| Chemical Properties | Back Directory | [storage temp. ]
Desiccate at RT | [solubility ]
Soluble to 10 mM in ethanol and to 100 mM in DMSO | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
S 14506 Hydrochloride is a highly potent selective 5-HT1A receptor full agonist and is involved in neuromodulation as well as in treatment of hypertension | [Definition]
ChEBI:4-fluoro-N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}benzamide hydrochloride is a hydrochloride salt that is obtained by reaction of 4-fluoro-N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}benzamide with one equivalent of hydrogen chloride. Highly potent selective 5-HT1A receptor full agonist (pKi values are 9.0, 6.6, 7.5, 6.6 and < 6.0 for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT2 and 5-HT3 receptors respectively). Possibly binds between the agonist binding site and the G protein interaction switch site, affecting the activation mechanism, and may display positive cooperativity. Anxiolytic following central administration in vivo. It has a role as a serotonergic agonist and an anxiolytic drug. It contains a 4-fluoro-N-{2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl}benzamide(1+). | [in vivo]
S-14506 hydrochloride (0.2-3.38 mg/kg; IP; single dose) dose dependently antagonizes Apomorphine (0.75 mg/kg, s.c.) induced stereotyped climbing and sniffing in mice. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors[2].
S-14506 hydrochloride (0.63 mg/kg; SC; single dose) is active in forced swimming test in rats. It induces imobility in rats[3].
| Animal Model: | Male swiss albino mice (25-30 g) and male Wistar rats (170-230 g)[2] | | Dosage: | 0.2 mg/kg, 0.8 mg/kg, 3.2 mg/kg, 3.8 mg/kg | | Administration: | IP; single dose, 30 min before test | | Result: | Inhibited stereotyped climbing and sniffing behaviours induced by dopamine agonists in mice and on spontaneous behaviours. |
| Animal Model: | Male Wistar rats (200-220 g)[3] | | Dosage: | 0.01 mg/kg, 0.63 mg/kg | | Administration: | SC; and gave antagonist 30 min after agonist | | Result: | Induced a dose-dependent imobility in rats. |
| [IC 50]
5-HT1 Receptor; 5-HT2A Receptor; 5-HT2C Receptor; D2 Receptor | [storage]
Desiccate at RT |
|
|