Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets

Pharmacology Biochemistry and Behavior

Volumn 102, Issue 1, 2012, Pages 95-100

  Duffy, Ruth A ^a   Morgan, Cynthia ^a   Naylor, Robert ^b   Higgins, Guy A ^c   Varty, Geoffrey B ^d   Lachowicz, Jean E ^a   Parker, Eric M ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b UNIVERSITY OF BRADFORD   (United Kingdom)

^c InterVivo Solutions Inc   (Canada)

^d SANOFI   (France)

Author keywords

Chemotherapy induced nausea and vomiting (CINV); Ferret: emesis; Neurokinin NK1; NK1 antagonist; Post operative nausea and vomiting (POVN)

Indexed keywords

CALCIUM; NEUROKININ 1 RECEPTOR; NEUROKININ 2 RECEPTOR; NEUROKININ 3 RECEPTOR; ROLAPITANT;

ANIMAL EXPERIMENT; ANTIEMETIC ACTIVITY; ARTICLE; CALCIUM TRANSPORT; CHEMOTHERAPY INDUCED NAUSEA AND VOMITING; DRUG PROTEIN BINDING; FERRET; GERBIL; GUINEA PIG; HAPLORHINI; HUMAN; IN VITRO SELECTION; NONHUMAN; POSTOPERATIVE NAUSEA AND VOMITING; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; ANIMALS; ANTIEMETICS; CERCOPITHECUS AETHIOPS; CHO CELLS; COS CELLS; CRICETINAE; DOGS; FEMALE; FERRETS; GERBILLINAE; GUINEA PIGS; HUMANS; MACACA FASCICULARIS; MICE; NEUROKININ-1 RECEPTOR ANTAGONISTS; PROTEIN BINDING; RABBITS; RATS; RECEPTORS, NEUROKININ-1; SPIRO COMPOUNDS;

ANIMALIA; CAVIA; GERBILLINAE; MUSTELA; ORYCTOLAGUS CUNICULUS; RATTUS;

EID: 84859930834     PISSN: 00913057     EISSN: 18735177     Source Type: Journal    
DOI: 10.1016/j.pbb.2012.03.021     Document Type: Article

References (25)

