NAD 299 hydrochlorideSelective, high affinity 5-HT1A antagonist CAS# 184674-99-5 |
- SU14813
Catalog No.:BCC1971
CAS No.:627908-92-3
Quality Control & MSDS
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| Cas No. | 184674-99-5 | SDF | Download SDF |
| PubChem ID | 90488823 | Appearance | Powder |
| Formula | C18H24ClFN2O2 | M.Wt | 354.85 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO | ||
| Chemical Name | (3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide;hydrochloride | ||
| SMILES | C1CC(C1)N(C2CCC2)C3CC4=C(C=CC(=C4OC3)F)C(=O)N.Cl | ||
| Standard InChIKey | GSZJANKLCPHEEX-BTQNPOSSSA-N | ||
| Standard InChI | InChI=1S/C18H23FN2O2.ClH/c19-16-8-7-14(18(20)22)15-9-13(10-23-17(15)16)21(11-3-1-4-11)12-5-2-6-12;/h7-8,11-13H,1-6,9-10H2,(H2,20,22);1H/t13-;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro). Enhances the action of selective 5-HT reuptake inhibitors and reverses citalopram-induced inhibition of serotonergic cell firing. |
NAD 299 hydrochloride Dilution Calculator
NAD 299 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8181 mL | 14.0905 mL | 28.1809 mL | 56.3618 mL | 70.4523 mL |
| 5 mM | 0.5636 mL | 2.8181 mL | 5.6362 mL | 11.2724 mL | 14.0905 mL |
| 10 mM | 0.2818 mL | 1.409 mL | 2.8181 mL | 5.6362 mL | 7.0452 mL |
| 50 mM | 0.0564 mL | 0.2818 mL | 0.5636 mL | 1.1272 mL | 1.409 mL |
| 100 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.5636 mL | 0.7045 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The 5-HT(1A) receptor antagonist robalzotan completely reverses citalopram-induced inhibition of serotonergic cell firing.[Pubmed:10528148]
Eur J Pharmacol. 1999 Oct 8;382(2):133-8.
5-HT(1A) receptor antagonists have been suggested to increase the efficacy of selective serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitors in the treatment of depression by enhancing the increase in brain 5-HT induced by 5-HT reuptake blockade. Here, the novel 5-HT(1A) receptor antagonist robalzotan [(R)-3-N, N-dicyclobutylamino-8-fluoro-3, 4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R, 3R) tartrate monohydrate] (12.5, 25, 50, 100 microg/kg, i.v.) was found to completely reverse the acute inhibitory effect of citalopram (300 microg/kg i.v.) or paroxetine (100 microg/kg, i.v.) on the activity of 5-HT neurons in the dorsal raphe nucleus in rats. Robalzotan (5, 50 microg/kg, i.v.) by itself increased the firing rate of the majority of 5-HT cells studied. The present results suggest that robalzotan may indeed augment the increases in 5-HT output induced by selective 5-HT reuptake inhibitors by antagonizing the feedback inhibition of 5-HT cell firing produced by such drugs. Thus, robalzotan may be effective by enhancing the action of selective 5-HT reuptake inhibitors or as monotherapy in the treatment of depression.
Differential regional antagonism of 8-OH-DPAT-induced decrease in serotonin synthesis by two 5-HT1A receptor antagonists.[Pubmed:9652362]
Eur J Pharmacol. 1998 Apr 10;346(2-3):209-15.
The effects of two 5-HT1A receptor antagonists, (R)-3-N, N-dicyclobutylamino-8-fluoro-3,4-dihydro-2 H-1-benzopyran-5-carboxamide hydrogen (2 R,3 R)-tartrate monohydrate (NAD-299) and N-(2-(1-(2-methoxyphenyl)-piperazinyl))ethyl)-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) on the decrease in 5-hydroxytryptophan (5-HTP) accumulation evoked by (RS)-2-dipropylamino-8-hydroxy-1,2,3,4-tetrahydronaphthalene (8-OH-DPAT) in rats treated with the decarboxylase inhibitor, 3-hydroxyphenylhydrazine (NSD 1015) were studied in four rat brain regions: hippocampus, hypothalamus, striatum and frontal cortex. Dose-response studies revealed differential effects of both antagonists in the areas examined. Both antagonists were significantly more potent in antagonising the effect of 0.30 and 0.76 micromol/kg s.c. 8-OH-DPAT in hippocampus than in hypothalamus, striatum and frontal cortex in mentioned order. This order of potency was the opposite to that found for 8-OH-DPAT in decreasing the 5-HTP accumulation. Since previous studies by others have indicated that the reserve of somatodendritic 5-HT1A receptors is greater in dorsal raphe nucleus innervating frontal cortex and striatum than in median raphe nucleus which mainly innervates hippocampus, the observed different regional potency of the two 5-HT1A receptor antagonists may be explained by this difference in the 5-HT1A receptor reserve.
