Dual neurokinin NK1/NK2 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-arylmethyl-N′-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides
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2014, Journal of Dermatological ScienceCitation Excerpt :Publications of the results are pending (NCT00697710, NCT00703573). DNK333 is a new dual neurokinin 1/2 (NK1/NK2) receptor antagonist [85]. In one previous study the effects of DNK333 on bronchoconstriction in asthma patients has been studied [86].
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2005, Progress in Medicinal ChemistryCitation Excerpt :NK2 receptor affinities are between 17–60 nM, except for DNK333 (78), where the additional chlorine leads to a five times higher affinity to the NK2 receptor in comparison with the monochloro-derivative (72). Both DNK333 and the di-bromothiophene derivative (77) exhibit balanced binding affinities to both the NK1 and the NK2 receptors (Table 3.4)[122, 123]. DNK333 (78), based on its favourable receptor affinity properties, was chosen for further profiling.
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