| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
5-HT1 Receptor; 5-HT2C Receptor; 5-HT2A Receptor; D2 Receptor
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| ln Vitro |
G(i) protein dependence is shown in the 5-HT1A receptor agonist activity of S-14506 hydrochloride [4]. In HeLa cells treated with pertussis toxin, S-14506 hydrochloride (0.1 nM-100 μM; 10 min) exhibits strong affinity for the G-protein uncoupled state of the 5-HT receptor [4].
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| ln Vivo |
Apomorphine-resistant (0.75 mg/kg, sc) sensors' olfactory detection and climbing are dose-restrained by S-14506 hydrochloride (0.2-3.38 mg/kg; IP; single dose). In the lift swimming test, S-14506 Hydrochloride Butopamine D2 Receptor (0.63 mg/kg; SC; single dose) is active. It has the ability to produce lifting and immobility [2].
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| Enzyme Assay |
In vitro radioligand binding studies indicated S 14506 to bind with high affinity and in an apparently competitive manner to 5-HT1A sites, while having much less affinity for other 5-HT binding sites. S 14506 demonstrated exceptional anxiolytic potential in the pigeon conflict procedure; the magnitude of its effects exceeded that of the other 5-HT1A ligands 8-hydroxy-2-(n-propylamino) tetralin (8-OH-DPAT), (+)-flesinoxan, buspirone, and BMY 7378. The anticonflict action of S 14506 was antagonized by the 5-HT1A antagonist (–)-alprenolol. Like the prototypical 5-HT1A agonist 8-OH-DPAT, S 14506 induced forepaw treading, hypothermia and spontaneous tail flicks, antagonized morphine-induced analgesia, and produced stimulus generalization in rats discriminating 8-OH-DPAT from saline. The apparent in vivo efficacy of the 5-HT1A ligands in stimulating corticosterone release varied as follows: S 14506 > 8-OH-DPAT > (+)-flesinoxan > buspirone > BMY 7378.[2]
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| Animal Protocol |
Animal/Disease Models: Male Swiss albino mouse (25-30 g) and male Wistar rat (170-230 g) [2]
Doses: 0.2 mg/kg, 0.8 mg/kg, 3.2 mg/kg, 3.8 mg/kg Route of Administration: IP; single dose, 30 minutes before testing Experimental Results: Inhibition of dopamine agonist-induced stereotypic climbing and sniffing behaviors as well as spontaneous behaviors in mice. Animal/Disease Models: Male Wistar rat (200-220 g) [3] Doses: 0.01 mg/kg, 0.63 mg/kg Route of Administration: SC; and the antagonist was administered 30 minutes after the agonist. Experimental Results: Induced rat dose-dependent sexual activity. The apparent in vivo efficacy of the 5-HT1A ligands in stimulating corticosterone release varied as follows: S 14506 > 8-OH-DPAT > (+)-flesinoxan > buspirone > BMY 7378. This rank order corresponded with the rank order of magnitude of the anxiolytic action which the same compounds produced in the pigeon conflict procedure. The rank order of in vivo potency of these compounds in producing 5-HT1A agonist actions in rodents. (i.e., S 14506) > 8-OH-DPAT > (+)-flesinoxan > bus-pirone > BMY 7378) also corresponded with their rank order of potency in producing anticonflict effects. The data characterize S 14506 as an extremely potent, orally active, high-efficacy agonist at 5-HTl1A receptors that demonstrates exceptional anxiolytic potential in the pigeon conflict procedure. The results provide strong evidence that the activation of central nervous system (CNS) 5-HT1A receptors yields marked anticonflict effects and that the anxiolytic potential of 5-HT1A ligands is proportional to their efficacy at 5-HT1A re-ceptors. [2] |
| References |
[1]. Protais P, et al. Dopamine receptor antagonist properties of S 14506, 8-OH-DPAT, raclopride and clozapine in rodents. Eur J Pharmacol. 1994 Dec 12;271(1):167-77.
[2]. Francis C. Colpaert, et al. S 14506: A novel, potent, high-efficacy 5-HT1A agonist and potential anxiolytic agent. 1992, 21-48. [3]. Schreiber R, et al. The potent activity of the 5-HT1A receptor agonists, S 14506 and S 14671, in the rat forced swim test is blocked by novel 5-HT1A receptor antagonists. Eur J Pharmacol. 1994 Dec 27;271(2-3):537-41. [4]. Assié MB, et al. Correlation between low/high affinity ratios for 5-HT(1A) receptors and intrinsic activity. Eur J Pharmacol. 1999 Dec 10;386(1):97-103. |
| Additional Infomation |
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+).
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| Molecular Formula |
C24H27CLFN3O2
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|---|---|
| Molecular Weight |
443.94148850441
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| Exact Mass |
443.177
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| Elemental Analysis |
C, 64.93; H, 6.13; Cl, 7.99; F, 4.28; N, 9.47; O, 7.21
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| CAS # |
286369-38-8
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| Related CAS # |
135722-25-7;286369-38-8 (HCl);
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| PubChem CID |
131905
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.COC1C=CC2=C(C(N3CCN(CCNC(C4=CC=C(F)C=C4)=O)CC3)=CC=C2)C=1
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| InChi Key |
HWLZKPKZVOLFGK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26FN3O2.ClH/c1-30-21-10-7-18-3-2-4-23(22(18)17-21)28-15-13-27(14-16-28)12-11-26-24(29)19-5-8-20(25)9-6-19;/h2-10,17H,11-16H2,1H3,(H,26,29);1H
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| Chemical Name |
4-fluoro-N-[2-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]ethyl]benzamide;hydrochloride
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| Synonyms |
S 14506 HCl; S14506HCl; S14506 HCl; S 14506 hydrochloride; 135721-98-1; 286369-38-8; S 14506; 4-FLUORO-N-[2-[4-(7-METHOXY-1-NAPHTHALENYL)-1-PIPERAZINYL]ETHYL]BENZAMIDE HYDROCHLORIDE; S-14506 Hydrochloride; S14506Hydrochloride; S14506 hydrochloride; S-14506.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~563.14 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2526 mL | 11.2628 mL | 22.5256 mL | |
| 5 mM | 0.4505 mL | 2.2526 mL | 4.5051 mL | |
| 10 mM | 0.2253 mL | 1.1263 mL | 2.2526 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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