membrane transport modulators



Top Publications

  1. Ringstad N, Horvitz H. FMRFamide neuropeptides and acetylcholine synergistically inhibit egg-laying by C. elegans. Nat Neurosci. 2008;11:1168-76 pubmed publisher
    ..elegans hermaphrodite is therefore under the control of a presumptive sensory system and is inhibited by the convergence of signals from neuropeptides and the small-molecule neurotransmitter acetylcholine. ..
  2. Mani B, O Dowd J, Kumar L, Brueggemann L, Ross M, Byron K. Vascular KCNQ (Kv7) potassium channels as common signaling intermediates and therapeutic targets in cerebral vasospasm. J Cardiovasc Pharmacol. 2013;61:51-62 pubmed publisher
    ..In conclusion, we identify Kv7 channels as common targets of vasoconstrictor spasmogens and as candidates for therapeutic intervention for cerebral vasospasm...
  3. Jepps T, Olesen S, Greenwood I. One man's side effect is another man's therapeutic opportunity: targeting Kv7 channels in smooth muscle disorders. Br J Pharmacol. 2013;168:19-27 pubmed publisher
    ..This review discusses the potential of targeting Kv7 channels in the smooth muscle to treat diseases such as hypertension, bladder instability, constipation and preterm labour...
  4. Orhan G, Wuttke T, Nies A, Schwab M, Lerche H. Retigabine/Ezogabine, a KCNQ/K(V)7 channel opener: pharmacological and clinical data. Expert Opin Pharmacother. 2012;13:1807-16 pubmed publisher
    ..Retigabine/Ezogabine (RTG) is a third-generation antiepileptic drug (AED) with a novel mechanism of action. It enhances the activity of voltage-gated K(V)7 potassium channels...
  5. Liu Y, Zhang H, Li X, Wang Y, Lu H, Qi X, et al. Inhibition of voltage-gated channel currents in rat auditory cortex neurons by salicylate. Neuropharmacology. 2007;53:870-80 pubmed
  6. Srinivas N. Is there a place for drug combination strategies using clinical pharmacology attributes?--review of current trends in research. Curr Clin Pharmacol. 2009;4:220-8 pubmed
    ..In summary, based on the collated information, a pragmatic approach would render feasibility for a balanced therapy management using combined clinical pharmacology attributes of drugs. ..
  7. Perret D, Luo Z. Targeting voltage-gated calcium channels for neuropathic pain management. Neurotherapeutics. 2009;6:679-92 pubmed publisher
  8. Prasad U, Gray D, Purcell H. Review of the If selective channel inhibitor ivabradine in the treatment of chronic stable angina. Adv Ther. 2009;26:127-37 pubmed publisher
    ..This review provides an insight into this new agent, its historical background, mechanism of action, and pathophysiologic basis, and provides up-to-date evidence-based information on its optimum use in stable angina. ..
  9. Potschka H. Targeting regulation of ABC efflux transporters in brain diseases: a novel therapeutic approach. Pharmacol Ther. 2010;125:118-27 pubmed publisher

More Information


  1. Kobayashi S, Hattori M, Elekes K, Ito E, Matsuo R. FMRFamide regulates oscillatory activity of the olfactory center in the slug. Eur J Neurosci. 2010;32:1180-92 pubmed publisher
  2. Doherty T, Seddighi M. Local anesthetics as pain therapy in horses. Vet Clin North Am Equine Pract. 2010;26:533-49 pubmed publisher
    ..The available studies of systemically administered lidocaine in horses provide evidence for the analgesic and anesthetic effects of intravenous lidocaine in this species. ..
  3. Namkung W, Phuan P, Verkman A. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011;286:2365-74 pubmed publisher
    ..The small molecule inhibitors identified here permit pharmacological dissection of TMEM16A/CaCC function and are potential development candidates for drug therapy of hypertension, pain, diarrhea, and excessive mucus production. ..
