Influence of a neurokinin-1 receptor antagonist (aprepitant) on gastric sensorimotor function in healthy volunteers

Neurogastroenterology and Motility

Volumn 25, Issue 12, 2013, Pages

  Ang, D ^a   Pauwels, A ^a   Akyuz, F ^a   Vos, R ^a   Tack, J ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Functional dyspepsia; Gastric barostat; Neurokinin antagonist; Visceral sensitivity

Indexed keywords

APREPITANT; PLACEBO;

ADULT; ANOREXIA; ARTICLE; ASTHENIA; BAROSTAT; CONSTIPATION; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DOUBLE BLIND PROCEDURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG TOLERABILITY; DYSPEPSIA; FEMALE; HICCUP; HUMAN; HUMAN EXPERIMENT; MALE; NAUSEA; NORMAL HUMAN; PERCEPTION; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SENSORIMOTOR FUNCTION; STOMACH DISTENSION;

FUNCTIONAL DYSPEPSIA; GASTRIC BAROSTAT; NEUROKININ ANTAGONIST; VISCERAL SENSITIVITY;

ADULT; DOUBLE-BLIND METHOD; FEMALE; GASTROINTESTINAL MOTILITY; HEALTHY VOLUNTEERS; HUMANS; MALE; MORPHOLINES; NEUROKININ-1 RECEPTOR ANTAGONISTS; PAIN PERCEPTION; PAIN THRESHOLD; PLACEBOS;

EID: 84888064496     PISSN: 13501925     EISSN: 13652982     Source Type: Journal    
DOI: 10.1111/nmo.12210     Document Type: Article

References (55)

