Neuropharmacological profile of l-pGlu-(1-benzyl)-l-His-l-ProNH2, a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters

Epilepsy Research

Volumn 87, Issue 2-3, 2009, Pages 223-233

  Rajput, Satyendra Kumar ^a   Singh, Jitendra Narain ^a   Ingole, Shubhada ^a   Jain, Gaurav ^a   Kaur, Navneet ^a   Monga, Vikramdeep ^a   Meena, Chhuttan Lal ^a   Jain, Rahul ^a   Sharma, Shyam Sunder ^a  

^a NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH NIPER   (India)

Author keywords

Cardiovascular system; Cerebral blood flow; DRG neurons; Functional observation battery; Seizure; Sodium current

Indexed keywords

GLUTAMIC ACID(1BENZYL)HISTIDYLPROLINAMIDE; KAINIC ACID; NP 355; PENTETRAZOLE; PICROTOXIN; PROTIRELIN; PROTIRELIN DERIVATIVE; SODIUM CHLORIDE; SODIUM ION; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICONVULSANT ACTIVITY; ARTICLE; BEHAVIOR; BRAIN BLOOD FLOW; CONTROLLED STUDY; CONVULSION; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTRIC SHOCK; MALE; MEAN ARTERIAL PRESSURE; MOUSE; NEUROPROTECTION; NEWBORN; NONHUMAN; PRIORITY JOURNAL; RAT; SEIZURE; SODIUM CURRENT;

ANALYSIS OF VARIANCE; ANIMALS; ANTICONVULSANTS; BEHAVIOR, ANIMAL; BLOOD PRESSURE; BRAIN; CEREBROVASCULAR CIRCULATION; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROPHYSIOLOGY; ELECTROSHOCK; GANGLIA, SPINAL; KAINIC ACID; MALE; MICE; MOTOR ACTIVITY; NEURONS; PENTYLENETETRAZOLE; PICROTOXIN; RATS; RATS, SPRAGUE-DAWLEY; SEIZURES; STATISTICS, NONPARAMETRIC; THYROTROPIN-RELEASING HORMONE;

EID: 70450221677     PISSN: 09201211     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.eplepsyres.2009.09.007     Document Type: Article

References (55)