  4. Baastrup C, Finnerup N. Pharmacological management of neuropathic pain following spinal cord injury. CNS Drugs. 2008;22:455-75 pubmed
    ..Cannabinoids have been found to relieve other types of central pain, and serotonin noradrenaline reuptake inhibitors as well as opioids relieve peripheral neuropathic pain and may be used to treat patients with SCI pain. ..
  5. Gavva N, Davis C, Lehto S, Rao S, Wang W, Zhu D. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol Pain. 2012;8:36 pubmed publisher
    ..Further, a reduction of magnitude in Tb decrease after repeated dosing of an antagonist suggests that TRPM8's role in Tb maintenance may not pose an issue for developing TRPM8 antagonists as therapeutics. ..
  6. Beéry E, Rajnai Z, Abonyi T, Makai I, Bánsághi S, Erdo F, et al. ABCG2 modulates chlorothiazide permeability--in vitro-characterization of its interactions. Drug Metab Pharmacokinet. 2012;27:349-53 pubmed
    ..1 respectively. Inhibition of ABCG2 in Caco-2 cells reduced the efflux ratio to 1.4, suggesting that ABCG2 plays a role in limiting chlorothiazide bioavailability in humans. ..
  7. Runyon S, Burgess J, Abraham P, Keverline Frantz K, Flippen Anderson J, Deschamps J, et al. Synthesis, structural identification, and ligand binding of tropane ring analogs of paroxetine and an unexpected aza-bicyclo[3.2.2]nonane rearrangement product. Bioorg Med Chem. 2005;13:2439-49 pubmed
    ..2.2]nonane derivative 10a. ..
  8. Zucker M, Weizman A, Rehavi M. Repeated swim stress leads to down-regulation of vesicular monoamine transporter 2 in rat brain nucleus accumbens and striatum. Eur Neuropsychopharmacol. 2005;15:199-201 pubmed
    ..001). The down-regulation of VMAT2 in this dopaminergic regions may serve as an adaptatory mechanism in the response to prolonged stress, and may be relevant to chronic stress-induced depression. ..
  9. Li J, Gong Y, Li C, Lu Y, Liu Y, Shao Y. Long-term efficacy and safety of sodium-glucose cotransporter-2 inhibitors as add-on to metformin treatment in the management of type 2 diabetes mellitus: A meta-analysis. Medicine (Baltimore). 2017;96:e7201 pubmed publisher
  10. Ma Y, Rees D, Gibson J, Ellory J. The conductance of red blood cells from sickle cell patients: ion selectivity and inhibitors. J Physiol. 2012;590:2095-105 pubmed publisher
    ..The ability to record P(sickle)-like activity in single RBCs will facilitate further studies and eventual molecular identification of the pathway involved. ..
  11. Sones W, Davis A, Leblanc N, Greenwood I. Cholesterol depletion alters amplitude and pharmacology of vascular calcium-activated chloride channels. Cardiovasc Res. 2010;87:476-84 pubmed publisher
  12. Jones D, Lau S, Monks T. Thioether metabolites of 3,4-methylenedioxyamphetamine and 3,4-methylenedioxymethamphetamine inhibit human serotonin transporter (hSERT) function and simultaneously stimulate dopamine uptake into hSERT-expressing SK-N-MC cells. J Pharmacol Exp Ther. 2004;311:298-306 pubmed
  13. Qin X, Yue Z, Sun B, Yang W, Xie J, Ni E, et al. Sphingosine and FTY720 are potent inhibitors of the transient receptor potential melastatin 7 (TRPM7) channels. Br J Pharmacol. 2013;168:1294-312 pubmed publisher
    ..Moreover, we also tested the effects of the structural analogues of SPH, N,N-dimethyl-D-erythro-sphingosine (DMS), ceramides and FTY720 on TRPM7...
