Name: Lesogaberan napadisylate
Rating: 5 (10 reviews)

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HIT ID:HIT214323869
Cas No:477956-38-0
常用名:Lesogaberan napadisylate
别名:AZD-3355 napadisylate
IUPAC:[(2S)-3-amino-2-fluoropropyl]phosphinic acid; naphthalene-2-sulfonic acid
IUPAC:[(2S)-3-amino-2-fluoropropyl]phosphinic acid; naphthalene-2-sulfonic acid
InChI key:GEUAKFFEFNASOW-HVDRVSQOSA-N

分子式:C13H17FNO5PS
分子量:349.31
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:NC[C@H](F)CP(O)=O.OS(=O)(=O)c1ccc2ccccc2c1
SMILES:NC[C@H](F)CP(O)=O.OS(=O)(=O)c1ccc2ccccc2c1

Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

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