Pathophysiology of the Enteric Nervous System 2004
DOI: 10.1002/9780470760307.ch17
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Tachykinin Receptor Antagonists: Silencing Neuropeptides with a Role in the Disturbed Gut

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Cited by 3 publications
(7 citation statements)
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“…Given the redundancy of mechanisms controlling neurosensory and neuromuscular functions in the gut, it is conceivable that effective treatment of functional gut disorders may require combination therapy or the design of multiple ligands. One example is provided by TK receptor antagonists; it has been suggested that the analgesic efficacy of multi‐ or pan‐TK receptor antagonists is superior to that of monoreceptor antagonists 131 . Another example is provided by the possible combination of a 5‐HT 3 receptor antagonist with a 5‐HT 4 receptor agonist to modulate visceral sensitivity, peristalsis and fluid absorption.…”
Section: Serotonergic Modulation Of Visceral Sensationmentioning
confidence: 99%
See 1 more Smart Citation
“…Given the redundancy of mechanisms controlling neurosensory and neuromuscular functions in the gut, it is conceivable that effective treatment of functional gut disorders may require combination therapy or the design of multiple ligands. One example is provided by TK receptor antagonists; it has been suggested that the analgesic efficacy of multi‐ or pan‐TK receptor antagonists is superior to that of monoreceptor antagonists 131 . Another example is provided by the possible combination of a 5‐HT 3 receptor antagonist with a 5‐HT 4 receptor agonist to modulate visceral sensitivity, peristalsis and fluid absorption.…”
Section: Serotonergic Modulation Of Visceral Sensationmentioning
confidence: 99%
“…One example is provided by TK receptor antagonists; it has been suggested that the analgesic efficacy of multi-or pan-TK receptor antagonists is superior to that of monoreceptor antagonists. 131 Another example is provided by the possible combination of a 5-HT 3 receptor antagonist with a 5-HT 4 receptor agonist to modulate visceral sensitivity, peristalsis and fluid absorption. 5-HT 3 receptor antagonists slow transit, and 30% of patients treated with alosetron develop constipation.…”
Section: Serotonergic Modulation Of Visceral Sensationmentioning
confidence: 99%
“…Another example is provided by tachykinin receptor antagonists; it has been suggested that the analgesic efficacy and motility inhibition of multi-tachykinin or pan-tachykinin receptor antagonists are superior to that of monoreceptor antagonists. 26,27 Pharmacodynamic versus pathophysiologic target. When drugs target a single receptor mechanism, heterogeneity in pathophysiology (eg, dysmotility vs hypersensitivity) has a negative impact on the therapeutic gain if patients are not selected on the basis of the specific disorder.…”
Section: The Pharmacodynamic Targetmentioning
confidence: 99%
“…One example is provided by tachykinin receptor antagonists, which have so far given disappointing results because of inherent differences among animal models and humans: it has been suggested that the analgesic efficacy of multi- or pan-tachykinin receptor antagonists is superior to that of mono-receptor antagonists (Holzer, 2004a). …”
Section: The “Magic Bullet”: a Concept That Needs Rethinkingmentioning
confidence: 99%
“…Through the locations of NK receptors on intrinsic nerves, extrinsic nerves, inflammatory cells, and smooth muscle, inhibition of tachykinin receptors has the potential to inhibit motility, sensitivity, secretion, and inflammation in the gastrointestinal tract (Holzer, 2004a; Lecci et al, 2004). NK 1 receptor antagonists also have antiemetic properties (Holzer, 2004a). Several tachykinin receptor antagonists have been developed so far, but the results, in general, have been disappointing.…”
Section: Classes Of Drugs Used or Under Development In Ibsmentioning
confidence: 99%