144734-36-1

144734-36-1 structure

Name: 4F 4PP oxalate
Chemical Name: (4-Fluorophenyl)[1-(4-phenylbutyl)-4-piperidinyl]methanone ethane dioate (1:1)
CAS Number: 144734-36-1
Molecular Formula: C₂₄H₂₈FNO₅
Molecular Weight: 429.48100
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2017-03-24 21:09:27
Modify Date: 2024-01-05 20:49:36
4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM)[1][2][3][4].

Name	(4-Fluorophenyl)[1-(4-phenylbutyl)-4-piperidinyl]methanone ethane dioate (1:1)
Synonyms	D-myo-Inositol-1,3,4,5-tetrakisphosphate,octapotassium salt

Description	4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM)[1][2][3][4].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2A Receptor:5.3 nM (Ki) 5-HT2C Receptor:620 nM (Ki)
In Vivo	4F 4PP (100 nM) reduces the lowest [D-ala2,N-me-phe4,gly.l5]-enkephalin (DAMGO) concentration and can produce a significant depression of evoked field potentials[1].
References	[1]. Aira Z, et al. Selective impairment of spinal mu-opioid receptor mechanism by plasticity of serotonergic facilitation mediated by 5-HT2A and 5-HT2B receptors. Pain. 2012;153(7):1418-1425. [2]. Lee SH, et al. Peripheral serotonin receptor 2B and transient receptor potential channel 4 mediate pruritus to serotonergic antidepressants in mice. J Allergy Clin Immunol. 2018;142(4):1349-1352.e16. [3]. Rodríguez-Muñoz M, et al. Fenfluramine diminishes NMDA receptor-mediated seizures via its mixed activity at serotonin 5HT2A and type 1 sigma receptors. Oncotarget. 2018;9(34):23373-23389. Published 2018 May 4. [4]. Gerhold KJ, et al. Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci. 2015;35(26):9580-9594.