China
Africa
Explore chapters and articles related to this topic
Therapeutic Efficacy of Black Pepper in Gastrointestinal Disorders
Published in Megh R. Goyal, Preeti Birwal, Durgesh Nandini Chauhan, Herbs, Spices, and Medicinal Plants for Human Gastrointestinal Disorders, 2023
Piperine is a piperidine alkaloid with a pungent flavor and it has been studied in rats or mice in association with stomach mucosal harm induced by pressure, indomethacin, ethanol or pylorus ligature. This material shielded the stomach from ulceration by reducing the quantity of intravenous and oral gastric juice, acidity and pepsin-A function with respective dosage of 1.5 and 25 mg/kg, respectively.18
Antihistamines, Decongestants, and Expectorants during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Piperidine was discovered in 1850 and is a substrate in the manufacture of several classes of drugs (SSRIs, antipsychotics, vasodilators), including antihistamines. Birth defects were not increased in frequency among 127 infants exposed to azatadine during the first trimester (Gilbert et al., 2005). The frequency of congenital anomalies was not increased among 285 infants whose mothers took cyproheptadine during embryogenesis (Gilbert et al., 2005; see Table 11.3). No epidemiological studies of birth defects or adverse fetal effects among infants born to mothers who took diphenylpyraline during pregnancy are published. Animal teratology studies of cyproheptadine are not consistent (de la Fuente and Alia, 1982; Rodriguez-Gonzalez et al., 1983; Weinstein et al., 1975), making it impossible to interpret the findings. No animal teratology studies of azatadine are published.
Other Sleep Modulators
Published in Shojiro Inoué, Biology of Sleep Substances, 2020
Piperidine (see Figure 1) is a biogenic amine and a normal constituent of the central nervous system of both invertebrates and vertebrates, and regarded as a neuromodulator or a hypnogenic substance.1 This substance is also widely distributed in the peripheral organs. Kasé et al.2 demonstrated that piperidine intraperitoneally (i.p.) injected at doses of 40 and 80 mg/kg induced pronounced sedation and prolongation of hexobarbital-induced narcosis in mice. They also suggested that piperidine may act as a stimulator of the nicotinic cholinergic receptor. Stepita-Klauco et al.3 found that brain concentrations of piperidine increased to 36.6 nmol/g during dormancy from 2.0 nmol/g during the active state in mice. The brain content of piperidine also increased during dormancy or hibernation in snails.4 Miyata et aj 5,6,9-12 Qkano et al.,7,8 and Aisaka et al.13 studied extensively the biological and pharmacological properties of piperidine, such as its hypnogenic activity;5 its concentrations in the brain,6 7 blood,8 and urine;8 its changes in brain levels depending on seasonal activity,9 anesthesia,10,12 or sleep deprivation;12 and its vasodilating activity.13
Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Dong-Jun Fu, Si-Meng Liu, Jia-Jia Yang, Jun Li
Piperidine is a privileged scaffold in the field of drug discovery which provides numerous opportunities in exploring this moiety as an anticancer agent by acting on various receptors of utmost importance (Figure 2)14. Pomalidomide (7) was a FDA approved drug to treat multiple myeloma by inhibiting TNFα15. Piperidine 8 displayed the antiproliferative activity with IC50 values from 5.4 µM to 8.5 µM against A549, MCF7, DU145, and HeLa cell lines16. Piperidine derivative 9 was a novel human heat shock protein 70 inhibitor for the treatment of drug-resistant tumours17. 5-Phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivative 10 occupied high antiproliferative activities against SGC-7901, MGC-803 and Bcap-37 cells18. Piperidine 11 affected the cell viability and induced G2/M phase cell cycle arrest in K562 cells19. Piperidine 12 was a selective inhibitor against triple-negative breast cancer cell line MDA-MB-46820.
Development and validation of probe drug cocktails for the characterization of CYP450-mediated metabolism by human heart microsomes
Published in Xenobiotica, 2019
Jade Huguet, Fleur Gaudette, Veronique Michaud, Jacques Turgeon
Bufuralol 1-hydroxylation maximal velocity was decreased 2.3-times compared to a 3.6-times decrease in its apparent Km when incubated in cocktail #2 versus alone (Table 5, Figure 2(A)). Bufuralol 1-hydroxylation CLint was increased 1.7-time when incubated in cocktail #2 (Table 5). Ethoxyresorufin O-deethylase (EROD) activity with rhCYP1A1 was unchanged by the presence of other substrates in cocktail #2 (Figure 2(B)). Repaglinide hydroxylation on the piperidine ring through rhCYP2C8 fitted a substrate inhibition model (Figure 2(C), Table 5) when the drug was incubated as part of cocktail #2. Ratios of kinetic parameters derived from a substrate inhibition model from incubations performed with either cocktail #2 or alone were close to unity for Km (Km cocktail#2/Km solo = 0.9, p > .05) and Vmax (Vmax cocktail#2/Vmax solo = 1.06, p > .05). Repaglinide maximal velocity of its M1 metabolite formation with rhCYP2C8 was increased 4.56-times when incubations were performed with cocktail #2 while its apparent Km was decreased by 2.82-times (p < .05, Figure 2(D) and Table 5). Repaglinide clearance through M1-formation pathway represents 2% of the hydroxylated-pathway when incubated alone with rhCYP2C8 and remains at 2% when co-incubated in cocktail #2.
Discovery of human autophagy initiation kinase ULK1 inhibitors by multi-directional in silico screening strategies
Published in Journal of Receptors and Signal Transduction, 2019
Poornimaa Mu, Ramanathan Karuppasamy
Scaffolds of each hit namely DB12686 (piperidine carboxamide), DB08341 (benzenesulfonamide), DB07936 (benzamide), and DB07163 (isoindolone) were analyzed for its interaction with the target protein. Further, the literature evidence reported that each of the scaffolds would effectively act as an anti-cancerous agent. Of note, Sulfonamide and benzamide derivatives were reported to act via a variety of mechanisms like angiogenesis inhibition, cell cycle alteration in G phase and suppression of transcriptional factors [52]. Note that isoindolone derivatives were found to be an efficient kinase inhibitor with anti-proliferative activity [53]. Furthermore, piperidine was found to inhibit cholesterol conversion [54].