  14. Chen H, Zhao L, Chu G, Kito G, Yamauchi N, Shigeyoshi Y, et al. FSH induces the development of circadian clockwork in rat granulosa cells via a gap junction protein Cx43-dependent pathway. Am J Physiol Endocrinol Metab. 2013;304:E566-75 pubmed publisher
    ..In addition, both lindane and CBX induced a clear phase-delay shift of Per2 oscillations. These findings suggest that FSH induces the development of the clock system by increasing the expression of Cx43. ..
  15. Charntikov S, Swalve N, Pittenger S, Fink K, Schepers S, Hadlock G, et al. Iptakalim attenuates self-administration and acquired goal-tracking behavior controlled by nicotine. Neuropharmacology. 2013;75:138-44 pubmed publisher
    ..Together, these finding support the notion that iptakalim may be an effective pharmacotherapy for increasing smoking cessation and a better understanding of its action could contribute to medication development. ..
  16. Volkow N, Wang G, Fowler J, Telang F, Maynard L, Logan J, et al. Evidence that methylphenidate enhances the saliency of a mathematical task by increasing dopamine in the human brain. Am J Psychiatry. 2004;161:1173-80 pubmed
    ..These findings support educational strategies that make schoolwork more interesting as nonpharmacological interventions to treat ADHD. ..
  17. Tahara E, Navarete F, Kowaltowski A. Tissue-, substrate-, and site-specific characteristics of mitochondrial reactive oxygen species generation. Free Radic Biol Med. 2009;46:1283-97 pubmed publisher
    ..Altogether, our data uncover and quantify many tissue-, substrate-, and site-specific characteristics of mitochondrial ROS release. ..
  18. Bourin M, Chenu F, Hascoet M. Topiramate and phenytoin anti-immobility effect in the mice forced swimming test is reversed by veratrine: Implication for bipolar depression treatment. Behav Brain Res. 2009;205:421-5 pubmed publisher
    ..The antidepressant-like effect of the anticonvulsants was completely reversed by veratrine suggesting that the antidepressant-like effect of topiramate and phenytoin on the FST might be due to their Na(+) channels blocking properties. ..
  19. Sonobe T, Inagaki T, Poole D, Kano Y. Intracellular calcium accumulation following eccentric contractions in rat skeletal muscle in vivo: role of stretch-activated channels. Am J Physiol Regul Integr Comp Physiol. 2008;294:R1329-37 pubmed publisher
    ..In conclusion, in vivo quantitative analyses demonstrated that ECC contractions elevate [Ca2+]i significantly more than ISO contractions and that stretch-activated channels may play a permissive role in this response. ..
  20. Fike C, Sidoryk Wegrzynowicz M, Aschner M, Summar M, Prince L, Cunningham G, et al. Prolonged hypoxia augments L-citrulline transport by system A in the newborn piglet pulmonary circulation. Cardiovasc Res. 2012;95:375-84 pubmed publisher
  21. Collier Z, Gust K, Gonzalez Morales B, Gong P, Wilbanks M, Linkov I, et al. A weight of evidence assessment approach for adverse outcome pathways. Regul Toxicol Pharmacol. 2016;75:46-57 pubmed publisher
  22. Katz P, Leiter L. The Role of the Kidney and SGLT2 Inhibitors in Type 2 Diabetes. Can J Diabetes. 2015;39 Suppl 5:S167-75 pubmed publisher
    ..Long-term safety data and results of ongoing cardiovascular outcome studies are awaited so we can fully understand the role that SGLT2 inhibitors will play in the comprehensive management of type 2 diabetes. ..
  23. Jansen G, van der Heijden J, Oerlemans R, Lems W, Ifergan I, Scheper R, et al. Sulfasalazine is a potent inhibitor of the reduced folate carrier: implications for combination therapies with methotrexate in rheumatoid arthritis. Arthritis Rheum. 2004;50:2130-9 pubmed
    ..Thus, when considering use of these drugs in combination therapies, the present results provide a rationale both for the use of folate supplementation and for spacing administration of these drugs over time. ..
