Antiallodynic action of 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2- methyoxyphenyl)-4-piperidinol (NNC05-2090), a betaine/GABA transporter inhibitor

Journal of Pharmacological Sciences

Volumn 125, Issue 2, 2014, Pages 217-226

  Jinzenji, Ayako ^a   Sogawa, Chiharu ^a   Miyawaki, Takuya ^a   Wen, Xue Fang ^a   Yi, Dan ^a   Ohyama, Kazumi ^b   Kitayama, Shigeo ^a   Sogawa, Norio ^a   Morita, Katsuya ^c  

^a OKAYAMA UNIVERSITY   (Japan)

^b OKAYAMA UNIVERSITY   (Japan)

^c Kure University   (Japan)

Author keywords

Antiallodynic action; Betaine GABA transporter; Monoamine transporter; Neuropathic pain; NNC05 2090

Indexed keywords

1 (4,4 DIPHENYL 3 BUTENYL)NIPECOTIC ACID; 1 [2 [TRIS(4 METHOXYPHENYL)METHOXY]ETHYL] 3 PIPERIDINECARBOXYLIC ACID; 1 [2 [TRIS(4 METHOXYPHENYL)METHYL]ETHYL] 3 PIPERIDINECARBOXYLIC ACID; 1 [3 (9H CARBAZOL 9 YL) 1 PROPYL] 4 (2 METHOXYPHENYL) 4 PIPERIDINOL; 1 [3 (9H CARBAZOL 9 YL)PROPYL] 4 (2 METHOXYPHENYL) 4 PIPERIDINOL; ANALGESIC AGENT; ANALGESIC, ANTIINFLAMMATORY, ANTIRHEUMATIC AND ANTIGOUT AGENTS; BETAINE GABA TRANSPORTER 1 PROTEIN; CARRIER PROTEINS AND BINDING PROTEINS; DOPAMINE TRANSPORTER; NORADRENALIN TRANSPORTER; SEROTONIN TRANSPORTER; UNCLASSIFIED DRUG; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID CARRIER; BETAINE; NNC 05-2090; PIPERIDINE DERIVATIVE;

ALLODYNIA; ANALGESIC ACTIVITY; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHO CELL LINE; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; FORCED SWIM TEST; IC 50; INTRACELLULAR TRANSPORT; MALE; MOUSE; NEUROPATHIC PAIN; NONHUMAN; PROTEIN EXPRESSION; ANIMAL; ANTAGONISTS AND INHIBITORS; CRICETULUS; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; GENETICS; INBRED MOUSE STRAIN; METABOLISM; NEURALGIA; PHYSIOLOGY;

ANIMALS; BETAINE; CHO CELLS; CRICETULUS; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; GABA PLASMA MEMBRANE TRANSPORT PROTEINS; GAMMA-AMINOBUTYRIC ACID; MALE; MICE, INBRED STRAINS; NEURALGIA; PIPERIDINES;

EID: 84903981995     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.13146FP     Document Type: Article

References (49)

