Diarylpropionitrile

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Diarylpropionitrile (DPN), also known as 2,3-bis(p-hydroxyphenyl)propionitrile (2,3-BHPPN), is a synthetic, non-steroidal, and highly selective agonist of ERβ (IC50 = 15 nM)[1] that is used widely in scientific research to study the function of this receptor.[1][2] It is 70-fold more selective for ERβ over ERα,[3] and has 100-fold lower affinity for GPER (GPR30) relative to estradiol.[4] DPN produces antidepressant- and anxiolytic-like effects in animals via activation of the endogenous oxytocin system.[5]

DPN is a racemic mixture of two enantiomers, (R)-DPN and (S)-DPN. Relative to (R)-DPN, (S)-DPN has between 3- and 7-fold higher affinity for ERβ and appears to have higher intrinsic activity in activating ERβ.[6][7] However, both enantiomers have very high affinity, potency, selectivity for ERβ and efficaciously activate ERβ.[6] In any case, it has been suggested that (S)-DPN might be the preferred enantiomer to use for scientific research.[6]

See also

References

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