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Safety Information

SML3509

Sigma-Aldrich

F13714

≥95% (HPLC)

Synonym(s):

(3-Chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methyl-6-methylaminopyridin-2-ylmethyl)amino]methyl}piperidin-1-yl)methanone, 1-(3-Chloro-4-fluorobenzoyl)-4-fluoro-N-[[5-methyl-6-(methylamino)-2-pyridinyl]methyl]-4-piperidinemethanamine, F 13714, F13714

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About This Item

Empirical Formula (Hill Notation):
C21H25ClF2N4O
CAS Number:
Molecular Weight:
422.90
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

F13714 is an orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist (pKi = 10.12 against 0.2 nM (±)-8-OH-DPAT binding to rat cortex tissue). F13714 inhibits 100 μM forskolin-induced cAMP accumulation in human 5-HT1A-expressing HeLa cells (pIC50 = 8.67) and displays antidepressant efficacy in vivo (ED50 = 0.05 mg/kg p.o., Emax >80%; rat forced swimming). F13714 and F15599 display differential biased agonism and, when administerd in vivo, F13714 preferentially activates raphe-located autoreceptors, while F15599 preferentially activates post-synaptic heteroreceptors.
Orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist with a differential mode of action as F15599 in vitro and in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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H Iderberg et al.
Neuropharmacology, 93, 52-67 (2015-02-04)
Serotonin 5-HT1A receptor agonists reduce L-DOPA-induced dyskinesia (LID) in animal models of Parkinson's disease (PD). Here, we compared the effects of novel 5-HT1A receptor 'biased agonists' on LID in hemiparkinsonian rats. F13714 preferentially activates pre-synaptic 5-HT1A autoreceptors. F15599 preferentially activates
Adrian Newman-Tancredi et al.
Neurochemical research, 43(5), 1035-1046 (2018-03-25)
Peak-dose dyskinesia is associated with the dramatic increase in striatal dopamine levels that follows L-DOPA administration. The 'false neurotransmitter' hypothesis postulates that the latter is likely due to an aberrant processing of L-DOPA by serotonergic neurons. In keeping with this
Yulong Zhao et al.
Psychopharmacology, 236(4), 1171-1185 (2018-12-13)
Fear conditioning is an important factor in the etiology of anxiety disorders. Previous studies have demonstrated a role for serotonin (5-HT)1A receptors in fear conditioning. However, the relative contribution of somatodendritic 5-HT1A autoreceptors and post-synaptic 5-HT1A heteroreceptors in fear conditioning
M-B Assié et al.
British journal of pharmacology, 149(2), 170-178 (2006-08-22)
Desensitization of somatodendritic 5-HT(1A) receptors is involved in the mechanism of action of several antidepressants, but the rapidity of this effect and the amount of agonist stimulation needed are unclear. We evaluated the capacity of the high-efficacy 5-HT(1A) agonist, F13714
Peter Heusler et al.
Neuropharmacology, 49(7), 963-976 (2005-06-21)
The subject of the present study was the functional and pharmacological characterization of human 5-HT(1A) receptor regulation of ion channels in Xenopus oocytes. Activation of the heterologously expressed human 5-HT(1A) receptor induced two distinct currents in Xenopus oocytes, consisting of

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