S-14,671

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S-14,671
File:S-14,671-structure.png
Systematic (IUPAC) name
N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}thiophene-2-carboxamide
Identifiers
CAS Number 135722-27​-9
ATC code none
PubChem CID 131907
ChemSpider 116529
Chemical data
Formula C22H25N3O2S
Molar mass 395.52 g/mol[[Script error: No such module "String".]]
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S-14,671 is a naphthylpiperazine derivative which acts as a 5-HT1A receptor agonist (pKi = 9.3) with high efficacy and exceptional in vivo potency, and also as a 5-HT2A and 5-HT2C receptor antagonist (both are pKi = 7.8).[1][2] It displays only low and non-significant affinity for 5-HT1B and 5-HT3 sites.[2]

In producing 5-HT1A-mediated effects such as hypothermia and spontaneous tail flicks in rodents, S-14,671 is active at doses as low as 5 mcg s.c., and is about 10-fold more potent than 8-OH-DPAT and 100-fold more potent than flesinoxan and buspirone.[1][2] Other 5-HT1A-mediated effects of S-14,671 include induction of flat-body posture, corticosterone secretion, inhibition of morphine-induced antinociception, and attenuation of the electrical activity of the dorsal raphe nucleus.[2]

S-14,671 has been found to possess powerful efficacy in the rodent forced swim test and in the pigeon conflict test, indicating marked antidepressant and anxiolytic effects, respectively, of which are also 5-HT1A-mediated.[3][4] It has never been trialed in humans, perhaps due to its potency being too great.[citation needed]

See also

References

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GABAA PAMs
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)

  1. ↑ 1.0 1.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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  4. ↑ Schreiber R, Brocco M, de Ladonchamps BL, Millan MJ (1995). "Involvement of 5-HT1A receptors in the anxiolytic action of S 14671 in the pigeon conflict test". Pharmacology, Biochemistry, and Behavior. 51 (2-3): 211–5. PMID 7667330. 
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