477956-38-0
Chemical Structure
Lesogaberan napadisylate
Synonym(s): AZD-3355 napadisylate
- CAS No.: 477956-38-0
- Formula:C13H17FNO5PS
- Molecular Weight:349.31
IUPAC Name: naphthalene-2-sulfonic acid compound with ((R)-3-amino-2-fluoropropyl)phosphinic acid (1:1)
InChIKey: GEUAKFFEFNASOW-ZYRQIYSTSA-N
SMILES: O=S(C1=CC=C2C=CC=CC2=C1)(O)=O.O=P(C[C@H](F)CN)O
Biological Activity: Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].
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Lesogaberan napadisylate | Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. | |||||||||||||||||||||
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Keywords