1. Amabeoku G.J. Gamma-aminobutyric acid and glutamic acid receptors may mediate theophylline-induced seizures in mice. Gen. Pharmacol. 32 (1999) 365-372
2. Cao J., O'Donnell D., Vu H., Payza K., Pou C., Godbout C., Jakob A., Pelletier M., Lembo P., Ahmad S., and Walker P. Cloning and characterization of a cDNA encoding a novel subtype of rat thyrotropin-releasing hormone receptor. J. Biol. Chem. 273 (1998) 32281-32287
3. Chavko M., Braisted J.C., Outsa N.J., and Harabin A.L. Role of cerebral blood flow in seizures from hyperbaric oxygen exposure. Brain Res. 791 (1998) 75-82
4. Czapinski P., Blaszczyk B., and Czuczwar S.J. Mechanisms of action of antiepileptic drugs. Curr. Top. Med. Chem. 5 (2005) 3-14
5. Das Gupta S., Deshpande S.B., and Warnick J.E. Segmental synaptic depression caused by diisopropylphosphorofluoridate and sarin is reversed by thyrotropin-releasing hormone in the neonatal rat spinal cord. Toxicol. Appl. Pharmacol. 95 (1988) 499-506
6. de Gortari P., Uribe R.M., Garcia-Vazquez A., Aguilar-Valles A., Martinez A., Valdes A., Charli J.L., Fernandez-Guardiola A., and Joseph-Bravo P. Amygdala kindling differentially regulates the expression of the elements involved in TRH transmission. Neurochem. Int. 48 (2006) 31-42
7. Dekin M.S., Richerson G.B., and Getting P.A. Thyrotropin-releasing hormone induces rhythmic bursting in neurons of the nucleus tractus solitarius. Science 229 (1985) 67-69
8. Deng P.Y., Porter J.E., Shin H.S., and Lei S. Thyrotropin-releasing hormone increases GABA release in rat hippocampus. J. Physiol. 577 (2006) 497-511
9. Deshpande S.B., Pilotte N.S., and Warnick J.E. Gender-specific action of thyrotropin-releasing hormone in the mammalian spinal cord. Faseb J. 1 (1987) 478-482
10. Dubinsky J.M., and Oxford G.S. Dual modulation of K channels by thyrotropin-releasing hormone in clonal pituitary cells. Proc. Natl. Acad. Sci. U.S.A. 82 (1985) 4282-4286
11. Engel S., Neumann S., Kaur N., Monga V., Jain R., Northup J., and Gershengorn M.C. Low affinity analogs of thyrotropin-releasing hormone are super-agonists. J. Biol. Chem. 281 (2006) 13103-13109
12. Gary K.A., Sevarino K.A., Yarbrough G.G., Prange Jr. A.J., and Winokur A. The thyrotropin-releasing hormone (TRH) hypothesis of homeostatic regulation: implications for TRH-based therapeutics. J. Pharmacol. Exp. Ther. 305 (2003) 410-416
13. Griffiths E.C., Kelly J.A., Ashcroft A., Ward D.J., and Robson B. Comparative metabolism and conformation of TRH and its analogues. Ann. N. Y. Acad. Sci. 553 (1989) 217-231
14. Heuer H., Schafer M.K., O'Donnell D., Walker P., and Bauer K. Expression of thyrotropin-releasing hormone receptor 2 (TRH-R2) in the central nervous system of rats. J. Comp. Neurol. 428 (2000) 319-336
15. Hori T., Yamasaki M., Asami T., Koga H., and Kiyohara T. Responses of anterior hypothalamic-preoptic thermosensitive neurons to thyrotropin releasing hormone and cyclo(his-pro). Neuropharmacology 27 (1988) 895-901
16. Hubler N., Gottschling B., Jacobs M., von Landenberg F., and Hewicker-Trautwein M. Functional observational battery and motor activity in rats after single administration of two NHE 1 inhibitors. Toxicol. Appl. Pharmacol. 208 (2005) 266-276
17. Inanaga K., Kumashiro H., Fukuyama Y., Ohtahara S., and Shirouzu M. Clinical study of oral administration of DN-1417, a TRH analog, in patients with intractable epilepsy. Epilepsia 30 (1989) 438-445
18. Irwin S. Comprehensive observational assessment. Ia. A systematic, quantitative procedure for assessing the behavioral and physiologic state of the mouse. Psychopharmacologia 13 (1968) 222-257
19. Jain, R., Monga, V., Kaur, N., Sharma, S.S., Kumar, S., Roy, N., Majumdar, J., Agarwal, S., Pawar, C., Kadam, R.U., Chavan, A., 2006. CNS effective thyrotropin releasing hormone analogs. WTO Indian Patent Application No. 2065/DEL/2006.
20. Jain R., Singh J., Perlman J.H., and Gershengorn M.C. Synthesis and biology of new thyrotropin-releasing hormone (TRH) analogues. Bioorg. Med. Chem. 10 (2002) 189-194
21. Jaworska-Feil L., Kajta M., Budziszewska B., Leskiewicz M., and Lason W. Protective effects of TRH and its stable analogue, RGH-2202, on kainate-induced seizures and neurotoxicity in rodents. Epilepsy Res. 43 (2001) 67-73
22. Johannessen Landmark C., and Johannessen S.I. Pharmacological management of epilepsy: recent advances and future prospects. Drugs 68 (2008) 1925-1939
23. Kaur N., Lu X., Gershengorn M.C., and Jain R. Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2. J. Med. Chem. 48 (2005) 6162-6165
24. Kaur N., Monga V., Josan J.S., Lu X., Gershengorn M.C., and Jain R. Synthesis, receptor binding, and activation studies of N(1)-alkyl-l-histidine containing thyrotropin-releasing hormone (TRH) analogues. Bioorg. Med. Chem. 14 (2006) 5981-5988
25. Kaur N., Monga V., Lu X., Gershengorn M.C., and Jain R. Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1. Bioorg. Med. Chem. 15 (2007) 433-443
26. Koskinen L.O., Koch M.L., and Svedberg J. Cerebrovascular effects of the TRH analogues pGlu-3-methyl-His-Pro amide and pGlu-Glu-Pro amide: a comparison with TRH. Ups. J. Med. Sci. 105 (2000) 73-83
27. Kreider M.S., Wolfinger B.L., and Winokur A. Systemic administration of kainic acid produces elevations in TRH in rat central nervous system. Regul. Pept. 28 (1990) 83-93
