Potent, selective and competitive non-peptide NK3
receptor antagonist (Ki
= 13 nM at hNK3
). Displays 90-fold and 7000-fold selectivity over hNK2
receptors respectively. Active in vivo
, inhibiting agonist-induced pupillary constriction.
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Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.
Giardina et al.
In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists.
Medhurst et al.
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