OPC-14523 hydrochloride |
| رقم الكتالوجGC61889 |
هيدروكلوريد OPC-14523 هو ناهض سيغما نشط عن طريق الفم ومستقبلات 5-HT1A ، مع تقارب عالي لمستقبلات سيجما (σ1 / 2 IC50 = 47/56 نانومتر) ، مستقبلات 5-HT1A (IC50 = 2.3 نانومتر) ، و 5- ناقل HT (IC50 = 80 نانومتر)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 145969-31-9
Sample solution is provided at 25 µL, 10mM.
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OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity[1][2].
OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC50=27 nM), but it shows very weak inhibitory activity on 3H-NE and 3H-DA reuptake[1].
OPC-14523 hydrochloride (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity[1].
References:
[1]. Tottori K, et al. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001;41(8):976-988.
[2]. Bermack JE, et al. Effects of the potential antidepressant OPC-14523 [1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate] a combined sigma and 5-HT1A ligand: modulation of neuronal activity in the dorsal raphe nucleus. J Pharmacol Exp Ther. 2004;310(2):578-583.
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