1. T.M. Ballard, S. Sanger, and G.A. Higgins Inhibition of shock-induced foot tapping behaviour in the gerbil by a tachykinin NK1 receptor antagonist Eur J Pharmacol 412 2001 255 264 (Pubitemid 32144941)
2. D.T. Beattie, I.J. Beresford, H.E. Connor, F.H. Marshall, A.B. Hawcock, and R.M. Hagan The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist Br J Pharmacol 116 1995 3149 3157 (Pubitemid 26008855)
3. C. Bountra, K. Bunce, T. Dale, C. Gardner, C. Jordan, and D. Twissell Anti-emetic profile of a non-peptide neurokinin NK1 receptor antagonist, CP-99,994, in ferrets Eur J Pharmacol 249 1993 R3 R4
4. L.J. Bristow, and L. Young Chromodacryorrhea and repetitive hind paw tapping: models of peripheral and central tachykinin NK1 receptor activation in gerbils Eur J Pharmacol 253 1994 245 252
5. M.P. Curran, and D.M. Robinson Aprepitant: a review of its use in the prevention of nausea and vomiting Drugs 69 2009 1853 1878
6. P. Diemunsch, and L. Grelot Potential of substance P antagonists as antiemetics Drugs 60 2000 533 546
7. P. Diemunsch, G.P. Joshi, and J.F. Brichant Neurokinin-1 receptor antagonists in the prevention of postoperative nausea and vomiting Br J Anaesth 103 2009 7 13
8. R.A. Duffy Potential therapeutic targets for Neurokinin 1 (NK1) receptor antagonists Expert Opin Emerg Drugs 9 2004 9 21 (Pubitemid 38715575)
9. R.A. Duffy, G.B. Varty, C.A. Morgan, and J.E. Lachowicz Correlation of neurokinin NK1 receptor occupancy in gerbil striatum with the behavioral effects of NK1 antagonists J Pharmacol Exp Ther 301 2002 1 7
10. T.M. Fong, H. Yu, and C.D. Strader Molecular basis for the species selectivity of the neurokin-1 receptor antagonist CP-96345 J Biol Chem 267 1992 25668 25671 (Pubitemid 23013958)
11. T.J. Gan, J. Gu, N. Singla, F. Chung, M.H. Pearman, and S.D. Bergese Rolapitant for the prevention of postoperative nausea and vomiting: a prospective, double-blinded, placebo-controlled randomized trial Anesth Analg 112 2011 804 812
12. C.J. Gardner, D.J. Twissell, T.J. Dale, J.D. Gale, C.C. Jordan, and G.J. Kilpatrick The broad spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonisr GR203040 Br J Pharmacol 116 1995 3158 3163 (Pubitemid 26008856)
13. C.J. Gardner, D.R. Armour, D.T. Beattie, J.D. Gale, A.B. Hawcock, and G.J. Kilpatrick GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity Regul Pept 65 1996 45 53 (Pubitemid 26273586)
14. A.P. Ray, S. Chebolu, J. Ramirez, and N.A. Darmani Ablation of least shrew central neurokinin NK1 receptors reduces GR73632-induced vomiting Behav Neurosci 123 2009 701 706
15. J.A. Rudd, C.C. Jordan, and R.J. Naylor 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 119 1996 931 936 (Pubitemid 26366488)
16. J.A. Rudd, M.P. Ngan, and M.K. Wai Inhibition of emesis by tachykinin NK1 receptor antagonists in Suncus murinus (house musk shrew) Eur J Pharmacol 366 1999 243 252 (Pubitemid 29080789)
17. N.M. Rupniak, and M.S. Kramer Discovery of the anti-depressant and anti-emetic efficacy of substance P receptor (NK1) antagonists Trends Pharmacol Sci 20 1999 485 490 (Pubitemid 30004020)
18. N.M.J. Rupniak, and A.R. Williams Differential inhibition of foot tapping and chromodacryorrhoea in gerbils by CNS penetrant and non-penetrant tachykinin NK1 receptor antagonists Eur J Pharmacol 265 1994 179 183 (Pubitemid 24356780)
19. A. Saria The tachykinin NK1 receptor in the brain: pharmacology and putative functions Eur J Pharmacol 375 1999 51 60 (Pubitemid 29317592)
20. L. Singh, M.J. Field, J. Hughes, B.S. Kuo, N. Suman-Chauhan, and B.R. Tuladhar The tachykinin NK1 receptor antagonist PD 154075 blocks cisplatin-induced emesis in the ferret Eur J Pharmacol 321 1997 209 216 (Pubitemid 27089553)
21. F.D. Tattersall, W. Rycroft, R.J. Hargreaves, and R.G. Hill The tachykinin NK1 receptor antagonist CP-99994 attenuates cisplatin-induced emesis in the ferret Eur J Pharmacol 250 1993 R5 R6
22. F.D. Tattersall, W. Rycroft, R.G. Hill, and R.J. Hargreaves Enantiomeric inhibition of apomorphine-induced emesis in the ferret by the neurokinin1 receptor antagonist CP-99,994 Neuropharmacology 33 1994 259 260
23. F.D. Tattersall, W. Rycroft, B. Francis, D. Pearce, K. Merchant, and A.M. MacLeod Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets Neuropharmacology 35 1996 1121 1129 (Pubitemid 27008187)
24. F.D. Tattersall, W. Rycroft, M. Cumberbarch, G. Mason, S. Tye, and D.J. Williamson The novel NK1 receptor antagonist MK0869 (L-754,030) and its water soluble phosphoryl prodrug, L-754-298, inhibit acute and delated cisplatin-induced emesis in ferrets Neuropharmacology 39 2000 552 563
25. J.W. Watson, S.F. Gonsalves, A.A. Fossa, S. McLean, T. Seeger, and S. Obach The anti-emetic effects of CP-99,994 in the ferret and the dog: role of the NK1 receptor Br J Pharmacol 115 1995 84 94