SB 203186 hydrochloride5-HT4 antagonist CAS# 207572-69-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 207572-69-8 | SDF | Download SDF |
| PubChem ID | 9926639 | Appearance | Powder |
| Formula | C16H21ClN2O2 | M.Wt | 308.81 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water | ||
| Chemical Name | 2-piperidin-1-ylethyl 1H-indole-3-carboxylate;hydrochloride | ||
| SMILES | C1CCN(CC1)CCOC(=O)C2=CNC3=CC=CC=C32.Cl | ||
| Standard InChIKey | LYMBEMCUJNDSBZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H20N2O2.ClH/c19-16(20-11-10-18-8-4-1-5-9-18)14-12-17-15-7-3-2-6-13(14)15;/h2-3,6-7,12,17H,1,4-5,8-11H2;1H | ||
| 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 | Potent 5-HT4 receptor antagonist with high affinity for human atrial 5-HT4 receptors. |
SB 203186 hydrochloride Dilution Calculator
SB 203186 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2382 mL | 16.1912 mL | 32.3824 mL | 64.7647 mL | 80.9559 mL |
| 5 mM | 0.6476 mL | 3.2382 mL | 6.4765 mL | 12.9529 mL | 16.1912 mL |
| 10 mM | 0.3238 mL | 1.6191 mL | 3.2382 mL | 6.4765 mL | 8.0956 mL |
| 50 mM | 0.0648 mL | 0.3238 mL | 0.6476 mL | 1.2953 mL | 1.6191 mL |
| 100 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.6476 mL | 0.8096 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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Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186.[Pubmed:8750913]
Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):28-35.
We investigated the blockade of the positive inotropic effects of 5-hydroxytryptamine (5-HT) by SB 203 186 (piperidinoethyl-indole-3-carboxylate hydrochloride) and its affinity for 5-HT4 receptors of human right atrium and piglet left atrium. We also compared the blocking effects of SB 203 186 against 5-HT-evoked tachycardia in anaesthetised adult Yucatan minipigs as well as new-born Camborough piglets. SB 203 186 caused competitive antagonism of the positive inotropic effects of 5-HT in electrically paced atrial preparations of man (pKB = 8.9) and piglet (pKB = 8.5) at concentrations (up to 0.3 micromol/l) which were devoid of depressant or stimulant effects. The affinity of SB 203 186 for atrial 5-HT4 receptors was 30-160 times higher than that of tropisetron. 5-HT caused tachycardia with similar potency and efficacy in Yucatan minipigs and new-born Camborough piglets. SB 203 186 (0.1-3 mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetised Yucatan minipigs or new-born Camborough piglets with similar potency. The blocking potency of SB 203 186 in Yucatan minipigs was 17 times higher than that of tropisetron. Intraduodenally administered SB 203 186 (0.3-3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg. The antagonism produced by the SB 203 186 administration in new-born Camborough piglets was dose-related and threefold greater through the intravenous route than through the intraduodenal route. We conclude that SB 203 186 is an antagonist with nanomolar affinity for both human and porcine atrial 5-HT4 receptor. The in vivo results demonstrate that the sinoatrial 5-HT4 receptors function is similar in new-born Camborough piglets and adult Yucatan minipigs. Both porcine breeds are valid models for human atrial 5-HT4 receptors as demonstrated with the antagonist SB 203 186.
Characterization of the 5-HT4 receptor mediating tachycardia in piglet isolated right atrium.[Pubmed:8298790]
Br J Pharmacol. 1993 Nov;110(3):1023-30.
1. In order to explore whether 5-HT4 receptor subtypes exist, we have characterized further the 5-HT4 receptor that mediates tachycardia in the piglet isolated right atrium. All experiments were carried out in the presence of propranolol (400 nM) and cocaine (6 microM). We used tryptamine derivatives, substituted benzamides and benzimidazolone derivatives as pharmacological tools. 2. Tachycardia responses to 5-hydroxytryptamine (5-HT) were mimicked by other tryptamine derivatives with the following order of potency: 5-HT > 5-methoxytryptamine alpha-methyl-5-HT = bufotenine bufotenine > 5-carboxamidotryptamine = tryptamine (after treatment with pargyline) > 5-methoxy-N,N-dimethyltryptamine > 2-methyl-5-HT. 3. The substituted benzamides were all partial agonists relative to 5-HT except (-)-zacopride which was a full agonist. The stimulant potency order was renzapride > cisapride = (-)-zacopride > metoclopramide > (+)-zacopride. 4. The benzimidazolone derivatives had contrasting effects. BIMU 8 (endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-(1-methyl(eth yl- 2-oxo-1H-benzimidazole-1-carboxamide hydrochloride) was a full agonist relative to 5-HT whilst BIMU 1 (endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-3-ethyl-2-oxo - 1H-benzimidazole-1-carboxamide hydrochloride) was a partial agonist with low intrinsic activity compared to 5-HT but had similar potency. We estimated a pKB of 7.9 for BIMU 1 antagonism of 5-HT-induced tachycardia. DAU 6215 (N-endo-8-methyl-8-azabicyclo[3.2.1]-oct-3-yl)-2,3-dihydro-2-oxo-lH-benzimidazole -l-carboxamide, hydrochloride) had no chronotropic activity and was found to be a simple competitive antagonist with a pKB of 7.15.SB 203186 (1-piperidinyl)ethyl lH-indole 3-carboxylate) was a potent antagonist with a pKB of 8.3.The affinity of SB 203186 was approximately 20 times higher than that of tropisetron (ICS 205-930;pKB= 6.9) and DAU 6215 (pKB= 7.0). GR1 13808 (([1-[2-[methylsulphonyl amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate) and SDZ 205-557 ((2-diethylaminoethyl)2-methoxy-4-amino-5-chloro-benzoate) also antagonized 5-HT-induced tachycardia but not by simple competitive blockade.6. The sinoatrial 5-HT4 receptor in the piglet has a pharmacological profile that correlates well with 5-HT4 receptors characterized in rat oesophagus, guinea-pig ileum and colon, mouse embryonic colliculi neurones and human atrium.
