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S-14671 is a naphthylpiperazine derivative … S-14671 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). It displays only low and non-significant affinity for 5-HT1B and 5-HT3 sites. In producing 5-HT1A-mediated effects such as hypothermia and spontaneous tail flicks in rodents, S-14671 is active at doses as low as 5 µg subcutaneously, and is about 10-fold more potent than 8-OH-DPAT and 100-fold more potent than flesinoxan and buspirone. Other 5-HT1A-mediated effects of S-14671 include induction of flat-body posture, corticosterone secretion, inhibition of morphine-induced antinociception, and attenuation of the electrical activity of the dorsal raphe nucleus. S-14671 has been found to possess powerful efficacy in the rodent forced swim test and in the pigeon , indicating marked antidepressant and anxiolytic effects, respectively, of which are also 5-HT1A-mediated. It has never been trialed in humans, perhaps due to its potency being too great.erhaps due to its potency being too great.
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Skeletal formula of S-14671
, Space-filling model of the S-14671 molecule
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none
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N-{2-[4-piperazin-1-yl]ethyl}thiophene-2-carboxamide
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25
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| rdfs:comment |
S-14671 is a naphthylpiperazine derivative … S-14671 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). It displays only low and non-significant affinity for 5-HT1B and 5-HT3 sites. S-14671 has been found to possess powerful efficacy in the rodent forced swim test and in the pigeon , indicating marked antidepressant and anxiolytic effects, respectively, of which are also 5-HT1A-mediated. It has never been trialed in humans, perhaps due to its potency being too great.erhaps due to its potency being too great.
|
| rdfs:label |
S-14671
|
