UK-414,495 is a drug developed by Pfizer for the treatment of female sexual arousal disorder (FSAD). It functions as a potent and selective inhibitor of the enzyme neutral endopeptidase (NEP), which typically breaks down the neuropeptide VIP (vasoactive intestinal peptide).
By inhibiting NEP, UK-414,495 increases VIP activity, leading to enhanced blood flow to the genital region, increased lubrication, and muscle relaxation. Studies in anesthetized rabbits have demonstrated that UK-414,495 significantly potentiates pelvic nerve-stimulated increases in vaginal and clitoral blood flow, with no effect on basal genital blood flow or systemic cardiovascular parameters.
This suggests that NEP inhibitors like UK-414,495 could restore sexual arousal in women with FSAD by enhancing endogenous VIP activity without inducing arousal in the absence of sexual stimulation. The drug’s ability to enhance genital blood flow and its potential to avoid the hypotensive effects associated with exogenous VIP administration make it a promising candidate for treating FSAD.
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| Other Names | (Rac)-UK-414495 |
|---|---|
| IUPAC Name | 2-[[1-[(5-ethyl-1, 3, 4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl]pentanoic acid |
| CAS | 337962-93-3 |
| Molecular Weight | 339.5 |
| Molecular Formula | C16H25N3O3S |
| SMILES | CCCC(CC1(CCCC1)C(=O)NC2=NN=C(S2)CC)C(=O)O |