  24. Orth P, Hesketh J, Mak C, Yang Y, Lin S, Beatch G, et al. RSD1235 blocks late INa and suppresses early afterdepolarizations and torsades de pointes induced by class III agents. Cardiovasc Res. 2006;70:486-96 pubmed
    ..We suggest that these protective actions of RSD1235 may result, at least in part, from its ability to inhibit late I(Na) during action potential repolarization. ..
  25. Marusalin J, Matier B, Rheault M, Donini A. Aquaporin homologs and water transport in the anal papillae of the larval mosquito, Aedes aegypti. J Comp Physiol B. 2012;182:1047-56 pubmed publisher
    ..Together, the results suggest that AQP(s) could be responsible for facilitating water transport at the papillae epithelium...
  26. Ma L, Wei Y, Zhou Y, Ma X, Wu X. Effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin in rats. Arch Pharm Res. 2011;34:1939-43 pubmed publisher
    ..Therefore, excipient selection is an important factor to consider in rational formulation design. ..
  27. Nishimura T, Sai Y, Fujii J, Muta M, Iizasa H, Tomi M, et al. Roles of TauT and system A in cytoprotection of rat syncytiotrophoblast cell line exposed to hypertonic stress. Placenta. 2010;31:1003-9 pubmed publisher
    ..MeAIB, a system A specific substrate, inhibited hypertonic stress-induced [(14)C]betaine uptake. These results suggest that TauT and system A play cytoprotective roles in syncytiotrophoblasts exposed to hypertonic stress. ..
  28. Raghu K, Yadav G, Singh R, Prathapan A, Sharma S, Bhadauria S. Evaluation of adverse cardiac effects induced by arsenic trioxide, a potent anti-APL drug. J Environ Pathol Toxicol Oncol. 2009;28:241-52 pubmed
    ..Our results also indicate that the status of the body's main electrolyte content (such as magnesium and potassium) is also an influencing factor on the magnitude of toxicity of arsenic trioxide. ..
  29. Masamoto Y, Kawabata F, Fushiki T. Intragastric administration of TRPV1, TRPV3, TRPM8, and TRPA1 agonists modulates autonomic thermoregulation in different manners in mice. Biosci Biotechnol Biochem. 2009;73:1021-7 pubmed
    ..Our findings suggest the possibility that each thermoTRP is a key sensor inducing reasonable autonomic thermoregulation according to its own activated temperature range. ..
  30. Vale C, Nicolaou K, Frederick M, Vieytes M, Botana L. Cell volume decrease as a link between azaspiracid-induced cytotoxicity and c-Jun-N-terminal kinase activation in cultured neurons. Toxicol Sci. 2010;113:158-68 pubmed publisher
    ..The results presented here indicate that the JNK activation induced by AZA-1 is secondary to the decrease in cellular volume elicited by the toxin. ..
  31. Kopec K, Jones B, Thomas J, Spais C, McKenna B, Saville L, et al. Successful identification of glycine transporter inhibitors using an adaptation of a functional cell-based assay. J Biomol Screen. 2009;14:1185-94 pubmed publisher
    ..The screening campaign identified 300 small molecules as selective GlyT1 inhibitors for lead optimization, demonstrating the utility of this cost-effective method. ..
  32. Sasaki H, Toyomura K, Matsuzaki W, Okamoto A, Yamaguchi N, Nakamura H, et al. Regulation of alkaline ceramidase activity by the c-Src-mediated pathway. Arch Biochem Biophys. 2014;550-551:12-9 pubmed publisher
    ..Serum starvation increased both ceramidase activity at pH 8.8 and expression of ACER2. Our data suggest that c-Src-mediated signal positively regulates ACER activity in a Ca(2+)-independent manner. ..
  33. Zwierzyńska E, Pietrzak B. [Retigabine - a new antiepileptic drug with a different mechanism of action]. Postepy Hig Med Dosw (Online). 2013;67:973-81 pubmed publisher
    ..The efficacy of retigabine is being tested in other types of seizures and disorders characterized by neuronal hyperexcitability. Neuroprotective activity of retigabine is also being researched. ..
