benzeneacetamides

Summary

Summary: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.

Top Publications

  1. Fang F, Liu G. Novel squamosamide derivative (compound FLZ) attenuates Abeta25-35-induced toxicity in SH-SY5Y cells. Acta Pharmacol Sin. 2008;29:152-60 pubmed publisher
  2. Zhang D, Hu X, Wei S, Liu J, Gao H, Qian L, et al. Squamosamide derivative FLZ protects dopaminergic neurons against inflammation-mediated neurodegeneration through the inhibition of NADPH oxidase activity. J Neuroinflammation. 2008;5:21 pubmed publisher
    ..Hence, prevention of microglial over-activation has been shown to be a prime target for the development of therapeutic agents for inflammation-mediated neurodegenerative diseases...
  3. Zhang D, Zhang J, Liu G. The novel squamosamide derivative FLZ protects against 6-hydroxydopamine-induced apoptosis through inhibition of related signal transduction in SH-SY5Y cells. Eur J Pharmacol. 2007;561:1-6 pubmed
    ..The results suggested that FLZ has potential neuroprotective effect on 6-OHDA-induced apoptosis of SH-SY5Y cells through regulating related signal-transduction...
  4. Zhang D, Zhang J, Liu G. The novel squamosamide derivative (compound FLZ) attenuated 1-methyl, 4-phenyl-pyridinium ion (MPP+)-induced apoptosis and alternations of related signal transduction in SH-SY5Y cells. Neuropharmacology. 2007;52:423-9 pubmed
    ..The results suggest that cFLZ possesses potent neuroprotective activity and may be a potential anti-Parkinson's disease drug worthy for further study...
  5. Fang F, Liu G. Protective effects of compound FLZ on beta-amyloid peptide-(25-35)-induced mouse hippocampal injury and learning and memory impairment. Acta Pharmacol Sin. 2006;27:651-8 pubmed
    ..To study the protective effects of compound FLZ, a novel synthetic analogue of natural squamosamide, on learning and memory impairment and lesions of the hippocampus caused by icv injection of beta-amyloid(25-35)(Abeta(25-35)) in mice...
  6. Feng W, Wei H, Liu G. Pharmacological study of the novel compound FLZ against experimental Parkinson's models and its active mechanism. Mol Neurobiol. 2005;31:295-300 pubmed
    ..Additionally, FLZ inhibited cytochrome-c release from mitochondria and caspase-3 activation by dopamine in PC-12 cells. The above results suggest that compound FLZ possesses anti-PD activity through neuroprotection...
  7. Crescenzi E, Palumbo G, de Boer J, Brady H. Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin Cancer Res. 2008;14:1877-87 pubmed publisher
    ..We set out to find a means to specifically induce senescent tumor cells to undergo cell death and not to reenter the cell cycle that may have general application in cancer therapy...
  8. Hou Y, Yu Y, Liu G, Luo Y. A natural squamosamide derivative FLZ reduces amyloid-beta production by increasing non-amyloidogenic AbetaPP processing. J Alzheimers Dis. 2009;18:153-65 pubmed publisher
    ..These findings suggest that FLZ reduces Abeta production by promoting AbetaPP non-amyloidogenic alpha-secretase processing. As such, FLZ may have therapeutic potential for the treatment of AD...
  9. Lee T, Schwandner R, Swaminath G, Weiszmann J, Cardozo M, Greenberg J, et al. Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2. Mol Pharmacol. 2008;74:1599-609 pubmed publisher

More Information

Publications61

  1. Lindstrom R, Kim T. Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenac. Curr Med Res Opin. 2006;22:397-404 pubmed
    ..Preclinical data suggest nepafenac may also provide unique efficacy in the posterior segment...
  2. Xie P, Jiao X, Liang X, Feng W, Wei H, Liu G. [Synthesis and antioxiactivity of squamosamide cyclic analogs]. Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 2004;26:372-8 pubmed
    ..To design and synthesize a series of squamosamide cyclic analogues and to test their antioxidation activity...
  3. Fang F, Liu G. A novel cyclic squamosamide analogue compound FLZ improves memory impairment in artificial senescence mice induced by chronic injection of D-galactose and NaNO2. Basic Clin Pharmacol Toxicol. 2007;101:447-54 pubmed
  4. Bonadonna R, Heise T, Arbet Engels C, Kapitza C, Avogaro A, Grimsby J, et al. Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study. J Clin Endocrinol Metab. 2010;95:5028-36 pubmed publisher
    ..Glucokinase plays a key role in glucose homeostasis. Glucokinase activators can lower glucose levels in both animal and human type 2 diabetes, but their mechanism of action has never been explored in humans...
