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LY310762

LY310762 is a 5-HT_1D antagonist with K_i of ~0.2 μM.

Catalog No.S2669

: Tel: +1-832-582-8158[email protected]

LY310762 Chemical Structure
Molecular Weight: 430.94

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

LY310762 is available in the following compound libraries:

Chemical Library (96-well) GPCR Small Molecule Compound Library (96-well) Inhibitor Library (96-well)

Product Information

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Combination Therapy

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Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	LY310762 is a 5-HT_1D antagonist with K_i of ~0.2 μM.
Targets	5-HT_1D
IC50	0.2 μM (K_i) ^[1]
In vitro	LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [³H]5-HT outflow from guinea pig cortical slices with an EC50 of 30 nM. The maximum potentiation of the potassium-induced outflow which is obtained with LY310762 is about 40%. ^[1] LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan. ^[2]
In vivo	Systemic administration of LY310762 (10 mg/kg i.p.) produces a further significant enhancement in the 5-HT response to fluoxetine (20 mg/kg i.p.) when compared to animals receiving a control vehicle injection. In fluoxetine treated animals, levels of 5-HT increases from 312±43% to a maximum of 683% after LY310762. In control animals, levels of 5-HT remains unchanged (250%). LY310762 administered alone also significantly increases basal levels of 5-HT above vehicle controls, reaching a maximum of 258% compared to the pre-injection control. ^[1]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay:
^[1]

[³H]-5-HT outflow from guinea pig cortical slices	Male Dunkin Hartley Guinea Pigs (350-400 g) are killed by asphyxiation with CO₂ and their brains rapidly removed. Cortical slices (350 × 350 μm) are prepared, washed once in basal buffer (10 mM HEPES, 133 mM NaCl, 4.8 mM KCl, 1.2 mM KH₂PO₄, 1.2 mM MgSO₄, 1.5 mM CaCl₂, 11.1 mM glucose, 10 μM pargyline pH 7.4) and incubated in basal buffer at 25 mg/mL wet weight with [³H]5-HT (50 nM) for 30 minutes at 37 °C. The slices are washed three times in basal buffer and transferred to baskets (10 mm i.d. polypropylene tubes with 150 μm nylon mesh bases) at approximately 5 mg wet weight per basket. The baskets are used to transfer the tissue between the washing and release buffers. In order to obtain stable baseline release, the slices are incubated for 11 minutes in basal buffer (0.5 mL), transferred for 4 minutes to a second tube containing basal buffer (0.5 mL) and then, for a further 4 minutes, to basal buffer (0.5 mL) or to a buffer in which NaCl has been substituted with KCl, on an equimolar basis, to give a KCl concentration of 30 mM (release sample). All buffers used in the 11 minutes and the two 4 minutes incubations contained 1 μM paroxetine. Following the incubations, the tissue is digested with Soluene-350 (0.7 mL) and the baskets rinsed with propan-2-ol (0.7 mL). The tritium label in the tissue samples and in the buffers from the three incubation periods is estimated by liquid scintillation spectroscopy. LY310762 being tested is present throughout the three incubation periods and is tested in six replicates. The basal release is measured in four replicates and the control release in eight replicates. The tritium label in the release sample is expressed as the percentage of the total tritium in the tissue at the time the sample is collected (% fractional release). Stimulated release is calculated as the % fractional release produced by the high potassium buffer minus that of basal release. The percentage increase in release produced by LY310762 is calculated as the increase over the control stimulated release, where the control release is 100%. For individual experiments the mean of the replicate data is calculated. The results are the means and standard errors of at least three separate experiments.

