Aprepitant and L-758298. Antiemetic, antidepressant, tachykinin NK1, antagonist

Drugs of the Future

Volumn 27, Issue 3, 2002, Pages 211-222

  Sorbera, L A ^a   Castaner, J ^a   Bayes, M ^a   Silvestre, J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

2 [1 [3,5 BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY] 3 (4 FLUOROPHENYL) 4 (3 OXO 1 PHOSPHORYL 1,2,4 TRIAZOL 5 YLMETHYL)MORPHOLINE; 2 [1 IMINO 2 (2 METHOXYPHENYL)ETHYL] 7,7 DIPHENYLPERHYDROISOINDOL 4 ONE; 2 [3,5 BIS(TRIFLUOROMETHYL)BENZYLOXY] 4 (3 OXO 1,2,4 TRIAZOL 5 YLMETHYL) 3 PHENYLMORPHOLINE; 3 (2 METHOXY 5 TRIFLUOROMETHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; 3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; [2 METHOXY 5 (1 TETRAZOLYL)BENZYL](2 PHENYL 3 PIPERIDINYL)AMINE; APREPITANT; CISPLATIN; DNK 333; GRANISETRON; L 754939; NALPITANTIUM; NEUROKININ; NEUROKININ NK1 RECEPTOR; NKP 608; ONDANSETRON; PRODRUG; SUBSTANCE P; TACHYKININ; TACHYKININ RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL MODEL; ANXIETY NEUROSIS; DEPRESSION; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; NAUSEA; NAUSEA AND VOMITING; REVIEW; VOMITING;

EID: 0036107079     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2002.027.03.661047     Document Type: Review

References (47)

1. Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro) phenyl-4-(3-oxo-1,2,4,-trizol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist
2. 1 antagonist
3. Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs
4. On the occurrence of substance P-containing fibers in sympathetic ganglia: Immunohistochemical evidence
5. Substance P, VIP-, and enkephalin-like immunoreactivity in the human vagus nerve
6. Substance P
7. History of tachykinin peptides
8. Distinct mechanism for antidepressant activity by blockade of central substance P receptors
9. In vivo and in vitro characterisation of NK, antagonist MK-869
10. 1 receptor antagonist
11. 1 receptor antagonists
12. 1 receptor activation in gerbils
13. Characterisation of the tachykinin-induced hindlimb thumping response in gerbils
14. 1 receptor antagonist: Behavioural effects
15. 1 receptor antagonists
16. 1 receptor antagonists in a novel gerbil elevated plus-maze
17. 1 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
18. Substance P receptor antagonist I: Conversion of phosphoramidate prodrug after i.v. administration to rats and dogs
19. Substance P-induced vasoditatation is mediated by the neurokinin type 1 receptor but does not contribute to basal vascular tone in man
20. The therapeutic potential of substance P (NK-1 receptor) antagonists (SPA)
21. Reduction of cisptatin-induced emesis by a selective neurokinin-1-receptor antagonist
22. Establishing the dose of the oral NK-1 antagonist MK-869 for chemotherapy induced nausea and vomiting
23. Prevention of cisplatin-induced emesis by the oral neurokinin-1 antagonist, MK-869, in combination with granisetron and dexamethasone or with dexamethasone alone
24. Effect of an NK-1 antagonist (MK-0869) on patient-reported impact of chemotherapy-induced nausea and vomiting (CINV) on daily life
25. Prevention of cisplatin-induced emesis by the selective neurokinin-1 antagonist, L-754,030, and its prodrug, L-758,298
26. Comparison of L-758,298, a prodrug for the selective neurokinin-1 antagonist, L-754,030, with ondansetron for the prevention of cisplatin-induced emesis
27. Comparison of a neurokinin-1 antagonist, L-758,298, and scopolamine with placebo in the prevention of motion-induced nausea in man
28. 1 receptor antagonist L-754,030) in the acute treatment of migraine
29. The substance P receptor antagonist L-754,030 (MK-0869) is ineffective in the treatment of postherpetic neuralgia
30. Comparison of a neurokinin-1 antagonist, L-754,030, to placebo, acetaminophen and ibuprofen in the dental pain model
31. 1 receptor
32. 2) antagonists: Fermentation, isolation, physico-chemical properties, and biological activity
33. Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist
34. Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1- Arylmethyl-3-(2-oxo-azepan-3-yl) carbamoyl]allyl-N -methyl-3,5-bis(trifluoromethyl)-benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-aryl-methyl-N'-methylhydrazino]-N- [(R)-2-oxo-azepan-3-yl]propiona mides
35. 2 receptor antagonist for the treatment of asthma and rhinitis
36. 1 receptor antagonist
37. 1 receptor antagonist
38. Pharmacology of NKP608, a novel selective neurokinin-1 receptor antagonist with oral activity
39. 1 receptor antagonist, in ferrets
40. 1 receptor antagonists in ferrets by their ability to inhibit GR73632-induced foot tapping in gerbils