  34. Watkins W, Lemoine R, Chong L, Cho A, Renau T, Kuo B, et al. Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives. Bioorg Med Chem Lett. 2004;14:5133-7 pubmed
  35. Martínez François J, Lu Z. Intrinsic versus extrinsic voltage sensitivity of blocker interaction with an ion channel pore. J Gen Physiol. 2010;135:149-67 pubmed publisher
  36. Koschinski A, Wengler G, Wengler G, Repp H. Rare earth ions block the ion pores generated by the class II fusion proteins of alphaviruses and allow analysis of the biological functions of these pores. J Gen Virol. 2005;86:3311-20 pubmed
  37. Lv P, Kim H, Lee J, Sihn C, Fathabad Gharaie S, Mousavi Nik A, et al. Genetic, cellular, and functional evidence for Ca2+ inflow through Cav1.2 and Cav1.3 channels in murine spiral ganglion neurons. J Neurosci. 2014;34:7383-93 pubmed publisher
    ..2 currents in neurons. Finally, using shRNA gene knockdown methodology, and histological analyses of SGNs from Cav1.2(+/-) and Cav1.3(+/-) mice, we were able to establish the differential roles of Cav1.2 and Cav1.3 in SGNs. ..
  38. Gajula P, Sharma S, Ampapathi R, Chakraborty T. Total synthesis of (29S,37S)-isomer of malevamide E, a potent ion-channel inhibitor. Org Biomol Chem. 2013;11:257-60 pubmed publisher
    ..The strategy developed herein is amenable for the synthesis of the other possible isomers in search for the correct stereoisomer of the naturally occurring molecule. ..
  39. Tabata K, Matsunaga K, Sakane A, Sasaki T, Noda T, Yoshimori T. Rubicon and PLEKHM1 negatively regulate the endocytic/autophagic pathway via a novel Rab7-binding domain. Mol Biol Cell. 2010;21:4162-72 pubmed publisher
    ..Furthermore, we show that Rubicon but not PLEKHM1 uniquely regulates membrane trafficking via simultaneously binding both Rab7 and PI3-kinase. ..
  40. Brugnara C, De Franceschi L. [Clinical trials of new therapeutic pharmacology for sickle cell disease]. Sante. 2006;16:263-8 pubmed
    ..It prevents the activation of leucocytes, platelets and endothelial cells in patients with sickle cell disease and vascular remodelling. The L-arginine, the NO precursor, provides could be beneficial in sickle cell patients. ..
  41. Cerruto M, Asimakopoulos A, Artibani W, Del Popolo G, La Martina M, Carone R, et al. Insight into new potential targets for the treatment of overactive bladder and detrusor overactivity. Urol Int. 2012;89:1-8 pubmed publisher
    ..Targeting afferent pathways and/or bladder smooth muscles by modulating activity of ligand receptors and ion channels could be effective to suppress OAB. ..
  42. Rech J, Eckert W, Maher M, Banke T, Bhattacharya A, Wickenden A. Recent advances in the biology and medicinal chemistry of TRPA1. Future Med Chem. 2010;2:843-58 pubmed publisher
    ..In addition, we provide an update on TRPA1 medicinal chemistry and the progress in the search for novel TRPA1 antagonists. ..
  43. Jabr Milane L, van Vlerken L, Yadav S, Amiji M. Multi-functional nanocarriers to overcome tumor drug resistance. Cancer Treat Rev. 2008;34:592-602 pubmed publisher
    ..In preclinical studies, the use of multi-functional nanocarriers has shown significant promise in enhancing cancer therapy, especially against MDR tumors. ..
  44. Lodge N, Li Y. Ion channels as potential targets for the treatment of depression. Curr Opin Drug Discov Devel. 2008;11:633-41 pubmed
    ..The therapeutic utility of some ion channels will be limited by their role in multiple physiological or pathophysiological processes. Nevertheless, a number of strategies are being employed to provide improved specificity of action. ..
