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Volumn 106, Issue 1, 2008, Pages 121-127

Pharmacological characterization of T-2328, 2-fluoro-4′-methoxy- 3′-[[[(2S,3S)-2-phenyl-3-piperidinyl]amino]methyl]-[1,1′-biphenyl] -4-carbonitrile dihydrochloride, as a brain-penetrating antagonist of tachykinin NK1 receptor

Author keywords

Anti emetic; Brain penetrative; Cisplatin; Delayed emesis; NK1 antagonist

Indexed keywords

2 FLUORO 4' METHOXY 3' [[(2 PHENYL 3 PIPERIDINYL)AMINO]METHYL] [1,1' BIPHENYL] 4 CARBONITRILE; 5 AMINOVALERYLSUBSTANCE P [7-11][9 PROLINE 10 (N METHYLLEUCINE)]; APREPITANT; CISPLATIN; ION CHANNEL; NEUROKININ 1 RECEPTOR ANTAGONIST; NEUROKININ 2 RECEPTOR; NEUROKININ 3 RECEPTOR; SAREDUTANT; T 2328; TACHYKININ RECEPTOR ANTAGONIST; TALNETANT; UNCLASSIFIED DRUG;

EID: 38549151079     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.FP0071400     Document Type: Article
Times cited : (14)