  5. Dermitzaki E, Gravanis A, Venihaki M, Stournaras C, Margioris A. Opioids suppress basal and nicotine-induced catecholamine secretion via a stabilizing effect on actin filaments. Endocrinology. 2001;142:2022-31 pubmed
    ..It also appears that basal catecholamine secretion is associated with opioid-sensitive machinery regulating the continuous formation of short-lived areas of cortical actin filament disassembly...
  6. Hirose H, Aoki I, Kimura T, Fujikawa T, Numazawa T, Sasaki K, et al. Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity. J Pharmacol Exp Ther. 2001;297:790-7 pubmed
    ..Thus, compound A may have fewer cardiac or CNS side effects than nonselective compounds...
  7. Belcheva M, Wong Y, Coscia C. Evidence for transduction of mu but not kappa opioid modulation of extracellular signal-regulated kinase activity by G(z) and G(12) proteins. Cell Signal. 2000;12:481-9 pubmed
    ..In this and prior studies, Galpha(z) and Galpha(12) immunoreactivity were detected in untransfected COS-7 cells, suggesting that these G proteins may be endogenous mediators of chronic mu inhibitory actions on ERK...
  8. Dalby Brown W, Jessen C, Hougaard C, Jensen M, Jacobsen T, Nielsen K, et al. Characterization of a novel high-potency positive modulator of K(v)7 channels. Eur J Pharmacol. 2013;709:52-63 pubmed publisher
    ..Our findings with NS15370 consolidate neuronal K(v)7 channels as targets for anti-epileptic and psychiatric drug development...
  9. Bucci F, Waterbury L, Amico L. Prostaglandin E2 inhibition and aqueous concentration of ketorolac 0.4% (acular LS) and nepafenac 0.1% (nevanac) in patients undergoing phacoemulsification. Am J Ophthalmol. 2007;144:146-7 pubmed
    ..To determine the prostaglandin E(2) (PGE(2)) levels and aqueous concentrations achieved with ketorolac 0.4% (Acular LS; Allergan, Inc, Irvine, California, USA) and nepafenac 0.1% (Nevanac; Alcon Laboratories, Inc, Fort Worth, Texas, USA)...
  10. Butelman E, Kreek M. kappa-Opioid receptor agonist-induced prolactin release in primates is blocked by dopamine D(2)-like receptor agonists. Eur J Pharmacol. 2001;423:243-9 pubmed
  11. Beattie D, Cheruvu M, Mai N, O Keefe M, Johnson Rabidoux S, Peterson C, et al. The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexone. Naunyn Schmiedebergs Arch Pharmacol. 2007;375:205-20 pubmed
    ..The clinical significance of the data from this study remains to be determined...
  12. Dhanesha N, Joharapurkar A, Shah G, Kshirsagar S, Patel V, Patel K, et al. Treatment with exendin-4 improves the antidiabetic efficacy and reverses hepatic steatosis in glucokinase activator treated db/db mice. Eur J Pharmacol. 2013;714:188-92 pubmed publisher
    ..Overall, our data indicate that combination of GKA and GLP-1 receptor agonist Ex-4 improves glucose homeostasis, shows antiobesity activity, without causing harmful side effects like fatty liver. ..
  13. Parsadaniantz S, Lebeau A, Duval P, Grimaldi B, Terlain B, Kerdelhue B. Effects of the inhibition of cyclo-oxygenase 1 or 2 or 5-lipoxygenase on the activation of the hypothalamic-pituitary-adrenal axis induced by interleukin-1beta in the male Rat. J Neuroendocrinol. 2000;12:766-73 pubmed
  14. Takahashi A, Mori E, Su X, Nakagawa Y, Okamoto N, Uemura H, et al. ATM is the predominant kinase involved in the phosphorylation of histone H2AX after heating. J Radiat Res. 2010;51:417-22 pubmed
    ..These results indicate that ATM is the predominant protein which is active in the phosphorylation of histone H2AX after heating...
  15. Wentland M, Xu G, Cioffi C, Ye Y, Duan W, Cohen D, et al. 8-Aminocyclazocine analogues: synthesis and structure-activity relationships. Bioorg Med Chem Lett. 2000;10:183-7 pubmed
    ..Most targets were efficiently synthesized from the triflate of cyclazocine or its enantiomers using Pd-catalyzed amination procedures...
