CAS 182563-08-2|LY 334370

Introduction:Basic information about CAS 182563-08-2|LY 334370, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameLY 334370
CAS Number182563-08-2Molecular Weight351.42
Density/Boiling Point504.1ºC at 760 mmHg
Molecular FormulaC21H22FN3OMelting Point/
MSDS/Flash Point258.7ºC

Names

Name4-fluoro-N-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]benzamide
SynonymMore Synonyms

LY 334370 BiologicalActivity

DescriptionLY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
Related CatalogSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease
Target

Ki: 1.6 nM (5-HT1F)

In VitroLY334370 has no vasoconstrictor effects on human cerebral arteries in vitro until a dose of 10-5 M, at which it produces a contraction of 8.5±5.7%; however, this is not significant[1].
In VivoFollowing intravenous administration of LY334370 at 3 mg/kg (n=3) or 10 mg/kg (n=6) electrical stimulation evokes an increase in dural blood vessel diameter of 135±6% and 106±11%, respectively, which is not significantly different from the respective control values. LY334370 has no effect on dural blood vessel diameter per se, since the actualdural blood vessel diameter is 43±4 arbitrary units before drug and 43±4 arbitrary units 15 min after injection of LY334370 (10 mg/kg)[1].
Cell AssayHuman cerebral artery is used in this study. Segments are prepared as previously described, but briefly they are placed in a buffer solution containing (mM) NaCl 119, NaHCo3 15, KCl 4.6, CaCl2 1.5, NaH2PO4 1.2, MgCl2 1.2, and glucose 5.5. Sections of vessel about 0.5 mm in diameter and 1 to 2 mm in length are mounted in a temperature-controlled tissue bath (37°C) containing buffer solution bubbled with 95% O2 and 5% CO2. The vessel segments are given a tension of 4 mN and allowed to stabilize at this tension for 1 to 1.5 h. Vessel reactivity is tested by exposure to 60 mM KCl. This is done twice for each segment and only if the response is similar to the segment used for LY334370 testing. Responses to LY334370 is calculated as a percentage of the maximum KC1 response[1].
Animal AdminMale Sprague-Dawley rats (300 to 400 g) are anesthetized with pentobarbitone sodium. Briefly, a femoral artery and both femoral veins are cannulated for blood pressure recording, intravenous injection of drugs and infusion of anesthetic, respectively. Rats are placed in a stereotaxic frame, the skull exposed and thinned by drilling to reveal a branch of the middle meningeal artery whose diameter is measured continuously through the intact skull using intravital microscopy and a video dimension analyser. Neurogenic vasodilation is evoked using a bipolar stimulating electrode placed on the surface of the cranial window approximately 200 μM from the vessel of interest. A control vasodilation response to electrical stimulation is produced and 5 min later LY334370 (3 or 10 mg/kg, iv.) is given and the electrical stimulation repeated after a further 15 min. The mean maximum percentage increase in dural vessel diameter relative to pre-stimulus baseline is calculated for each response and comparisons of vasodilation responses evoked in the presence or absence of LY334370 are made by analysis of variance (ANOVA) followed by paired t-tests[1].
References

[1]. Shepheard S, et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Cephalalgia. 1999 Dec;19(10):851-8.

Chemical & Physical Properties

Boiling Point504.1ºC at 760 mmHg
Molecular FormulaC21H22FN3O
Molecular Weight351.42
Flash Point258.7ºC
PSA48.13000
LogP5.18140
InChIKeyMDMJLMDBRQXOOI-UHFFFAOYSA-N
SMILESCN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc23)CC1
Storage condition2-8℃

Synonyms

LY 334370
LY334370
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