LY-53857 - CAS 60634-51-7
Catalog number: 60634-51-7
Category: Inhibitor
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Molecular Formula:
C23H32N2O3
Molecular Weight:
500.58
COA:
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Targets:
5-HT Receptor
Description:
LY-53857 is a selective and potent 5-HT2 serotonin receptor antagonist. It was developed by Eli Lilly and Company.
Purity:
98%
Appearance:
White solid
Synonyms:
LY 53857; LY-53857; LY53857. 6-Methyl-1-(1-methylethyl)ergoline-8β-carboxylic acid 2-hydroxy-1-methylpropyl ester maleate salt;LY53857;Ergoline-8-carboxylic acid, 6-methyl-1-(1-methylethyl)-, 2-hydroxy-1-methylpropyl ester, (8beta)-, (Z)-2-butenedioate (1:1) (salt)
Solubility:
0.1 M HCl: 25 mg/mL
Storage:
-20°C Freezer
MSDS:
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Quality Standard:
In-house standard
Quantity:
Milligrams-Grams
Boiling Point:
554.8°C at 760 mmHg
InChIKey:
DYJVZTAMQYDCLP-VCSAJMHUSA-N
InChI:
InChI=1S/C23H32N2O3.C4H4O4/c1-13(2)25-12-16-10-21-19(18-7-6-8-20(25)22(16)18)9-17(11-24(21)5)23(27)28-15(4)14(3)26;5-3(6)1-2-4(7)8/h6-8,12-15,17,19,21,26H,9-11H2,1-5H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14?,15?,17-,19-,21-;/m1./s1
Canonical SMILES:
CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O
Current Developer:
LY-53857 was developed by Eli Lilly and Company.
1.Evidence for a 5-HT1-like receptor mediating the amplifying action of 5-HT in the rabbit ear artery.
de la Lande IS Br J Pharmacol. 1992 Sep;107(1):550-5.
1. The nature of the 5-hydroxytryptamine (5-HT) receptors which amplify the vasoconstrictor effect of methoxamine was examined in the rabbit isolated perfused ear artery with intact endothelium. Indices of amplification were leftward shifts of methoxamine dose-response (DR) curves produced by 5-HT (0.3 microM) (Method I), and the appearance of vasoconstrictor responses to 5-HT receptor agonists when methoxamine was present in a near-threshold concentration (Method II). 2. The amplifying effect of 5-HT (Method I) was unaffected by prazosin (0.08 microM), was partly depressed by 5-HT2-receptor antagonists in high concentrations (ketanserin 0.5 microM, LY53857, 1.0 microM), and was abolished by a non-selective antagonist of 5-HT1 and 5-HT2 receptors (methiothepin, 0.01 microM). 3. Amplifying potencies of agonists assessed by both Methods I and II were in the order 5-carbox-amidotryptamine (5-CT) greater than 5-HT greater than alpha-methyl 5-HT. The potency of sumatriptan (assessed by Method II only) was intermediate between those of 5-HT and alpha-methyl 5-HT. 4. Ketanserin and LY53857 inhibited the amplifying action of 5-CT to about the same extent as that of 5-HT. 5. The amplifying potencies of the agonists are in marked contrast to the reported contractile potencies in the rabbit aorta where the receptor is 5-HT2, but are almost identical with reported contractile potencies in the dog saphenous vein where the receptor is 5-HT1-like.
2.The tricyclic antidepressant clomipramine increases plasma glucose levels of mice.
Sugimoto Y;Inoue K;Yamada J J Pharmacol Sci. 2003 Sep;93(1):74-9.
Effects of the tricyclic antidepressant clomipramine on plasma glucose levels in mice were studied. Clomipramine at doses ranging 5 - 20 mg/kg elicited significant hyperglycemia in mice. Hyperglycemia elicited by clomipramine was not reduced by pretreatment with the 5-hydroxytryptamine (5-HT) depleter p-chlorophenylalanine. The 5-HT(1/2/5/7)-receptor antagonist methysergide and the 5-HT(2A/2B/2C)-receptor antagonist LY 53857 enhanced clomipramine-induced hyperglycemia, while the 5-HT(1A/1B)-receptor antagonist (-)-propranolol and the 5-HT(3/4)-receptor antagonist tropisetron did not affect it. The 5-HT(2B/2C)-receptor antagonist SB 206553 facilitated hyperglycemia induced by clomipramine, although the 5-HT(2A)-receptor antagonist ketanserin was without effect. Clomipramine-induced hyperglycemia was reduced by prior adrenalectomy. These results suggest that clomipramine induces hyperglycemia in mice by blocking the 5-HT(2B )and/or 5-HT(2C) receptors, which results in facilitation of adrenaline release.
3.Comparison between ketanserin and LY 53857 on vascular and cardiac 5-HT2 and alpha 1-adrenergic receptors in the pithed rat.
Dabiré H;Chaouche-Teyara K;Cherqui C;Fournier B;Schmitt H Arch Int Pharmacodyn Ther. 1990 Jul-Aug;306:57-64.
In normotensive pithed rats, both ketanserin and LY 53857 potently antagonized the increase in blood pressure induced by 5-HT in a noncompetitive manner. However, LY 53857 differs from ketanserin in that it shifts the pressor dose-response curve to 5-HT in a parallel way at low doses but in a noncompetitive way at higher doses. Ketanserin and LY 53857 were weak antagonists of the pressor effects of phenylephrine. LY 53857 was more potent and more selective than ketanserin for 5-HT2 vs alpha 1-adrenergic receptors.
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