  16. Palma Carlos M, Palma Carlos A, Medina M. "In vivo" and "in vitro" tests in the diagnosis of Beta-lactams allergy. Eur Ann Allergy Clin Immunol. 2007;39:157-61 pubmed
    ..Skin test gave an overall positivity of 85% and determination of specific IgE of 42%. Skin tests have a greater sensitivity but "in vitro" tests are an useful associated diagnostic method...
  17. Shippenberg T, LeFevour A, Thompson A. Sensitization to the conditioned rewarding effects of morphine and cocaine: differential effects of the kappa-opioid receptor agonist U69593. Eur J Pharmacol. 1998;345:27-34 pubmed
    ..U69593 prevents sensitization and cross-sensitization induced by cocaine, but does not modify morphine-induced sensitization or the cross-sensitization which develops to cocaine after morphine administration...
  18. D Addario C, Di Benedetto M, Candeletti S, Romualdi P. The kappa-opioid receptor agonist U-69593 prevents cocaine-induced phosphorylation of DARPP-32 at Thr(34) in the rat brain. Brain Res Bull. 2007;73:34-9 pubmed
    ..These data could be considered consistent with the ability of kappa opioid agonists to attenuate many behavioural and neurochemical effects of cocaine...
  19. Tang M, Khan M, Croxford J, Tan K, Angeli V, Gasser S. The DNA damage response induces antigen presenting cell-like functions in fibroblasts. Eur J Immunol. 2014;44:1108-18 pubmed publisher
    ..Hence, the DDR may alert the immune system to the presence of potentially dangerous cells by upregulating the expression of ligands that can induce the activation of innate and adaptive immune cells...
  20. Ferain T, Hoveyda H, Ooms F, Schols D, Bernard J, Fraser G. Agonist-induced internalization of CC chemokine receptor 5 as a mechanism to inhibit HIV replication. J Pharmacol Exp Ther. 2011;337:655-62 pubmed publisher
  21. Perreault M, Seeman P, Szechtman H. Kappa-opioid receptor stimulation quickens pathogenesis of compulsive checking in the quinpirole sensitization model of obsessive-compulsive disorder (OCD). Behav Neurosci. 2007;121:976-91 pubmed
    ..The animal model findings point to a potential role of kappa opioid systems in hastening the pathogenesis of OCD and to the possibility that distinct brain regions may mediate the development and the expression of compulsive checking...
  22. Li L, Zhang J, Wang Y, Wei H, Liu G. Establishment of a HPLC method for preclinical pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rats. Biomed Chromatogr. 2008;22:867-72 pubmed publisher
  23. Ravid S, Podrid P, Lampert S, Lown B. Congestive heart failure induced by six of the newer antiarrhythmic drugs. J Am Coll Cardiol. 1989;14:1326-30 pubmed
  24. Heier J, Awh C, Busbee B, Waterbury L, Daniel P, Stoller G, et al. Vitreous nonsteroidal antiinflammatory drug concentrations and prostaglandin E2 levels in vitrectomy patients treated with ketorolac 0.4%, bromfenac 0.09%, and nepafenac 0.1%. Retina. 2009;29:1310-3 pubmed publisher
    ..To assess vitreous concentrations of nonsteroidal antiinflammatory drugs (NSAIDs) and prostaglandin E(2) in patients treated with NSAIDs before vitrectomy...
  25. Debnath A. Prospects and strategies for the discovery and development of small-molecule inhibitors of six-helix bundle formation in class 1 viral fusion proteins. Curr Opin Investig Drugs. 2006;7:118-27 pubmed
    ..Small-molecule inhibitors that disrupt six-helix bundle formation and prevent viral infection have been identified. This review will focus on the discovery of these small-molecule inhibitors...
  26. Horan P, de Costa B, Rice K, Haaseth R, Hruby V, Porreca F. Differential antagonism of bremazocine- and U69,593-induced antinociception by quadazocine: further functional evidence of opioid kappa receptor multiplicity in the mouse. J Pharmacol Exp Ther. 1993;266:926-33 pubmed
    ..abstract truncated at 250 words)..
  27. Fang F, Wang Q, Liu G. FLZ, synthetic squamosamide cyclic derivative, attenuates memory deficit and pathological changes in mice with experimentally induced aging. Naunyn Schmiedebergs Arch Pharmacol. 2012;385:579-85 pubmed publisher
    ..These findings suggested that FLZ improves the performance in the step-down task and the pathological alternations in senescent mice...
