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. Author manuscript; available in PMC: 2014 Mar 1.
Published in final edited form as: ChemMedChem. 2013 Jan 29;8(3):385–395. doi: 10.1002/cmdc.201200585

Table 6.

Examples of EP1 receptor antagonists bearing a carboxylic acid or 2,2,2-trifluoroethan-1-ol or trifluoro-methylketone hydrate isostere.[28]

graphic file with name nihms-455683-t0028.jpg
Compd X Ki[a] [nm] B/P[b] t1/2[c] [h]
30 COOH 3 – <1
31 graphic file with name nihms-455683-t0029.jpg 3 – 1
32 graphic file with name nihms-455683-t0030.jpg 4 1 2
[a]

EP1 inhibitory constant.

[b]

Brain/plasma (B/P) ratio.

[c]

Half-life (t1/2) in rat.