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. Author manuscript; available in PMC: 2013 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2011 Dec 20;20(3):1337–1345. doi: 10.1016/j.bmc.2011.12.013

Table 1.

Vasopressin receptor affinity and PAMPA-BBB results for potential SRX246 based PET and SPECT ligands

Compound hV1a Ki (nM) hV1b Ki (nM) hV2 Ki (nM) cLogP Pe (10−6 cm s−1) Predicted CNS penetration
11a 1.1 >1000 >1000 5.62 2.2 CNS±
11b 0.61 1154 >10,000 4.42 5.3 CNS+
11c 0.63 1300 >10,000 4.75 4.5 CNS+