28. Kubek M.J., and Garg B.P. Thyrotropin-releasing hormone in the treatment of intractable epilepsy. Pediatr. Neurol. 26 (2002) 9-17
29. Lamour Y., Senut M.C., Dutar P., and Bassant M.H. Neuropeptides and septo-hippocampal neurons: electrophysiological effects and distributions of immunoreactivity. Peptides 9 (1988) 1351-1359
30. Lloyd R.L., Pekary A.E., Sattin A., and Amundson T. Antidepressant effects of thyrotropin-releasing hormone analogues using a rodent model of depression. Pharmacol. Biochem. Behav. 70 (2001) 15-22
31. + channel activity in mammalian septal neurons. Proc. Natl. Acad. Sci. U.S.A. 87 (1990) 8150-8154
32. Loscher W. New visions in the pharmacology of anticonvulsion. Eur. J. Pharmacol. 342 (1998) 1-13
33. Lu X., Bidaud I., Ladram A., and Gershengorn M.C. Pharmacological studies of thyrotropin-releasing hormone (TRH) receptors from Xenopus laevis: is xTRHR3 a TRH receptor?. Endocrinology 144 (2003) 1842-1846
34. Malhotra J., and Gupta Y.K. Effect of adenosine receptor modulation on pentylenetetrazole-induced seizures in rats. Br. J. Pharmacol. 120 (1997) 282-288
35. Manocha A., Mediratta P.K., and Sharma K.K. Studies on the anticonvulsant effect of U50488H on maximal electroshock seizure in mice. Pharmacol. Biochem. Behav. 76 (2003) 111-117
36. Mendyk A., Salat K., Librowski T., Czarneck R., and Malawska B. Influence of new gamma-aminobutyric acid amide derivatives and its phthalimide precursors on the central nervous system activity in mice. Pol. J. Pharmacol. 53 (2001) 689-693
37. Momiyama T., Ishihara K., Kimura K., Todo N., Fujita Y., Serikawa T., and Sasa M. Long-term antiepileptic effects of chronic intake of CNK-602A, a thyrotropin-releasing hormone analogue, on spontaneously epileptic rats. Epilepsia 37 (1996) 328-331
38. Monga V., Meena C., Kaur N., Kumar S., Pawar C., Sharma S., and Jain R. Facile synthesis of N-α-Boc-1,2-dialkyl-l-histidines: utility in the synthesis of thyrotropin-releasing hormone (TRH) analogs and evaluation of the CNS activity. J. Heterocyclic Chem. 45 (2008) 1603-1608
39. Nehlig A., Vergnes M., Waydelich R., Hirsch E., Charbonne R., Marescaux C., and Seylaz J. Absence seizures induce a decrease in cerebral blood flow: human and animal data. J. Cereb. Blood Flow Metab. 16 (1996) 147-155
40. Nillni E.A., and Sevarino K.A. The biology of pro-thyrotropin-releasing hormone-derived peptides. Endocr. Rev. 20 (1999) 599-648
41. Noda Y., Furukawa K., Kohayakawa H., and Oka M. Effects of RGH-2202 on behavioral deficits after focal cerebral ischemia in rats. Pharmacol. Biochem. Behav. 52 (1995) 695-699
42. Ogasawara T., Itoh Y., Tamura M., Ukai Y., Yoshikuni Y., and Kimura K. NS-3, a TRH-analog, reverses memory disruption by stimulating cholinergic and noradrenergic systems. Pharmacol. Biochem. Behav. 53 (1996) 391-399
43. Ogawa N., Hirose Y., Mori A., Kajita S., and Sato M. Involvement of thyrotropin-releasing hormone (TRH) neural system of the brain in pentylenetetrazol-induced seizures. Regul. Pept. 12 (1985) 249-256
44. Ohno Y., and Warnick J.E. Effects of thyrotropin-releasing hormone on phencyclidine- and ketamine-induced spinal depression in neonatal rats. Neuropharmacology 27 (1988) 1013-1018
45. Pekary A.E., Sattin A., Meyerhoff J.L., and Chilingar M. Valproate modulates TRH receptor, TRH and TRH-like peptide levels in rat brain. Peptides 25 (2004) 647-658
46. Pitkänen A., Schwartzkroin P.A., and Moshé S.L. Models of Seizures and Epilepsy (2006), Academic Press, New York pp. 153-159
47. Prokai L. Central nervous system effects of thyrotropin-releasing hormone and its analogues: opportunities and perspectives for drug discovery and development. Prog. Drug Res. 59 (2002) 133-169
48. Rajput S.K., Krishnamoorthy S., Pawar C., Kaur N., Monga V., Meena C.L., Jain R., and Sharma S.S. Antiepileptic potential and behavioral profile of l-pGlu-(2-propyl)-l-His-l-ProNH2, a newer thyrotropin-releasing hormone analog. Epilepsy Behav. 14 (2009) 48-53
49. Renaud L.P., Blume H.W., Pittman Q.J., Lamour Y., and Tan A.T. Thyrotropin-releasing hormone selectively depresses glutamate excitation of cerebral cortical neurons. Science 205 (1979) 1275-1277
50. Scalabrino G.A., Hogan N., O'Boyle K.M., Slator G.R., Gregg D.J., Fitchett C.M., Draper S.M., Bennett G.W., Hinkle P.M., Bauer K., Williams C.H., Tipton K.F., and Kelly J.A. Discovery of a dual action first-in-class peptide that mimics and enhances CNS-mediated actions of thyrotropin-releasing hormone. Neuropharmacology 52 (2007) 1472-1481
51. Simasko S.M., and Horita A. Localization of thyrotropin-releasing hormone (TRH) receptors in the septal nucleus of the rat brain. Brain Res. 296 (1984) 393-395
52. Singh J.N., Jain G., Ramarao P., and Sharma S.S. Inhibition of sodium current by carbamazepine in dorsal root ganglion neurons in vitro. Ind. J. Physiol. Pharmacol. 53 (2009) 147-154
53. Sun Y., Lu X., and Gershengorn M.C. Thyrotropin-releasing hormone receptors-similarities and differences. J. Mol. Endocrinol. 30 (2003) 87-97
54. Urayama A., Yamada S., Kimura R., Zhang J., and Watanabe Y. Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice. Life Sci. 72 (2002) 601-607
55. Wu J., Yoon S.H., Wu W.M., and Bodor N. Synthesis and biological evaluations of brain-targeted chemical delivery systems of [Nva2]-TRH. J. Pharm. Pharmacol. 54 (2002) 945-950