1. Courteix C, Eschalier A, Lavarenne J. Streptozotocin-induced diabetic rats: behavioural evidence for a model of chronic pain. Pain. 1993;543:81-88. (Pubitemid 23137271)
2. Elliott KJ. Taxonomy and mechanisms of neuropathic pain. Semin Neurol. 1994;14:195-205. (Pubitemid 24372103)
3. Woolf CJ, Doubell TP. The pathophysiology of chronic pain-increased sensitivity to low threshold A beta-fibre inputs. Curr Opin Neurobiol. 1994;4:523-534.
4. Calcut NA, Jorge MC, Yaksh TL, Chaplan SR. Tactile allodynia and formalin hyperalgesia in streptozotocin-diabetic rats: effects of insulin, aldose reductase inhibition and lidocaine. Pain. 1996;68:293-299. (Pubitemid 27025887)
5. Zimmermann M. Pathobiology of neuropathic pain. Eur J Pharmacol. 2001;429:23-37. (Pubitemid 33043979)
6. Cambell JN, Meyer RA. Mechanisms of neuropathic pain. Neuron. 2006;52:77-92. (Pubitemid 44466361)
7. Evans JE, Frosholm, Rotter A. Embryonic and postnatal expression of four gamma-aminobutyric acid transporter mRNAs in the mouse brain and leptomeninges. J Comp Neuronal. 1996;376:431-446. (Pubitemid 26419117)
8. Moore KA, Kohno T, Karchewski LA, Scholz J, Baba H, Woolf CJ. Partial peripheral nerve injury promotes a selective loss of GABAergic inhibition in the superficial dorsal horn of the spinal ford. J Neurosci. 2002;22:6724-6731. (Pubitemid 35386428)
9. Iversen LL. Role of transmitter uptake mechanisms in synaptic neurotransmission. Br J Pharmacol. 1971;41:571-591.
10. Gether U, Peter HA, Larsson OM, Shousboe A. Neurotransmitter transporters: molecular function of important drug targets. Trends Pharmacol Sci. 2006;27:375-383. (Pubitemid 43977787)
11. Bröer S, Gether U. The solute carrier 6 family of transporters. British J Pharmacol. 2012;167:256-278.
12. Guastella J, Nelson N, Nelson H, Czyzyk L, Keynan S, Miedel MC, et al. Cloning and expression of a rat brain GABA transporter. Science. 1990;249:13032306.
13. Borden LA, Smith KE, Harting PR, Bramchek TA, Weinshank RL. Molecular heterogeneity of the gamma-aminobutyric acid (GABA) transport system. Cloning of two novel high affinity GABA transporters from rat brain. J Biol Chem. 1992;267:21098-21104.
14. Liu QR, Lopez-Corcuera B, Mandiyan S, Nelson H, Nelson N. Molecular characterization of four pharmacologically distinct γ-aminobutyric acid transporters in mouse brain. J Biol Chem. 1993;268:2106-2112. (Pubitemid 23033620)
15. Dalby NO. Inhibition of g-aminobutyric acid uptake: Anatomy, physiology and effects against epileptic seizures. Eur J Pharmacol. 2003;479:127-137. (Pubitemid 37377882)
16. Madsen KK, White HS, Schousboe A. Neuronal and non-neuronal GABA transporters as targets for antiepileptic drugs. Pharmacol Ther. 2010;125:394-401.
17. Durkin MM, Smith KE, Borden LA, Weinshank RL, Branchek TA, Gustafson EL. Localization of messenger RNAs encoding three GABA transporters in rat brain: an in situ hybridization study. Brain Res Mol Brain Res. 1995;33:7-21.
18. Borden LA. GABA transporter heterogeneity: Pharmacology and cellular localization. Neurochem Int. 1996;29:335-356. (Pubitemid 26297678)
19. Conti F, Melone M, DeBiasi S, Minelli A, Brecha NC, Ducati A. Neuronal and glial localization of GAT-1, a high-affinity gamma-aminobutyric acid plasma membrane transporter, in human cerebral cortex: with a note on its distribution in monkey cortex. J Comp Neurol. 1998;396:51-63. (Pubitemid 28242451)
20. Minelli A, DeBiase S, Brecha N, Zuccarello LV, Conti F. GAT-3, a high affinity GABA plasma membrane transporter, is localized to astrocytic processes, and it is not confined to the vicinity of GABAergic synapses in the cerebral cortex. J Neurosci. 1996;16:6255-6264. (Pubitemid 26313999)
21. Conti F, Zuccarello LV, Barbaresi P, Minelli A, Brecha NC, Melone M. Neuronal, glial and epithelial localization of gamma-aminobutyric acid transporter 2, a high-affinity gamma-aminobutyric acid plasma membrane transporter, in the cerebral cortex and neighboring structures. J Comp Neurol. 1999;109:482-494. (Pubitemid 29262257)
22. Lopez-Corcuera B, Liu QR, Mandiyan S, Nelson H, Nelson N. Expression of a mouse brain cDNA encoding novel gamma-aminobutyric acid transporter. J Biol Chem. 1992;267:17491-17493.
23. Borden LA, Smith KE, Gustafson EL, Branchek TA, Weinshank RL. Cloning and expression of a betaine/GABA transporter from human brain. J Neurochem. 1995;64:977-984.
24. Zhu XM, Ong WY. A light and electron microscopic study of betaine/GABA transporter distribution in the monkey cerebral neocortex and hippocampus. J Neurocytol. 2004;33:233-240.