[³H]-5-HT outflow from guinea pig cortical slices

Male Dunkin Hartley Guinea Pigs (350-400 g) are killed by asphyxiation with CO₂ and their brains rapidly removed. Cortical slices (350 × 350 μm) are prepared, washed once in basal buffer (10 mM HEPES, 133 mM NaCl, 4.8 mM KCl, 1.2 mM KH₂PO₄, 1.2 mM MgSO₄, 1.5 mM CaCl₂, 11.1 mM glucose, 10 μM pargyline pH 7.4) and incubated in basal buffer at 25 mg/mL wet weight with [³H]5-HT (50 nM) for 30 minutes at 37 °C. The slices are washed three times in basal buffer and transferred to baskets (10 mm i.d. polypropylene tubes with 150 μm nylon mesh bases) at approximately 5 mg wet weight per basket. The baskets are used to transfer the tissue between the washing and release buffers. In order to obtain stable baseline release, the slices are incubated for 11 minutes in basal buffer (0.5 mL), transferred for 4 minutes to a second tube containing basal buffer (0.5 mL) and then, for a further 4 minutes, to basal buffer (0.5 mL) or to a buffer in which NaCl has been substituted with KCl, on an equimolar basis, to give a KCl concentration of 30 mM (release sample). All buffers used in the 11 minutes and the two 4 minutes incubations contained 1 μM paroxetine. Following the incubations, the tissue is digested with Soluene-350 (0.7 mL) and the baskets rinsed with propan-2-ol (0.7 mL). The tritium label in the tissue samples and in the buffers from the three incubation periods is estimated by liquid scintillation spectroscopy. LY310762 being tested is present throughout the three incubation periods and is tested in six replicates. The basal release is measured in four replicates and the control release in eight replicates. The tritium label in the release sample is expressed as the percentage of the total tritium in the tissue at the time the sample is collected (% fractional release). Stimulated release is calculated as the % fractional release produced by the high potassium buffer minus that of basal release. The percentage increase in release produced by LY310762 is calculated as the increase over the control stimulated release, where the control release is 100%. For individual experiments the mean of the replicate data is calculated. The results are the means and standard errors of at least three separate experiments.

Animal Study:
^[1]

Animal Models	Dunkin Hartley guinea pigs weighting 350-400 g
Formulation
Dosages	10 mg/kg
Administration	Administered via i.p.

References

Chemical Information

Download LY310762 SDF

Molecular Weight (MW)	430.94
Formula	C₂₄H₂₇FN₂O₂.HCl
CAS No.	192927-92-7
Synonyms	N/A

Solubility (25°C) DMSO 0.4 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	1-(2-(4-(4-fluorobenzoyl)piperidin-1-yl)ethyl)-3,3-dimethylindolin-2-one hydrochloride

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Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Related 5-HT Receptor Antagonists & Agonists

WAY-100635 HCl
WAY 100635 is a potent and selective 5-HT agonist with IC50 of 0.95 nM.
BRL-15572
BRL-15572 is a 5-HT_1D antagonist with pK_i of 7.9.
BMY 7378
BMY 7378 is a multiple inhibitors of α_2C-adrenoceptor and α_1D-adrenoceptor with pK_i of 6.54 and 8.2, respectively.
RS-127445
RS-127445 is a selective 5-HT2B antagonist with pK_i of 9.5 and pIC50 of 10.4.
SB-269970 HCl
SB-269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT₇ receptor antagonist with pK_i of 8.3.
BRL 54443
BRL 54443 is a 5-HT_1E and 5-HT_1F receptor agonist with pK_i of 8.7 and 9.25, respectively.
SB 271046
SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i of 8.9.
IEM 1754 Dihydrobromide
IEM 1754 dihydrobroMide is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
VUF 10166
VUF10166 is a novel, potent and competitive antagonist to 5-HT₃A with K_i of 0.04 nM.
Prucalopride
Prucalopride is a selective, high affinity 5-HT receptor agonistfor 5-HT4a and 5-HT4b with K_i of 2.5 nM and 8 nM, respectively.

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Product Categories

LY310762

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

LY310762 is available in the following compound libraries:

Product Information

Compare 5-HT Receptor Antagonists & Agonists

Combination Therapy

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay:
^[1]

Animal Study:
^[1]

References

Chemical Information

Research Area

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related 5-HT Receptor Antagonists & Agonists

