LY334370 - 5-HT Receptor Agonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY334370Cat. No.: HY-103107CAS No.: 182563-08-2分式: CHFNO分量: 351.42作靶點: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實

2、驗 DMSO : 55.5 mg/mL (157.93 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8456 mL 14.2280 mL 28.4560 mL5 mM 0.5691 mL 2.8456 mL 5.6912 mL10 mM 0.2846 mL 1.4228 mL 2.8456 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 LY334370個選擇

3、性的 5-HT1F 受體激動劑，其 Ki 值為 1.6 nM。IC50 & Target Ki: 1.6 nM (5-HT1F)體外研究 LY334370 has no vasoconstrictor effects on human cerebral arteries in vitro until a dose of 10-5 M, at whichit produces a contraction of 8.55.7%; however, this is not significant 1.體內(nèi)研究Following intravenous administration of LY3343

4、70 at 3 mg/kg (n=3) or 10 mg/kg (n=6) electrical stimulation1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEevokes an increase in dural blood vessel diameter of 1356% and 10611%, respectively, which is notsignificantly different from the respective control values. LY334370 has no effect on dural bl

5、ood vesseldiameter per se, since the actualdural blood vessel diameter is 434 arbitrary units before drug and 434arbitrary units 15 min after injection of LY334370 (10 mg/kg) 1.PROTOCOLCell Assay 1 Human cerebral artery is used in this study. Segments are prepared as previously described, but briefl

6、y theyare 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 aremounted in a temperature-controlled tissue bath (37C) containing buffer solution bubbled with

7、95% O2 and5% CO2. The vessel segments are given a tension of 4 mN and allowed to stabilize at this tension for 1 to1.5 h. Vessel reactivity is tested by exposure to 60 mM KCl. This is done twice for each segment and only ifthe response is similar to the segment used for LY334370 testing. Responses t

8、o LY334370 is calculated as apercentage of the maximum KC1 response 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male Sprague-Dawley rats (300 to 400 g) are anesthetized with pentobarbitone sodium. Briefly, a femoralAdministration 1 artery a

9、nd both femoral veins are cannulated for blood pressure recording, intravenous injection of drugs andinfusion of anesthetic, respectively. Rats are placed in a stereotaxic frame, the skull exposed and thinned bydrilling to reveal a branch of the middle meningeal artery whose diameter is measured con

10、tinuously throughthe intact skull using intravital microscopy and a video dimension analyser. Neurogenic vasodilation isevoked using a bipolar stimulating electrode placed on the surface of the cranial window approximately 200 M from the vessel of interest. A control vasodilation response to electri

11、cal stimulation is produced and 5 minlater LY334370 (3 or 10 mg/kg, iv.) is given and the electrical stimulation repeated after a further 15 min. Themean maximum percentage increase in dural vessel diameter relative to pre-stimulus baseline is calculatedfor each response and comparisons of vasodilat

12、ion responses evoked in the presence or absence ofLY334370 are made by analysis of variance (ANOVA) followed by paired t-tests 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Shepheard S, et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Cephalalgia. 1999Dec;19(10):851-8.McePdfHeightCautio