25. Schousboe A, Larsson OM, Sarup A, White, HS. Role of the betaine/GABA transporter (BGT-1/GAT2) for the control of epilepsy. Eur J Pharmacol. 2004;500:281-287. (Pubitemid 39304015)
26. --dependent betaine transporter that is regulated by hypertonicity. J Biol Chem. 1992;267:649-652.
27. Seltzer Z, Dubner R, Shir Y. A novel behavioral model of neuropathic pain disorders produced in rats by partial sciatic nerve injury. Pain. 1990;43:205-218. (Pubitemid 20385185)
28. Malmberg AB, Basbaum AI. Partial sciatic nerve injury in the mouse as a model of neuropathic pain: Behavioral and neuro-anatomical correlates. Pain. 1998;76:215-222. (Pubitemid 28304959)
29. Morita K, Monotyama N, Kitayama T, Morioka N, Kifune K, Dohi T. Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice. J Pharmacol Exp Ther. 2006;326:633-645.
30. 2α in conscious mice. Pain. 1995;61:285-290.
31. Hylden JL, Wilcox GL. Intrathecal morphine in mice: a new technique. Eur J Pharmacol. 1980;67:313-316. (Pubitemid 10007057)
32. Honda K, Harada A, Takano Y, Kamiya H. Involvement of M3 muscarinic receptors of the spinal cord in formalin-induced nociception in mice. Brain Res. 2000;859:38-44. (Pubitemid 30138191)
33. Sogawa CA, Sogawa N, Yamamoto T, Oda N, Inoue T, Onodera K, et al. Localization of metallothionein (MT and expression of MT isoforms induced by cadmium in rat dental pulp. Jpn J Pharmacol. 2001;86:65-72.
34. Sogawa C, Mitsuhata C, Kumagai-Morioka K, Sogawa N, Ohyama K, Morita K, et al. Expression and function of variants of human catecholamine transporters lacking the fifth transmembrane region encoded by exon 6. PLos One. 2010;5:e11945.
35. Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T. Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn-Schmiedeberg's Arch Pharmacol. 2000;361:214-220. (Pubitemid 30062455)
36. Sogawa C, Sogawa N, Tagawa J, Fujino A, Ohyama K, Asanuma M, et al. 5-Methoxy-N,N-diisopropyltryptamine (Foxy), a selective and high affinity inhibitor of serotonin transporter. Toxicol Lett. 1997;170:75-82.
37. Sogawa C, Sogawa N, Ohyama K, Kkura-Hanajiri R, Goda Y, Sora I, et al. Methylone and monoamine transporters: correlation with toxicity. Curr Neuropharmacol. 2011;9:58-62.
38. Gerile, Sogawa C, Ohyama K, Masuko T, Kusama T, Morita K, et al. Inhibitory action of antidepressants on mouse betaine/GABA transporter (BGT1) heterologously expressed in cell cultures. Int J Mol Sci. 2012;13:2578-2589.
39. Kitayama S, Shimada S, Xu H, Markham L, Donovan MD, Uhl GR. Dopamine transporter site-directed mutations differentially alter substrate transport and cocaine binding. Proc Natl Acad Sci U S A. 1992;89:7782-7785.
40. Sugimura M, Kitayama S, Morita K, Irifune M, Takarada T, Kawahara M, Dohi T. Effects of volatile and intravenous anesthetics on the uptake of GABA, glutamate and dopamine by their transporters heterologously expressed in COS cells and in rat brain synaptosomes. Toxicol Lett. 2001;123:69-76. (Pubitemid 32763090)
41. Porsolt RD, Bertin A, Jalfre M. Behavioural despair in mice: a primary screening test for antidepressants. Arch int Pharmacodyn. 1997;229:327-336.
42. Thomsen C, Sørensen PO, Egebjerg J. 1-(3-(9H-Carbazol-9-yl)-1- propyl)-4-(2-methyoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA transporter. Br. J. Pharmacol. 1997;120:983-985. (Pubitemid 27122632)
43. Dalby NO, Thomsen C, Fink-Jensen A, Lundbeck J, Søkilde B, Man CM, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 1997;28:51-61. (Pubitemid 27306794)
44. Li Y, Li Y, Gu P, Fu B. Liu F, Li E. Analgesic effect of intrathecally g-aminobutyric acid transporter-1 inhibitor NO-711 administrating on neuropathic pain in rats. Neurosci Lett. 2011;494:6-9.
45. Lehre AC, Rowley NM, Zhou Y, Holmseth C, Guo C, Holen T, et al. Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice. Epilepsy Res. 2011;95:70-81.
46. Langer ZS, Schoemaker H. Effects of antidepressants on monoamine transporters. Prog Neuropsychopharmacol Biol Psychiat. 1988;12:193-216.
47. Todd AJ. Neuronal circuitry for pain processing in the dorsal horn. Nature Rev Neurosci. 2010;11:823-836.
48. Sansone RA, Sansone LA. Antidepressants and pain management. Psychiatry. 2008;5:16-19.
49. Ikeda T, Ishida Y, Naono R, Takeda R, Abe H, Nakamura T, et al. Effects of intrathecal administration of newer antidepressants on mechanical allodynia in rat models of neuropathic pain. Neurosci Res. 2009;63:42-46.