Synonym
LY310762; LY 310762; LY-310762; LY310762 HCl.
IUPAC/Chemical Name
1-(2-(4-(4-fluorobenzoyl)piperidin-1-yl)ethyl)-3,3-dimethylindolin-2-one hydrochloride
InChi Key
BOCLFQZPFYNVFD-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H27FN2O2.ClH/c1-24(2)20-5-3-4-6-21(20)27(23(24)29)16-15-26-13-11-18(12-14-26)22(28)17-7-9-19(25)10-8-17;/h3-10,18H,11-16H2,1-2H3;1H
SMILES Code
O=C1N(CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)C4=C(C=CC=C4)C1(C)C.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor.
In vivo activity:
This study aimed to investigate whether, behind the predominant serotonergic vasoconstrictor action, THE 5-HT system may exert renal vasodilator actions, and, if so, characterize the 5-HT receptors and possible indirect pathways. Renal perfusion pressure (PP), systemic blood pressure (SBP) and heart rate (HR) measurement in in situ autoperfused rat kidney was determined in phenylephrine infused rats. These vasodilator responses were potentiated by 5-HT₂ antagonism (ritanserin, 1 mg/kg i.v.), whereas the responses were abolished by 5-HT₁ /₇ antagonist (methiothepin, 100 μg/kg i.v.) or 5-HT1D antagonist (LY310762, 1 mg/kg i.v.).
Reference: Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. https://pubmed.ncbi.nlm.nih.gov/25854421/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
3.0 |
6.96 |
| DMSO |
16.7 |
38.76 |
| DMSO:PBS (pH 7.2) (1:6) |
0.1 |
0.32 |
| Ethanol |
0.5 |
1.16 |
| Water |
4.3 |
10.00 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
430.95
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. García-Pedraza JÁ, García M, Martín ML, Morán A. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. doi: 10.1111/1440-1681.12397. PMID: 25854421.
2. Choi IS, Cho JH, An CH, Jung JK, Hur YK, Choi JK, Jang IS. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67. doi: 10.1111/j.1476-5381.2012.01964.x. PMID: 22462474; PMCID: PMC3481043.
In vivo protocol:
1. García-Pedraza JÁ, García M, Martín ML, Morán A. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. doi: 10.1111/1440-1681.12397. PMID: 25854421.
2. Choi IS, Cho JH, An CH, Jung JK, Hur YK, Choi JK, Jang IS. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67. doi: 10.1111/j.1476-5381.2012.01964.x. PMID: 22462474; PMCID: PMC3481043.
1: García-Pedraza JÁ, García M, Martín ML, Morán A. 5-HT(1D) receptor inhibits renal sympathetic neurotransmission by nitric oxide pathway in anesthetized rats. Vascul Pharmacol. 2015 May 21. pii: S1537-1891(15)00105-6. doi: 10.1016/j.vph.2015.05.003. [Epub ahead of print] PubMed PMID: 26003124.
2: García-Pedraza JÁ, García M, Martín ML, Morán A. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. doi: 10.1111/1440-1681.12397. PubMed PMID: 25854421.
3: García-Pedraza JÁ, García M, Martín ML, Gómez-Escudero J, Rodríguez-Barbero A, Román LS, Morán A. Peripheral 5-HT₁D and 5-HT₇ serotonergic receptors modulate sympathetic neurotransmission in chronic sarpogrelate treated rats. Eur J Pharmacol. 2013 Aug 15;714(1-3):65-73. doi: 10.1016/j.ejphar.2013.05.045. Epub 2013 Jun 11. PubMed PMID: 23769743.
4: Choi IS, Cho JH, An CH, Jung JK, Hur YK, Choi JK, Jang IS. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67. doi: 10.1111/j.1476-5381.2012.01964.x. PubMed PMID: 22462474; PubMed Central PMCID: PMC3481043.
5: Pullar IA, Boot JR, Broadmore RJ, Eyre TA, Cooper J, Sanger GJ, Wedley S, Mitchell SN. The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig. Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93. PubMed PMID: 15189767.
