| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
5-HT4 receptor (selective antagonist; no IC50/Ki/EC50 reported in this study). [2]
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| ln Vitro |
Pretreatment with SB-203186 (10 μM) increases sinus zone constriction brought on by 5-HT [2].
In isolated rat gastric circular muscle strips, pretreatment with SB 203186 HCl at 10^-6 M for 10 minutes significantly enhanced 5-HT-induced contractions in the antrum and fundus, indicating the presence of relaxant 5-HT4 receptors. In the corpus, SB 203186 HCl had no effect on 5-HT-induced contractions. [2] |
| ln Vivo |
Neonatal Canberra pigs receiving intraduodenal SB-203186 (0.3–3 mg/kg) are protected against 5-HT-induced tachycardia; the maximal blockage occurs after 20 minutes, and the dose of 0.3 mg/kg is maintained for almost three hours [1]. In anesthetized Yucatan minipigs or neonatal Canberra piglets with comparable potency, SB-203186 (0.1-3 mg/kg, intravenously) significantly counteracts 5-HT-induced tachycardia [1].
In anaesthetized adult Yucatan minipigs (11-13 kg, vagotomized, pretreated with propranolol 1 mg/kg i.v.), SB 203186 administered intravenously at cumulative doses of 0.1, 0.3, 1, and 3 mg/kg produced dose-related surmountable antagonism of 5-HT-induced tachycardia (0.3-1000 μg/kg i.v.). The apparent pA2 was 70 μg/kg (DR10 = 457 μg/kg). Tropisetron (1.7 mg/kg i.v.) produced similar antagonism to SB 203186 0.1 mg/kg. [1] In anaesthetized newborn Camborough piglets (2-5 days old, vagotomized, propranolol 1 mg/kg i.v.), SB 203186 i.v. (0.1, 0.3, 1 mg/kg) caused similar antagonism of 5-HT tachycardia (1-30 μg/kg i.v.) with apparent pA2 = 53 μg/kg and DR10 = 457 μg/kg. Intraduodenal administration (0.3, 1, 3 mg/kg) also produced dose-related blockade, but was approximately 3-fold less potent than i.v. route. [1] Time-course: After i.v. bolus of SB 203186 (0.1 mg/kg), maximal antagonism of 5-HT (10 μg/kg)-evoked tachycardia occurred within 5 min, with 50% recovery at ~30 min and full recovery by 2 h. After intraduodenal dose (0.3 mg/kg), maximal blockade was reached at 20 min, with >3 h half-recovery and only partial recovery by 3 h. [1] |
| Cell Assay |
Human right atrial appendages: Obtained from patients undergoing cardiac surgery. Strips were mounted in 50 ml organ baths containing modified Krebs solution (mmol/L: Na+ 125, K+ 5, Ca2+ 2.25, Mg2+ 0.5, Cl- 98.5, SO42- 0.5, HCO3- 29, HPO42- 1, EDTA 0.04) supplemented with fumarate 5, pyruvate 5, L-glutamate 5, glucose 10, and equilibrated with 95% O2/5% CO2 at 37°C. Tissues were paced at 2-s intervals (5 ms duration, threshold voltage). Cocaine (6 μmol/L), (±)-propranolol (400 nmol/L), and ascorbate (200 μmol/L) were present. A single cumulative concentration-effect curve to 5-HT was determined in the absence or presence of SB 203186 (preincubated ≥60 min). Responses were expressed as percentage of the increase achieved by (-)-isoprenaline (200 μmol/L). Schild regression (Arunlakshana and Schild) was used to calculate pKB. [1]
Piglet left atria: Obtained from 2-5 day old Camborough piglets under halothane anesthesia. Left atria were dissected into strips and set up as for human tissue, with additional rolipram (20 μmol/L) present. Same experimental protocol and analysis. [1] |
| Animal Protocol |
For mechanical activity measurement, rat gastric fundus, corpus, and antrum circular muscle strips were mounted in organ baths containing oxygenated Krebs-Ringer solution at 37°C under 1 g resting tension. After 60 min equilibration, SB 203186 HCl (10^-6 M) was applied 10 minutes before and during cumulative addition of 5-HT (3×10^-9 to 3×10^-4 M depending on region). Contractions were recorded isometrically and expressed relative to carbachol (10^-5 M)-induced contraction. [2]
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| Toxicity/Toxicokinetics |
At concentrations up to 0.3 μmol/L in vitro, SB 203186 was devoid of depressant or stimulant effects on atrial contractility. In vivo, SB 203186 (up to 3 mg/kg i.v.) did not significantly alter basal mean blood pressure or heart rate in either Yucatan minipigs or Camborough piglets (see Table 1). [1]
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| References |
[1]. S G Parker, et al. Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):28-35.
[2]. Tohru Komada, et al. Pharmacological characterization of 5-Hydroxytryptamine-receptor subtypes in circular muscle from the rat stomach. Biol Pharm Bull. 2007 Mar;30(3):508-13. [3]. P G McLean, et al. 5-HT4 receptor antagonist affinities of SB207710, SB205008, and SB203186 in the human colon, rat oesophagus, and guinea-pig ileum peristaltic reflex. Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):132-40. |
| Additional Infomation |
SB 203186 HCl is a selective 5-HT4 receptor antagonist. In this study, it was synthesized in‑house. Its enhancement of 5-HT-induced contractions in rat gastric antrum and fundus circular muscle suggests the presence of functional relaxant 5-HT4 receptors in these tissues. [2]
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| Molecular Formula |
C16H20CLN2O2-
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|---|---|
| Molecular Weight |
307.8
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| Exact Mass |
308.129
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| Elemental Analysis |
C, 62.23; H, 6.85; Cl, 11.48; N, 9.07; O, 10.36
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| CAS # |
207572-69-8
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| Related CAS # |
207572-69-8 (HCl);398454-65-4;
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| PubChem CID |
9926639
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
328
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C(C1=CNC2=CC=CC=C12)OCCN1CCCCC1
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| InChi Key |
LYMBEMCUJNDSBZ-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-piperidin-1-ylethyl 1H-indole-3-carboxylate;hydrochloride
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| Synonyms |
SB203186 SB-203186SB 203186 HCl SB203186 hydrochlorideSB 203186 HCl
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~323.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2489 mL | 16.2443 mL | 32.4886 mL | |
| 5 mM | 0.6498 mL | 3.2489 mL | 6.4977 mL | |
| 10 mM | 0.3249 mL | 1.6244 mL | 3.2489 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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