References (23)
  • 1
    • 0027523466 scopus 로고
    • Neurotransmitter functions of mammalian tachykinins
    • Otsuka M, Yoshioka K. Neurotransmitter functions of mammalian tachykinins. Physiol Rev. 1993;73:229-308.
    • (1993) Physiol Rev , vol.73 , pp. 229-308
    • Otsuka, M.1    Yoshioka, K.2
  • 3
    • 24144472503 scopus 로고    scopus 로고
    • Species differences in tachykinin receptor distribution: Further evidence that the substance P (NK1) receptor predominates in human brain
    • Rigby M, O'Donnell R, Rupniak NM. Species differences in tachykinin receptor distribution: further evidence that the substance P (NK1) receptor predominates in human brain. J Comp Neurol. 2005;490:335-353.
    • (2005) J Comp Neurol , vol.490 , pp. 335-353
    • Rigby, M.1    O'Donnell, R.2    Rupniak, N.M.3
  • 4
    • 0347816226 scopus 로고    scopus 로고
    • The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: A multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin - the Aprepitant Protocol 052 Study Group
    • Hesketh PJ, Grunberg SM, Gralla RJ, Warr DG, Roila F, de Wit R, et al. The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin - the Aprepitant Protocol 052 Study Group. J Clin Oncol. 2003;21:4112-4119.
    • (2003) J Clin Oncol , vol.21 , pp. 4112-4119
    • Hesketh, P.J.1    Grunberg, S.M.2    Gralla, R.J.3    Warr, D.G.4    Roila, F.5    de Wit, R.6
  • 5
    • 0038728753 scopus 로고    scopus 로고
    • Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America
    • Poli-Bigelli S, Rodrigues-Pereira J, Carides AD, Julie Ma G, Eldridge K, Hipple A, et al. Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America. Cancer. 2003;97:3090-3098.
    • (2003) Cancer , vol.97 , pp. 3090-3098
    • Poli-Bigelli, S.1    Rodrigues-Pereira, J.2    Carides, A.D.3    Julie Ma, G.4    Eldridge, K.5    Hipple, A.6
  • 6
    • 0032508514 scopus 로고    scopus 로고
    • Distinct mechanism for antidepressant activity by blockade of central substance P receptors
    • Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek JJ, et al. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science. 1998;281:1640-1645.
    • (1998) Science , vol.281 , pp. 1640-1645
    • Kramer, M.S.1    Cutler, N.2    Feighner, J.3    Shrivastava, R.4    Carman, J.5    Sramek, J.J.6
  • 7
    • 22444442937 scopus 로고    scopus 로고
    • Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo
    • Furmark T, Appel L, Michelgard A, Wahlstedt K, Ahs F, Zancan S, et al. Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo. Biol Psychiatry. 2005;58:132-142.
    • (2005) Biol Psychiatry , vol.58 , pp. 132-142
    • Furmark, T.1    Appel, L.2    Michelgard, A.3    Wahlstedt, K.4    Ahs, F.5    Zancan, S.6
  • 8
    • 33747193244 scopus 로고    scopus 로고
    • Tachykinin receptors antagonists: From research to clinic
    • Quartara L, Altamura M. Tachykinin receptors antagonists: from research to clinic. Curr Drug Targets. 2006;7:975-992.
    • (2006) Curr Drug Targets , vol.7 , pp. 975-992
    • Quartara, L.1    Altamura, M.2
  • 9
    • 15144354434 scopus 로고    scopus 로고
    • Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl) phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl) methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist
    • Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, et al. Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl) phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl) methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. J Med Chem. 1998;41:4607-4614.
    • (1998) J Med Chem , vol.41 , pp. 4607-4614
    • Hale, J.J.1    Mills, S.G.2    MacCoss, M.3    Finke, P.E.4    Cascieri, M.A.5    Sadowski, S.6
  • 10
    • 0033625089 scopus 로고    scopus 로고
    • The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets
    • Tattersall FD, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, et al. The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets. Neuropharmacology. 2000;39:652-663.
    • (2000) Neuropharmacology , vol.39 , pp. 652-663
    • Tattersall, F.D.1    Rycroft, W.2    Cumberbatch, M.3    Mason, G.4    Tye, S.5    Williamson, D.J.6
  • 11
    • 34047189666 scopus 로고    scopus 로고
    • Aprepitant: A substance P antagonist for chemotherapy induced nausea and vomiting
    • Girish C, Manikandan S. Aprepitant: a substance P antagonist for chemotherapy induced nausea and vomiting. Indian J Cancer. 2007;44:25-30.
    • (2007) Indian J Cancer , vol.44 , pp. 25-30
    • Girish, C.1    Manikandan, S.2
  • 12
    • 0029658238 scopus 로고    scopus 로고
    • The action of the NK1 tachykinin receptor antagonist, CP 99,994, in antagonizing the acute and delayed emesis induced by cisplatin in the ferret
    • Rudd JA, Jordan CC, Naylor RJ. The action of the NK1 tachykinin receptor antagonist, CP 99,994, in antagonizing the acute and delayed emesis induced by cisplatin in the ferret. Br J Pharmacol. 1996;119:931-936.
    • (1996) Br J Pharmacol , vol.119 , pp. 931-936
    • Rudd, J.A.1    Jordan, C.C.2    Naylor, R.J.3
  • 15
  • 16
    • 0028174651 scopus 로고
    • Chromodacryorrhea and repetitive hind paw tapping: Models of peripheral and central tachykinin NK1 receptor activation in gerbils
    • Bristow LJ, Young L. Chromodacryorrhea and repetitive hind paw tapping: models of peripheral and central tachykinin NK1 receptor activation in gerbils. Eur J Pharmacol. 1994;253:245-252.
    • (1994) Eur J Pharmacol , vol.253 , pp. 245-252
    • Bristow, L.J.1    Young, L.2
  • 17
    • 0028113481 scopus 로고
    • Differential inhibition of foot tapping and chromodacryorrhoea in gerbils by CNS penetrant and non-penetrant tachykinin NK1 receptor antagonists
    • Rupniak NM, Williams AR. Differential inhibition of foot tapping and chromodacryorrhoea in gerbils by CNS penetrant and non-penetrant tachykinin NK1 receptor antagonists. Eur J Pharmacol. 1994;265:179-183.
    • (1994) Eur J Pharmacol , vol.265 , pp. 179-183
    • Rupniak, N.M.1    Williams, A.R.2
  • 18
    • 33645111467 scopus 로고    scopus 로고
    • Emerging drugs for chemotherapy-induced emesis
    • Navari RM, Province PS. Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006;11:137-151.
    • (2006) Expert Opin Emerg Drugs , vol.11 , pp. 137-151
    • Navari, R.M.1    Province, P.S.2
  • 19
    • 21344451918 scopus 로고    scopus 로고
    • Optimising antiemetic therapy: What are the problems and how can they be overcome?
    • Aapro M. Optimising antiemetic therapy: what are the problems and how can they be overcome? Curr Med Res Opin. 2005;21:885-897.
    • (2005) Curr Med Res Opin , vol.21 , pp. 885-897
    • Aapro, M.1
  • 20
    • 0038730808 scopus 로고    scopus 로고
    • Roles of substance P and NK(1) receptor in the brainstem in the development of emesis
    • Saito R, Takano Y, Kamiya HO. Roles of substance P and NK(1) receptor in the brainstem in the development of emesis. J Pharmacol Sci. 2003;91:87-94.
    • (2003) J Pharmacol Sci , vol.91 , pp. 87-94
    • Saito, R.1    Takano, Y.2    Kamiya, H.O.3
  • 22
    • 0034812947 scopus 로고    scopus 로고
    • Anti-emetics for cancer chemotherapy-induced emesis: Potential of alternative delivery systems
    • Kraut L, Fauser AA. Anti-emetics for cancer chemotherapy-induced emesis: Potential of alternative delivery systems. Drugs. 2001;61:1553-1562.
    • (2001) Drugs , vol.61 , pp. 1553-1562
    • Kraut, L.1    Fauser, A.A.2
  • 23
    • 33746381174 scopus 로고    scopus 로고
    • Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives
    • Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, et al. Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives. Bioorg Med Chem Lett. 2006;16:4504-4511.
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 4504-4511
    • Meurer, L.C.1    Finke, P.E.2    Owens, K.A.3    Tsou, N.N.4    Ball, R.G.5    Mills, S.G.6


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