  28. Vanderschuren L, Schoffelmeer A, Wardeh G, de Vries T. Dissociable effects of the kappa-opioid receptor agonists bremazocine, U69593, and U50488H on locomotor activity and long-term behavioral sensitization induced by amphetamine and cocaine. Psychopharmacology (Berl). 2000;150:35-44 pubmed
    ..By influencing dopaminergic neurotransmission, opioid drugs can alter the behavioral effects of psychostimulants...
  29. Chatzaki E, Makrigiannakis A, Margioris A, Kouimtzoglou E, Gravanis A. The Fas/FasL apoptotic pathway is involved in kappa-opioid-induced apoptosis of human endometrial stromal cells. Mol Hum Reprod. 2001;7:867-74 pubmed
    ..In conclusion, our data suggest that endometrial opioid dynorphins may participate in the apoptotic processes related to endometrial tissue remodelling during early pregnancy or menstruation...
  30. Takahashi K, Saishin Y, Saishin Y, Mori K, Ando A, Yamamoto S, et al. Topical nepafenac inhibits ocular neovascularization. Invest Ophthalmol Vis Sci. 2003;44:409-15 pubmed
    ..In this study, we tested the effect of topical nepafenac in three murine models of ocular neovascularization (NV)...
  31. Suzuki T, Izumimoto N, Takezawa Y, Fujimura M, Togashi Y, Nagase H, et al. Effect of repeated administration of TRK-820, a kappa-opioid receptor agonist, on tolerance to its antinociceptive and sedative actions. Brain Res. 2004;995:167-75 pubmed
    ..The difference in the potency for down-regulating the kappa-opioid receptors in the brain may account for the tolerance-development potency of the compounds...
  32. Schmidt B, Tambeli C, Levine J, Gear R. mu/delta Cooperativity and opposing kappa-opioid effects in nucleus accumbens-mediated antinociception in the rat. Eur J Neurosci. 2002;15:861-8 pubmed
  33. Durand G, Hubert M, Kuno H, Cook W, Boussiquet Leroux C, Owen R, et al. Muscarinic receptor antagonist-induced lenticular opacity in rats. Toxicol Sci. 2002;66:166-72 pubmed
    ..No such lenticular opacities have been reported in other animal species, including man, after treatment with muscarinic receptor antagonists...
  34. Simpson A, Murphy A, Yousef E. The acceptability of a four-part protocol for penicillin allergy testing by practicing allergists. Allergy Asthma Proc. 2009;30:192-201 pubmed publisher
    ..Forty-five percent of the fellows of the AAAAI would apply the proposed protocol to test for PCN allergy. Sixty-two percent said they may apply the protocol if a larger study was performed...
  35. Romano A, Gaeta F, Valluzzi R, Caruso C, Rumi G, Bousquet P. The very limited usefulness of skin testing with penicilloyl-polylysine and the minor determinant mixture in evaluating nonimmediate reactions to penicillins. Allergy. 2010;65:1104-7 pubmed publisher
  36. McDermott L, Iyer P, Vernetti L, Rimer S, Sun J, Boby M, et al. Design and evaluation of novel glutaminase inhibitors. Bioorg Med Chem. 2016;24:1819-39 pubmed publisher
    ..Property improvements were achieved by the replacement of the flexible n-diethylthio or the n-butyl moiety present in the leading inhibitors by heteroatom substituted heterocycloalkanes. ..
  37. Schoffelmeer A, Hogenboom F, Mulder A. Kappa1- and kappa2-opioid receptors mediating presynaptic inhibition of dopamine and acetylcholine release in rat neostriatum. Br J Pharmacol. 1997;122:520-4 pubmed
    ..As such, this study is the first to provide unequivocal in vitro evidence for the existence of functionally distinct kappa-opioid receptor subtypes in the brain...
  38. Fallone F, Britton S, Nieto L, Salles B, Muller C. ATR controls cellular adaptation to hypoxia through positive regulation of hypoxia-inducible factor 1 (HIF-1) expression. Oncogene. 2013;32:4387-96 pubmed publisher
    ..Our work offers new prospect for cancer therapy using ATR inhibitors with the potential to decrease cellular adaptation in hypoxic tumors. ..