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Cat.No.	Product Name	Water	DMSO	Ethanol
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S1333	Fluoxetine HCl	4 mg/mL	69 mg/mL	69 mg/mL
S2493	Olanzapine (Zyprexa)	<1 mg/mL	63 mg/mL	9 mg/mL
S1441	Venlafaxine	55.5 mg/mL	55.5 mg/mL	55.5 mg/mL
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S2459	Clozapine (Clozaril)	<1 mg/mL	65 mg/mL	32 mg/mL
S1283	Asenapine	<1 mg/mL	80 mg/mL	<1 mg/mL
S1336	Fluvoxamine maleate	<1 mg/mL	87 mg/mL	87 mg/mL
S2698	RS-127445	<1 mg/mL	56 mg/mL	8 mg/mL
S3005	Paroxetine HCl	10 mg/mL	73 mg/mL	35 mg/mL
S1432	Sumatriptan succinate	83 mg/mL	83 mg/mL	<1 mg/mL
S1488	Naratriptan HCl	22 mg/mL	74 mg/mL	<1 mg/mL
S1649	Zolmitriptan (Zomig)	<1 mg/mL	58 mg/mL	58 mg/mL
S2541	Clomipramine HCl (Anafranil)	70 mg/mL	70 mg/mL	70 mg/mL
S2691	BMY 7378	92 mg/mL	92 mg/mL	20 mg/mL
S2663	WAY-100635 HCl	<1 mg/mL	85 mg/mL	85 mg/mL
S2677	BRL-15572	<1 mg/mL	96 mg/mL	40 mg/mL
S1975	Aripiprazole (Abilify)	<1 mg/mL	90 mg/mL	<1 mg/mL
S2849	SB-269970 HCl	<1 mg/mL	11 mg/mL	<1 mg/mL
S2875	Prucalopride	<1 mg/mL	60 mg/mL	38 mg/mL
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S1345	Granisetron HCl	70 mg/mL	1 mg/mL	1 mg/mL
S1385	Mosapride citrate	<1 mg/mL	90 mg/mL	<1 mg/mL
S1390	Ondansetron HCl (Zofran)	24 mg/mL	66 mg/mL	10 mg/mL
S1436	Tianeptine sodium	92 mg/mL	92 mg/mL	92 mg/mL
S1607	Rizatriptan Benzoate (Maxalt)	46 mg/mL	20 mg/mL	<1 mg/mL
S1869	Dapoxetine HCl (Priligy)	68 mg/mL	68 mg/mL	68 mg/mL
S1898	Tropisetron	64 mg/mL	35 mg/mL	<1 mg/mL
S2669	LY310762	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1996	Ondansetron (Zofran)	<1 mg/mL	0.1 mg/mL	<1 mg/mL
S2582	Trazodone HCl (Desyrel)	<1 mg/mL	1 mg/mL	<1 mg/mL
S2025	Urapidil HCl	85 mg/mL	24 mg/mL	1 mg/mL
S2084	Duloxetine HCl (Cymbalta)	<1 mg/mL	67 mg/mL	<1 mg/mL
S2106	Azasetron HCl (Y-25130)	3 mg/mL	<1 mg/mL	<1 mg/mL
S2096	Almotriptan malate (Axert)	<1 mg/mL	94 mg/mL	53 mg/mL
S2112	Blonanserin (Lonasen)	<1 mg/mL	<1 mg/mL	<1 mg/mL
S3175	Atomoxetine HCl	2 mg/mL	58 mg/mL	37 mg/mL
S3183	Amitriptyline HCl	15 mg/mL	63 mg/mL	63 mg/mL
S2860	IEM 1754 Dihydrobromide	82 mg/mL	82 mg/mL	<1 mg/mL
S2852	BRL 54443	<1 mg/mL	46 mg/mL	2 mg/mL
S3050	Palonosetron HCl	67 mg/mL	<1 mg/mL	<1 mg/mL
S2865	VUF 10166	<1 mg/mL	21 mg/mL	61 mg/mL
S2856	SB 271046	<1 mg/mL	40 mg/mL	<1 mg/mL
S8010	PRX-08066	104 mg/mL	104 mg/mL	98 mg/mL
S8021	Vortioxetine (Lu AA21004) hydrobromide	<1 mg/mL	76 mg/mL	17 mg/mL
S4053	Sertraline HCl	<1 mg/mL	69 mg/mL	15 mg/mL
S4064	Escitalopram Oxalate	25 mg/mL	83 mg/mL	<1 mg/mL
S4109	Lorcaserin HCl	46 mg/mL	46 mg/mL	46 mg/mL
S4112	Desvenlafaxine Succinate	<1 mg/mL	80 mg/mL	<1 mg/mL
S4113	Desvenlafaxine	<1 mg/mL	37 mg/mL	3 mg/mL

Choose Your Country or Region

Product Categories

LY310762

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

LY310762 is available in the following compound libraries:

Product Information

Compare 5-HT Receptor Antagonists & Agonists

Combination Therapy

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [1]

Animal Study: [1]

References

Chemical Information

Research Area

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related 5-HT Receptor Antagonists & Agonists

Neuronal Signaling Pathway Products

Recently Viewed Items

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Kinase Assay:
^[1]

Animal Study:
^[1]