4F 4PP oxalate

Names

[ Name ]:
4F 4PP oxalate

[Synonym ]:
D-myo-Inositol-1,3,4,5-tetrakisphosphate,octapotassium salt

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₈FNO₅

[ Molecular Weight ]:
429.48100

[ Exact Mass ]:
429.19500

[ PSA ]:
94.91000

[ LogP ]:
3.83680

Related Compounds

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