Preclinical Evaluation of the Effects of Trazpiroben (TAK-906), a Novel, Potent Dopamine D 2 /D 3 Receptor Antagonist for the Management of Gastroparesis

Current therapies for gastroparesis metoclopramide and domperidone carry risks of extrapyramidal symptoms and life-threatening cardiac arrhythmias. Trazpiroben, a novel, potent dopamine D /D receptor antagonist, has low brain permeation and very low affinity for human ether-à-go-go-related gene (hER...

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Veröffentlicht in:	The Journal of pharmacology and experimental therapeutics 2021-10, Vol.379 (1), p.85-95
Hauptverfasser:	Whiting, Roger L, Choppin, Agnes, Luehr, Gary, Jasper, Jeffrey R
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antiemetics - pharmacology Antiemetics - therapeutic use CHO Cells Cricetinae Cricetulus Disease Management Dogs Domperidone - analogs & derivatives Domperidone - pharmacology Domperidone - therapeutic use Dopamine Antagonists - chemistry Dopamine Antagonists - pharmacology Dopamine Antagonists - therapeutic use Dopamine D2 Receptor Antagonists - chemistry Dopamine D2 Receptor Antagonists - pharmacology Dopamine D2 Receptor Antagonists - therapeutic use Dose-Response Relationship, Drug Drug Evaluation, Preclinical - methods Female Gastroparesis - drug therapy Gastroparesis - metabolism HEK293 Cells Humans Male Rats Rats, Sprague-Dawley Receptors, Dopamine D2 - metabolism Receptors, Dopamine D3 - antagonists & inhibitors Receptors, Dopamine D3 - metabolism
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