  45. Cohen Kfir E, Lee W, Eskandari S, Nelson N. Zinc inhibition of gamma-aminobutyric acid transporter 4 (GAT4) reveals a link between excitatory and inhibitory neurotransmission. Proc Natl Acad Sci U S A. 2005;102:6154-9 pubmed
    ..Therefore, this mode of zinc function signifies a link between excitatory and inhibitory neurotransmission and may play a neuroprotective role against glutamate-induced excitotoxicity. ..
  46. Smeets P, van Aubel R, Wouterse A, van den Heuvel J, Russel F. Contribution of multidrug resistance protein 2 (MRP2/ABCC2) to the renal excretion of p-aminohippurate (PAH) and identification of MRP4 (ABCC4) as a novel PAH transporter. J Am Soc Nephrol. 2004;15:2828-35 pubmed
    ..MRP4 is a novel PAH transporter that has higher affinity for PAH and is expressed more highly in kidney than MRP2, and may therefore be more important in renal PAH excretion. ..
  47. Mula M. Emerging drugs for focal epilepsy. Expert Opin Emerg Drugs. 2013;18:87-95 pubmed publisher
    ..Finally, new formulations, especially those adopting drug targeting technologies are promising in order to maximize the efficacy with very limited adverse effects. ..
  48. Oh S, Park J, Han S, Lee J, Roh E, Lee C. Development of selective blockers for Ca²(+)-activated Cl channel using Xenopus laevis oocytes with an improved drug screening strategy. Mol Brain. 2008;1:14 pubmed publisher
    ..Our results provide an optimal drug screening strategy suitable for high throughput screening, and propose N-(4-trifluoromethylphenyl)anthranilic acid as an improved CaCC blocker. ..
  49. Nörenberg W, Schunk J, Fischer W, Sobottka H, Riedel T, Oliveira J, et al. Electrophysiological classification of P2X7 receptors in rat cultured neocortical astroglia. Br J Pharmacol. 2010;160:1941-52 pubmed publisher
    ..Rat cultured cortical astroglia possesses functional P2X7 receptors. It is suggested that astrocytic P2X7 receptors respond to high local ATP concentrations during neuronal injury. ..
  50. Sampson L, Davies L, Barrett Jolley R, Standen N, Dart C. Angiotensin II-activated protein kinase C targets caveolae to inhibit aortic ATP-sensitive potassium channels. Cardiovasc Res. 2007;76:61-70 pubmed
    ..This translocation allows PKCepsilon access to K(ATP) channels compartmentalized within these specialized membrane microdomains and highlights a potential role for caveolae in targeting PKC isozymes to an ion channel effector. ..
  51. von der Weid P, Rahman M, Imtiaz M, van Helden D. Spontaneous transient depolarizations in lymphatic vessels of the guinea pig mesentery: pharmacology and implication for spontaneous contractility. Am J Physiol Heart Circ Physiol. 2008;295:H1989-2000 pubmed publisher
    ..The abolition of spontaneous APs by blockers of other excitatory ion channels suggests a contribution of these conductances to lymphatic pacemaking. ..
  52. Almaraz L, Manenschijn J, De La Pena E, Viana F. TRPM8. Handb Exp Pharmacol. 2014;222:547-79 pubmed publisher
    ..Finally, we examine the physiological role of TRPM8 and its emerging link to various human diseases, including pain, prostate cancer, dry eye disease, and metabolic disorders. ..
  53. Upadya M, Shrestha A, Kishen A. Role of efflux pump inhibitors on the antibiofilm efficacy of calcium hydroxide, chitosan nanoparticles, and light-activated disinfection. J Endod. 2011;37:1422-6 pubmed publisher
    ..The effect of EPI was more significant with LAD, when compared with Ca(OH)(2) and chitosan nanoparticles. This study highlighted the role of biofilm matrix in providing resistance to antimicrobials. ..