PF-4522654
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].
Product Specifications
CAS Number
1065109-28-5
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
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