1. Tack J, Talley NJ, Camilleri M et al. Functional gastroduodenal disorders. Gastroenterology 2006; 130: 1466-79.
2. Sarnelli G, Caenepeel P, Geypens B, Janssens J, Tack J. Symptoms associated with impaired gastric emptying of solids and liquids in functional dyspepsia. Am J Gastroenterol 2003; 98: 783-8.
3. Tack J, Bisschops R, Sarnelli G. Pathophysiology and treatment of functional dyspepsia. Gastroenterology 2004; 127: 1239-55.
4. Tack J, Piessevaux H, Coulie B, Caenepeel P, Janssens J. Role of impaired gastric accommodation to a meal in functional dyspepsia. Gastroenterology 1998; 115: 1346-52.
5. Kindt S, Tack J. Impaired gastric accommodation and its role in dyspepsia. Gut 2006; 55: 1685-91.
6. Tack J, Caenepeel P, Fischler B, Piessevaux H, Janssens J. Hypersensitivity to gastric distension is associated with symptoms in functional dyspepsia. Gastroenterology 2001; 121: 526-35.
7. Pennefather JN, Lecci A, Candenas ML, Patak E, Pinto FM, Maggi CA. Tachykinins and tachykinin receptors: a growing family. Life Sci 2004; 74: 1445-63.
8. Maggi CA, Patacchini R, Rovero P, Giachetti A. Tachykinin receptors and tachykinin receptor antagonists. J Auton Pharmacol 1993; 13: 23-93.
9. Otsuka M, Yoshioka K. Neurotransmitter functions of mammalian tachykinins. Physiol Rev 1993; 73: 229-308.
10. Culman J, Klee S, Ohlendorf C, Unger T. Effect of tachykinin receptor inhibition in the brain on cardiovascular and behavioural responses to stress. J Pharmacol Exp Ther 1997; 280: 238-46.
11. Saria A. The tachykinin NK1 receptor in the brain: pharmacology and putative functions. Eur J Pharmacol 1999; 375: 51-60.
12. Ribeiro-da-Silva A, Hokfelt T. Neuroanatomical localization of substance P in the CNS and sensory neurons. Neuropeptides 2000; 34: 256-71.
13. Quartara L, Altamura M, Evangelista S, Maggi CA. Tachykinin receptor antagonists in clinical trials. Expert Opin Invest Drugs 2009; 18: 1843-64.
14. Rupniak NMJ, Kramer MS. Discovery of the anti-depressant and anti-emetic efficacy of substance P receptor (NK1) antagonists. Trends Pharmacol Sci 1999; 20: 485-9.
15. Rupniak NM, Carlson EJ, Webb JK et al. Comparison of the phenotype of NK1R-/- mice with pharmacological blockade of the substance P (NK1) receptor in assays for antidepressant and anxiolytic drugs. Behav Pharmacol 2001; 12: 497-508.
16. Papp M, Vassout A, Gentsch C et al. The NK1 receptor antagonist NKP608 has an antidepressant-like effect in the chronic mild stress model of depression in rats. Behav Brain Res 2000; 115: 19-23.
17. Cheeta S, Tucci S, Sandhu J et al. Anxiolytic actions of the substance P (NK1) receptor antagonist L-760735 and the 5HT1A agonist 8-OH-DPAT in the social interaction test in gerbils. Brain Res 2001; 915: 170-5.
18. Varty GB, Cohen-Williams ME, Morgan CA et al. The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 2002; 27: 371-9.
19. Kramer MS, Cutler N, Ferghner J. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 1998; 281: 1640-5.
20. Patel L, Lindley C. Aprepitant-a novel NK1 receptor antagonist. Expert Opinion Pharmacother 2003; 4: 2279-96.
21. Prommer E. Aprepitant (EMEND): the role of substance P in nausea and vomiting. J Pain Palliat Care Pharmacother 2005; 19: 31-9.
22. Andrews PLR, Sanger GJ. Abdominal vagal afferent neurones: an important target for the treatment of gastrointestinal dysfunction. Curr Opin Pharmacol 2002; 2: 650-6.
23. Shimizu Y, Matsuyama H, Shiina T, Takewaki T, Furness JB. Tachykinins and their functions in the gastrointestinal tract. Cell Mol Life Sci 2008; 65: 295-311.
24. Grider JR. Tachykinins as transmitters of ascending contractile component of the peristaltic reflex. Am J Physiol 1989; 257: 709-14.
25. Crema F, Moro E, Nardelli G, De Ponti F, Frigo G, Crema A. Role of tachykininergic and cholinergic pathways in modulating canine gastric tone and compliance in vivo. Pharmacol Res 2002; 45: 341-7.
26. Greenwood-Van Meerveld B, Gibson MS, Johnson AC, Venkova K, Sutkowski-Markmann P. NK1 receptor mediated mechanisms regulate colonic hypersensitivity in the guinea pig. Pharmacol Biochem Behav 2003; 74: 1005-13.
27. Kamp EH, Beck DR, Gebhart GF. Combinations of neurokinin receptor antagonists reduce visceral hyperalgesia. J Pharmacol Exp Ther 2001; 299: 105-13.
28. Okano S, Nagaya H, Ikeura Y, Natsugari H, Inatomi N. Effects of TAK-637, a novel neurokinin-1 receptor antagonist, on colonic function in vivo. J Pharmacol Exp Ther 2001; 298: 559-64.
29. Ciechanownicz R, Sein-Anand J, Chodorowski Z, Bitel M, Petrusewicz J, Kordkiewicz RP. Salutary effects of tachykinin receptor antagonists in a rat model of post-operative ileus. J Surg Res 2006; 133: 197-202.
