PF-00446687

PF-00446687 is a drug developed by Pfizer for the treatment of erectile dysfunction, which is a non-peptide agonist selective for the melanocortin receptor subtype MC₄. It was found to be active in preliminary human trials, with the 200mg dose being of similar effectiveness to 100mg sildenafil, though lower doses were ineffective.

PF-00446687

Identifiers
IUPAC name (3R,4R,5S)-1-([(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl)-3,5-dimethyl-4-phenylpiperidin-4-ol
CAS Number	862281-92-3 Y
PubChem CID	11328898
ChemSpider	24669573
UNII	63P236Z73I
Chemical and physical data
Formula	C28H36F2N2O2
Molar mass	470.605 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@@H]1CN(C[C@@H]([C@]1(c2ccccc2)O)C)C(=O)[C@@H]3CN(C[C@H]3c4ccc(cc4F)F)C(C)(C)C
InChI InChI=1S/C28H36F2N2O2/c1-18-14-31(15-19(2)28(18,34)20-9-7-6-8-10-20)26(33)24-17-32(27(3,4)5)16-23(24)22-12-11-21(29)13-25(22)30/h6-13,18-19,23-24,34H,14-17H2,1-5H3/t18-,19+,23-,24+,28-/m0/s1 Key:WHPJOAUPIZDJNX-AGGGUQDCSA-N

Research

While it is unclear whether PF-00446687 itself will be potent and effective enough to be developed for medical use, it has demonstrated that selectively targeting the MC₄ subtype can produce similar aphrodisiac effects to older non-selective peptide-based melanocortin receptor agonists like melanotan II and bremelanotide, without the side effects caused by action at the other melanocortin receptor subtypes.^[1][2]

See also

• PL-6983
• PF-219,061
• UK-414,495