LY 272015 hydrochlorideHigh affinity 5-HT2B antagonist; orally active CAS# 172895-15-7 |
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Quality Control & MSDS
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| Cas No. | 172895-15-7 | SDF | Download SDF |
| PubChem ID | 9929423 | Appearance | Powder |
| Formula | C21H25ClN2O2 | M.Wt | 372.89 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 10 mM in ethanol | ||
| Chemical Name | 1-[(3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;hydrochloride | ||
| SMILES | CC1=CC2=C(C=C1)NC3=C2CCNC3CC4=CC(=C(C=C4)OC)OC.Cl | ||
| Standard InChIKey | BKAZOTIBKRWLQA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H24N2O2.ClH/c1-13-4-6-17-16(10-13)15-8-9-22-18(21(15)23-17)11-14-5-7-19(24-2)20(12-14)25-3;/h4-7,10,12,18,22-23H,8-9,11H2,1-3H3;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 | High affinity 5-HT2B receptor antagonist that displays selectivity over 5-HT2A and 5-HT2C receptors (Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively). Orally active. |
LY 272015 hydrochloride Dilution Calculator
LY 272015 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6818 mL | 13.4088 mL | 26.8176 mL | 53.6351 mL | 67.0439 mL |
| 5 mM | 0.5364 mL | 2.6818 mL | 5.3635 mL | 10.727 mL | 13.4088 mL |
| 10 mM | 0.2682 mL | 1.3409 mL | 2.6818 mL | 5.3635 mL | 6.7044 mL |
| 50 mM | 0.0536 mL | 0.2682 mL | 0.5364 mL | 1.0727 mL | 1.3409 mL |
| 100 mM | 0.0268 mL | 0.1341 mL | 0.2682 mL | 0.5364 mL | 0.6704 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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Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network.[Pubmed:21789169]
PLoS One. 2011;6(7):e21395.
Neurons of the respiratory network in the lower brainstem express a variety of serotonin receptors (5-HTRs) that act primarily through adenylyl cyclase. However, there is one receptor family including 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptors that are directed towards protein kinase C (PKC). In contrast to 5-HT(2A)Rs, expression and function of 5-HT(2B)Rs within the respiratory network are still unclear. 5-HT(2B)R utilizes a Gq-mediated signaling cascade involving calcium and leading to activation of phospholipase C and IP3/DAG pathways. Based on previous studies, this signal pathway appears to mediate excitatory actions on respiration. In the present study, we analyzed receptor expression in pontine and medullary regions of the respiratory network both at the transcriptional and translational level using quantitative RT-PCR and self-made as well as commercially available antibodies, respectively. In addition we measured effects of selective agonists and antagonists for 5-HT(2A)Rs and 5-HT(2B)Rs given intra-arterially on phrenic nerve discharges in juvenile rats using the perfused brainstem preparation. The drugs caused significant changes in discharge activity. Co-administration of both agonists revealed a dominance of the 5-HT(2B)R. Given the nature of the signaling pathways, we investigated whether intracellular calcium may explain effects observed in the respiratory network. Taken together, the results of this study suggest a significant role of both receptors in respiratory network modulation.
In vivo modulation of vagal-identified dorsal medullary neurones by activation of different 5-Hydroxytryptamine(2) receptors in rats.[Pubmed:11090119]
Br J Pharmacol. 2000 Dec;131(7):1445-53.
1. In in vivo experiments, DOI (a 5-HT(2) receptor agonist), MK-212 (a 5-HT(2C) receptor agonist), and BW-723C86 (a 5-HT(2B) receptor agonist) were applied by ionophoresis to neurones in the rat nucleus tractus solitarius (NTS) receiving vagal afferent input. 2. The majority of the putative 'monosynaptically' vagal activated cells were inhibited by both MK-212 (4/6) and DOI (2/4), but unaffected by BW-723C86 (12/14). In contrast, 'polysynaptically' activated NTS cells were excited by both BW-723C86 (13/19) and DOI (9/10). Inactive 'intermediate' cells were inhibited by BW-723C86 (9/12), MK-212 (5/6) and DOI (3/4), whilst active cells of this group were excited by BW-723C86 (7/13) and DOI (5/5). 3. The selective 5-HT(2B) receptor antagonist LY-202715 significantly reduced the excitatory actions of BW-723C86 on 'intermediate' and 'polysynaptic' cells (13/13), but not the inhibitory effects observed on inactive Group 2 cells (n=5) whereas the selective 5-HT(2C) receptor antagonist RS-102221 reversed the inhibitory effects of MK-212 and DOI on 'monosynaptic and 'intermediate' neurones. 4. Cardio-pulmonary afferent stimulation inhibited two of four putative 'monosynaptically' activated calls and all four inactive intermediate cells. These were also inhibited by DOI and MK-212. In contrast, cardio-pulmonary afferents excited all five active intermediate cells and all six putative 'polysynaptically' activated NTS cells, while all were also previously excited by BW-723C86 and/or DOI. 5. In conclusion, these data demonstrate that neurones in the NTS are affected differently by 5-HT(2) receptor ligands, in regard of their vagal postsynaptic location, the type of cardio-pulmonary afferent they receive and the different 5-HT(2) receptors activated.
