similarities in spatiotemporal and pharmacol. properties of CTs and SWs suggest that SW gives rise to CTs while muscle stretch is not required. Elevated relative basal Ca2+ in the IAS is likely due to the inability of cells to clear or sequester Ca2+ between rapid frequency voltage-dependent Ca2+ entry events, i.e., conditions that will lead to tone development. The conduction of CTs from distal to proximal IAS will lead to orally directed contractions and likely contribute to the maintenance of fecal continence.

Neurogastroenterology & Motility published new progress about Cytoplasm. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Xiaoxi published the artcileRegulating Molecular Recognition with C-Shaped Strips Attained by Chirality-Assisted Synthesis, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, the main research area is chirality assisted synthesis mol recognition mol shape strip; chirality-assisted synthesis; cooperative effects; host-guest interactions; shape control; supramolecular chemistry.

Chirality-assisted synthesis (CAS) is a general approach to control the shapes of large mol. strips. CAS is based on enantiomerically pure building blocks that are designed to strictly couple in a single geometric orientation. Fully shape-persistent structures can thus be created, even in the form of linear chains. With CAS, selective recognition between large host and guest mols. can reliably be designed de novo. To demonstrate this concept, three C-shaped strips that can embrace a pillar[5]arene macrocycle were synthesized. The pillar[5]arene bound to the strips was a better host for electron-deficient guests than the free macrocycle. Exptl. and computational evidence is provided for these unique cooperative interactions to illustrate how CAS could open the door towards the precise positioning of functional groups for regulated supramol. recognition and catalysis.

Angewandte Chemie, International Edition published new progress about Chirality. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Safety of 1,1-Di-n-octyl-4,4-bipyridinium Dibromide.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem