LY382884

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532165

CAS#: 211566-75-5

Description: LY382884 is a GLU(K5) receptor antagonist. LY382884 selectively binds the GLU(K5) kainate receptor subunit (K(b)=0.6 microM) and has 30 microM or greater affinity for cloned human AMPA receptor subtypes. GluR5-mediated glutamate signaling regulates hypothalamo-pituitary-adrenocortical stress responses at the paraventricular nucleus and median eminence.

Chemical Structure

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LY382884
CAS# 211566-75-5
Instruction

Theoretical Analysis

MedKoo Cat#: 532165
Name: LY382884
CAS#: 211566-75-5
Chemical Formula: C18H23NO4
Exact Mass: 317.16
Molecular Weight: 317.390
Elemental Analysis: C, 68.12; H, 7.30; N, 4.41; O, 20.16

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: LY-382884; LY 382884; LY382884.

IUPAC/Chemical Name: (3S,4aR,6S,8aR)-6-[(4-carboxyphenyl)methyl]-decahydroisoquinoline-3-carboxylic acid

InChi Key: YVMADKYPKNLVGU-BVUBDWEXSA-N

InChi Code: InChI=1S/C18H23NO4/c20-17(21)13-4-1-11(2-5-13)7-12-3-6-14-10-19-16(18(22)23)9-15(14)8-12/h1-2,4-5,12,14-16,19H,3,6-10H2,(H,20,21)(H,22,23)/t12-,14+,15-,16+/m1/s1

SMILES Code: O=C([C@H]1NC[C@]2([H])CC[C@H](CC3=CC=C(C(O)=O)C=C3)C[C@]2([H])C1)O

Appearance: Solid powder

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

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 317.39 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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1: Alt A, Weiss B, Ornstein PL, Gleason SD, Bleakman D, Stratford RE Jr, Witkin JM. Anxiolytic-like effects through a GLUK5 kainate receptor mechanism. Neuropharmacology. 2007 Jun;52(7):1482-7. Epub 2007 Mar 2. PubMed PMID: 17418283.

2: Binns KE, Turner JP, Salt TE. Kainate receptor (GluR5)-mediated disinhibition of responses in rat ventrobasal thalamus allows a novel sensory processing mechanism. J Physiol. 2003 Sep 1;551(Pt 2):525-37. Epub 2003 Aug 8. PubMed PMID: 12909680; PubMed Central PMCID: PMC2343236.

3: Evanson NK, Van Hooren DC, Herman JP. GluR5-mediated glutamate signaling regulates hypothalamo-pituitary-adrenocortical stress responses at the paraventricular nucleus and median eminence. Psychoneuroendocrinology. 2009 Oct;34(9):1370-9. doi: 10.1016/j.psyneuen.2009.04.011. Epub 2009 May 18. PubMed PMID: 19450932; PubMed Central PMCID: PMC2763572.

4: Palecek J, Neugebauer V, Carlton SM, Iyengar S, Willis WD. The effect of a kainate GluR5 receptor antagonist on responses of spinothalamic tract neurons in a model of peripheral neuropathy in primates. Pain. 2004 Sep;111(1-2):151-61. PubMed PMID: 15327819.

5: Rasmussen K, Vandergriff J. The selective iGluR1-4 (AMPA) antagonist LY300168 attenuates morphine-withdrawal-induced activation of locus coeruleus neurons and behavioural signs of morphine withdrawal. Neuropharmacology. 2003 Jan;44(1):88-92. PubMed PMID: 12559125.

6: Duncan GE, Inada K, Koller BH, Moy SS. Increased sensitivity to kainic acid in a genetic model of reduced NMDA receptor function. Brain Res. 2010 Jan 11;1307:166-76. doi: 10.1016/j.brainres.2009.10.023. Epub 2009 Oct 22. PubMed PMID: 19840778; PubMed Central PMCID: PMC2787847.

7: Christensen JK, Paternain AV, Selak S, Ahring PK, Lerma J. A mosaic of functional kainate receptors in hippocampal interneurons. J Neurosci. 2004 Oct 13;24(41):8986-93. PubMed PMID: 15483117.

8: Stanfa LC, Dickenson AH. The role of non-N-methyl-D-aspartate ionotropic glutamate receptors in the spinal transmission of nociception in normal animals and animals with carrageenan inflammation. Neuroscience. 1999;93(4):1391-8. PubMed PMID: 10501464.

9: Vesikansa A, Sallert M, Taira T, Lauri SE. Activation of kainate receptors controls the number of functional glutamatergic synapses in the area CA1 of rat hippocampus. J Physiol. 2007 Aug 15;583(Pt 1):145-57. Epub 2007 Jun 14. PubMed PMID: 17569736; PubMed Central PMCID: PMC2277228.

10: Lauri SE, Bortolotto ZA, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL. A critical role of a facilitatory presynaptic kainate receptor in mossy fiber LTP. Neuron. 2001 Nov 20;32(4):697-709. PubMed PMID: 11719209.

11: Breustedt J, Schmitz D. Assessing the role of GLUK5 and GLUK6 at hippocampal mossy fiber synapses. J Neurosci. 2004 Nov 10;24(45):10093-8. PubMed PMID: 15537878.

12: Bortolotto ZA, Clarke VR, Delany CM, Parry MC, Smolders I, Vignes M, Ho KH, Miu P, Brinton BT, Fantaske R, Ogden A, Gates M, Ornstein PL, Lodge D, Bleakman D, Collingridge GL. Kainate receptors are involved in synaptic plasticity. Nature. 1999 Nov 18;402(6759):297-301. PubMed PMID: 10580501.

13: Clarke VR, Collingridge GL. Characterisation of the effects of ATPA, a GLU(K5) kainate receptor agonist, on GABAergic synaptic transmission in the CA1 region of rat hippocampal slices. Neuropharmacology. 2004 Sep;47(3):363-72. PubMed PMID: 15275825.

14: Lauri SE, Segerstråle M, Vesikansa A, Maingret F, Mulle C, Collingridge GL, Isaac JT, Taira T. Endogenous activation of kainate receptors regulates glutamate release and network activity in the developing hippocampus. J Neurosci. 2005 May 4;25(18):4473-84. PubMed PMID: 15872094.

15: Xu C, Cui C, Alkon DL. Age-dependent enhancement of inhibitory synaptic transmission in CA1 pyramidal neurons via GluR5 kainate receptors. Hippocampus. 2009 Aug;19(8):706-17. doi: 10.1002/hipo.20544. PubMed PMID: 19123252.

16: Jane DE, Lodge D, Collingridge GL. Kainate receptors: pharmacology, function and therapeutic potential. Neuropharmacology. 2009 Jan;56(1):90-113. doi: 10.1016/j.neuropharm.2008.08.023. Epub 2008 Aug 28. Review. PubMed PMID: 18793656.

17: Bortolotto ZA, Lauri S, Isaac JT, Collingridge GL. Kainate receptors and the induction of mossy fibre long-term potentiation. Philos Trans R Soc Lond B Biol Sci. 2003 Apr 29;358(1432):657-66. Review. PubMed PMID: 12740111; PubMed Central PMCID: PMC1693169.

18: Mathew SS, Hablitz JJ. Calcium release via activation of presynaptic IP3 receptors contributes to kainate-induced IPSC facilitation in rat neocortex. Neuropharmacology. 2008 Jul;55(1):106-16. doi: 10.1016/j.neuropharm.2008.05.005. Epub 2008 May 14. PubMed PMID: 18508095; PubMed Central PMCID: PMC2580077.

19: Lauri SE, Bortolotto ZA, Nistico R, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL. A role for Ca2+ stores in kainate receptor-dependent synaptic facilitation and LTP at mossy fiber synapses in the hippocampus. Neuron. 2003 Jul 17;39(2):327-41. PubMed PMID: 12873388.

20: Campbell SL, Mathew SS, Hablitz JJ. Pre- and postsynaptic effects of kainate on layer II/III pyramidal cells in rat neocortex. Neuropharmacology. 2007 Jul;53(1):37-47. Epub 2007 Apr 29. PubMed PMID: 17543353; PubMed Central PMCID: PMC2033380.