PF-4522654

• Description:

  PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI) [1].

• UNSPSC:

  12352005

• Target:

  5-HT Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein; Neuronal Signaling

• Applications:

  Neuroscience-Neuromodulation

• Field of Research:

  Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/pf-4522654.html

• Smiles:

  FC(C1=NC(CCNCC2)=C2C(NC)=N1)(C3=CC=CC=C3)F

• Molecular Formula:

  C16H18F2N4

• Molecular Weight:

  304.34

• References & Citations:

  [1]R Ian Storer, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. J Med Chem. 2014 Jun 26;57 (12) :5258-69.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  5-HT2 Receptor; α-1 microglobulin

• CAS Number:

  [1065109-28-5]