30. Holzer-Petsche U. Modulation of gastric contractions in response to tachykinins and bethanechol by extrinsic nerves. Br J Pharmacol 1991; 103: 1958-62.
31. Azpiroz F, Malagelada JR. Importance of vagal input in maintaining gastric tone in the dog. J Physiol 1987; 384: 511-24.
32. Andrews PL, Lawes IN. The role of vagal and intramural inhibitory reflexes in the regulation of intragastric pressure in the ferret. J Physiol 1982; 326: 435-51.
33. Ladic LA, Buchan AMJ. Assocation of substance P and its receptor with efferent neurons projecting to the greater curvature of the rat stomach. J Auton Nerv Syst 1996; 58: 25-34.
34. Lewis LA, Travagli RA. Effects of substance P on identified neurons of the rat dorsal motor nucleus of the vagus. Am J Physiol 2001; 281: G164-72.
35. Zagorodnyuk V, Maggi CA. Tachykinin NK1 and NK2 receptors mediate non-adrenergic non-cholinergic excitatory neuromuscular transmission in the guinea-pig stomach. Neuroscience 1997; 80: 625-34.
36. Sternini C, Su D, Gamp PD, Bunnett NW. Cellular sites of expression of the neurokinin-1 receptor in the rat gastrointestinal tract. J Comp Neurol 1995; 358: 531-40.
37. Mussap CJ, Burcher E. Characterization and autoradiographic localization of tachykinin receptors in rat gastric fundus. J Pharmacol Exp Ther 1993; 266: 1043-53.
38. Smits GJ, Lefebvre RA. Tachykinin receptors involved in the contractile effect of the natural tachykinins in the rat gastric fundus. J Auton Pharmacol 1994; 14: 383-92.
39. Bueno L, Fioramonti J, Garcia-Villar R. Pathobiology of visceral pain: molecular mechanisms and therapeutic implications. III. Visceral afferent pathways: a source of new therapeutic targets for abdominal pain. Am J Physiol 2000; 278: G670-6.
40. Hargreaves R, Ferreira JC, Hughes D et al. Development of aprepitant, the first neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Ann N Y Acad Sci 2011; 1222: 40-8.
41. ® (aprepitant) capsules: prescribing information. USA [online]. Available at: http://www.merck.com/product/usa/pi_circulars/e/emend/emend_pi.pdf (accessed 10 August 2013).
42. Tack J, Broeckaert D, Coulie B, Janssens J. The influence of cisapride on gastric tone and the perception of gastric distension. Aliment Pharmacol Ther 1998; 12: 761-6.
43. Barber WD, Burks TF. Brain gut interactions: brain stem neuronal response to local gastric effects of substance P. Am J Physiol 1987; 253: G369-77.
44. Vanden Berghe P, Janssen P, Kindt S, Vos R, Tack J. Contribution of different triggers to the gastric accommodation reflex in humans. Am J Physiol Gastrointest Liver Physiol 2009; 297: G902-6.
45. Grider JR, Cable MP, Said SI et al. Vasoactive intestinal peptide as a neural mediator of gastric relaxation. Am J Physiol 1985; 248: G73-8.
46. Tack J, Demedts I, Meulemans A, Schuurkes J, Janssens J. Role of nitric oxide in the gastric accommodation reflex and in meal induced satiety in humans. Gut 2002; 51: 219-24.
47. Coulie B, Tack J, Sifrim D, Andrioli A, Janssens J. Role of nitric oxide in fasting gastric fundus tone and in 5-HT1 receptor mediated relaxation of gastric fundus. Am J Physiol 1999; 276: G373-7.
48. Van Oudenhove L, Kindt S, Vos R, Coulie B, Tack J. Influence of buspirone on gastric sensorimotor function in man. Aliment Pharmacol Ther 2008; 28: 1326-33.
49. Tack J, Vos R, Janssens J, Salter J, Jauffret S, Vandeplassche G. Influence of tegaserod on proximal gastric tone and on the perception of gastric distension. Aliment Pharmacol Ther 2003; 18: 1031-7.
50. Tack J, Broekaert D, Coulie B, Fischler B, Janssens J. Influence of the selective serotonin reuptake inhibitor paroxetine on gastric sensorimotor function in man. Aliment Pharmacol Ther 2003; 17: 603-8.
51. Holzer P. Tachykinins as targets of gastroenterological pharmacotherapy. Drug News Perspect 1998; 11: 394-401.
52. Patacchini R, Giuliani S, Turini A, Navarra G, Maggi CA. Effect of nepadutant at tachykinin NK2 receptors in human intestine and urinary bladder. Eur J Pharmacol 2000; 398: 389-97.
53. Lordal M, Navalesi G, Maggi CA, Theodorsson E, Hellstroem PM. The tachykinin NK2 receptor antagonist nepadutant is a powerful inhibitor of small bowel inhibitor of small bowel motility stimulated by neurokinin A in man. Gastroenterology 1999; 116: A1032.
54. Akyuz F, Mimidis K, Vos R, Tack J. Influence of NK1 receptor antagonist Aprepitant on rectal sensitivity and accommodation of the rectum in the healthy volunteer. Gastroenterology 2007; 4(Suppl. 2): A684.
55. Houghton LA, Cremonini F, Camilleri M et al. Effect of the NK3 receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterol Motil 2007; 19: 732-43.