UK-414,495

UK-414,495 is a drug developed by Pfizer for the treatment of female sexual arousal disorder. UK-414,495 acts as a potent, selective inhibitor of the enzyme neutral endopeptidase, which normally serves to break down the neuropeptide VIP. The consequent increase in VIP activity alters blood flow to the genital region leading to increased lubrication and muscle relaxation.[1][2][3]

UK-414,495
Identifiers
  • (2R)-2-({1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl}methyl)pentanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H25N3O3S
Molar mass339.45 g·mol−1
3D model (JSmol)
  • CCC[C@H](CC1(CCCC1)C(=O)NC2=NN=C(S2)CC)C(=O)O
  • InChI=1S/C16H25N3O3S/c1-3-7-11(13(20)21)10-16(8-5-6-9-16)14(22)17-15-19-18-12(4-2)23-15/h11H,3-10H2,1-2H3,(H,20,21)(H,17,19,22)/t11-/m1/s1 ☒N
  • Key:FWXXCSISWQQOGS-LLVKDONJSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

See also

References
  1. Armer R, Warne P, Witherington J (2006). "Recent disclosures of clinical drug candidates". Drug News & Perspectives. 19 (1): 65–72. ISSN 0214-0934. PMID 16550257.
  2. Angulo, J. (2010). "Neutral endopeptidase inhibition: could it have a role in the treatment of female sexual arousal disorder?". British Journal of Pharmacology. 160 (1): 48–50. doi:10.1111/j.1476-5381.2010.00693.x. PMC 2860205. PMID 20412067.
  3. Wayman, C.; Baxter, D.; Turner, L.; Van Der Graaf, P.; Naylor, A. (2010). "UK-414,495, a selective inhibitor of neutral endopeptidase, potentiates pelvic nerve-stimulated increases in female genital blood flow in the anaesthetized rabbit". British Journal of Pharmacology. 160 (1): 51–59. doi:10.1111/j.1476-5381.2010.00691.x. PMC 2860206. PMID 20412068.


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