  39. Picard M, Paradis L, Bégin P, Paradis J, Des Roches A. Skin testing only with penicillin G in children with a history of penicillin allergy. Ann Allergy Asthma Immunol. 2014;113:75-81 pubmed publisher
  40. Liu Z, Jin W, Dai Q, Chen X, Zhang H, Chi Z. Opioid activity of C8813, a novel and potent opioid analgesic. Life Sci. 2003;73:233-41 pubmed
    ..However, the inhibitory effect of C8813 in the rabbit vas deferens was very weak. These results indicated that C8813 was a potent analgesic and a high affinity agonist for the mu- and delta-opioid receptors...
  41. Xu H, Lu Y, Rice K, Ananthan S, Rothman R. SoRI 9409, a non-peptide opioid mu receptor agonist/delta receptor antagonist, fails to stimulate [35S]-GTP-gamma-S binding at cloned opioid receptors. Brain Res Bull. 2001;55:507-11 pubmed
    ..Viewed collectively, the in vitro data reported here predict that SoRI 9409 should be a mu antagonist in vivo, which is not observed. Resolving these discrepant findings will require additional research...
  42. Hammer M, Jonas W. Managing social conflict in complementary and alternative medicine research: the case of antineoplastons. Integr Cancer Ther. 2004;3:59-65 pubmed
    ..Yet contention around these substantive, "scientific" disagreements reflected conflict in attunement (trust, power, and affiliation) between Dr Burzynski and NCI. This article summarizes the findings from this case study...
  43. Wall P, Messier C. U-69,593 microinjection in the infralimbic cortex reduces anxiety and enhances spontaneous alternation memory in mice. Brain Res. 2000;856:259-80 pubmed
  44. Marinelli S, Connor M, Schnell S, Christie M, Wessendorf M, Vaughan C. delta-opioid receptor-mediated actions on rostral ventromedial medulla neurons. Neuroscience. 2005;132:239-44 pubmed
  45. Hussey H, Tisdale M. Effect of polyunsaturated fatty acids on the growth of murine colon adenocarcinomas in vitro and in vivo. Br J Cancer. 1994;70:6-10 pubmed
    ..These results suggest that PUFAs may play an important role in tumour growth and may offer a potential target for the development of chemotherapeutic agents...
  46. Margulis A, Houben E, Hallas J, Overbeek J, Pottegård A, Torp Pedersen T, et al. Ophthalmic nepafenac use in the Netherlands and Denmark. Acta Ophthalmol. 2017;95:509-517 pubmed publisher
    ..To describe nepafenac use in the Netherlands and Denmark with reference to its approved indications. For context, we also describe the use of ketorolac and diclofenac...
  47. Zanoli P, Baraldi M. Evidence that bremazocine prevents urine retention induced by intraspinal cord injection of colchicine in rats. J Auton Nerv Syst. 1990;30 Suppl:S191-3 pubmed
    ..The selective kappa-receptors agonist, U-69593, had little effect, while eledoisin or naloxone administration worsened rather than counteracted urine retention...
  48. Proffitt K, Madan B, Ke Z, Pendharkar V, Ding L, Lee M, et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 2013;73:502-7 pubmed publisher
    ..These results offer preclinical proof-of-concept that inhibiting mammalian Wnts can be achieved by targeting PORCN with small-molecule inhibitors such as C59, and that this is a safe and feasible strategy in vivo...
  49. Gu F, Zhang L, Teply B, Mann N, Wang A, Radovic Moreno A, et al. Precise engineering of targeted nanoparticles by using self-assembled biointegrated block copolymers. Proc Natl Acad Sci U S A. 2008;105:2586-91 pubmed publisher
    ..This approach may contribute to further development of targeted NPs as highly selective and effective therapeutic modalities...
  50. Hjelmstad G, Fields H. Kappa opioid receptor activation in the nucleus accumbens inhibits glutamate and GABA release through different mechanisms. J Neurophysiol. 2003;89:2389-95 pubmed
    ..These results indicate that KOP receptor activation inhibits GABA release by reducing Ca(2+) influx, but inhibits glutamate release at a step downstream of Ca(2+) entry...
  51. Wolf E, Braunstein A, Shih C, Braunstein R. Incidence of visually significant pseudophakic macular edema after uneventful phacoemulsification in patients treated with nepafenac. J Cataract Refract Surg. 2007;33:1546-9 pubmed
    ..1% suspension (Nevanac)...
  52. Bousquet P, Co Minh H, Arnoux B, Daures J, Demoly P. Importance of mixture of minor determinants and benzylpenicilloyl poly-L-lysine skin testing in the diagnosis of beta-lactam allergy. J Allergy Clin Immunol. 2005;115:1314-6 pubmed