GR-65630

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

MedKoo CAT#: 575963

CAS#: 117186-80-8

Description: GR-65630 is a 5-HT3 serotonin receptor ligand. [3H]GR65630 has been shown to label 5-HT3 receptors in homogenates of rat entorhinal cortex. Note: This product listed here is not radiolabelled [3H]GR65630. We only supply non-radiolabelled version of GR65630.

Chemical Structure

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GR-65630
CAS# 117186-80-8
Instruction

Theoretical Analysis

MedKoo Cat#: 575963
Name: GR-65630
CAS#: 117186-80-8
Chemical Formula: C16H17N3O
Exact Mass: 267.14
Molecular Weight: 267.330
Elemental Analysis: C, 71.89; H, 6.41; N, 15.72; O, 5.98

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: GR 65630; GR65630; GR-65630;

IUPAC/Chemical Name: 1-Propanone, 3-(5-methyl-1H-imidazol-4-yl)-1-(1-methyl-1H-indol-2-yl)-

InChi Key: AQCBJPZFJDPIGL-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N3O/c1-11-13(18-10-17-11)7-8-16(20)15-9-12-5-3-4-6-14(12)19(15)2/h3-6,9-10H,7-8H2,1-2H3,(H,17,18)

SMILES Code: Cc1nc[nH]c1CCC(=O)c2cc3ccccc3n2C

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: L-3,4-dihydroxyphenylalanine (l-DOPA) is the mainstay treatment for Parkinson's disease, but its effectiveness during early disease is marred by the eventual development of l-DOPA induced dyskinesia. In hemi-parkinsonian rats, the serotonin type 3 (5-HT3) antagonists ondansetron and granisetron alleviated dyskinesia induced by l-DOPA without impeding its anti-parkinsonian action; in parkinsonian marmosets, ondansetron alleviated dyskinesia and enhanced l-DOPA anti-parkinsonian action.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 267.33 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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8: Feng JJ, Cheng FC, Lin CH, Wei JW, Yang SD. Characterization of 5-HT transporter and receptor system in HeLaS3 cells by [(3)H]8-OH-DPAT and other serotonergic ligands. Arch Biochem Biophys. 2011 Feb 1;506(1):66-72. doi: 10.1016/j.abb.2010.10.024. Epub 2010 Nov 5. PMID: 21056540.


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10: Walstab J, Hammer C, Lasitschka F, Möller D, Connolly CN, Rappold G, Brüss M, Bönisch H, Niesler B. RIC-3 exclusively enhances the surface expression of human homomeric 5-hydroxytryptamine type 3A (5-HT3A) receptors despite direct interactions with 5-HT3A, -C, -D, and -E subunits. J Biol Chem. 2010 Aug 27;285(35):26956-26965. doi: 10.1074/jbc.M110.122838. Epub 2010 Jun 3. PMID: 20522555; PMCID: PMC2930695.


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12: Combrink S, Kostanian A, Walstab J, Barann M, Brüss M, Göthert M, Bönisch H. Characterization of the naturally occurring Arg344His variant of the human 5-HT 3A receptor. Pharmacol Rep. 2009 Sep-Oct;61(5):785-97. doi: 10.1016/s1734-1140(09)70134-3. PMID: 19904001.


13: Heimes K, Feistel B, Verspohl EJ. Impact of the 5-HT3 receptor channel system for insulin secretion and interaction of ginger extracts. Eur J Pharmacol. 2009 Dec 10;624(1-3):58-65. doi: 10.1016/j.ejphar.2009.09.049. Epub 2009 Oct 7. PMID: 19818348.


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17: Simmen U, Kelber O, Okpanyi SN, Jaeggi R, Bueter B, Weiser D. Binding of STW 5 (Iberogast) and its components to intestinal 5-HT, muscarinic M3, and opioid receptors. Phytomedicine. 2006;13 Suppl 5:51-5. doi: 10.1016/j.phymed.2006.03.012. Epub 2006 Sep 14. PMID: 16973340.


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19: Abdel-Aziz H, Windeck T, Ploch M, Verspohl EJ. Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum. Eur J Pharmacol. 2006 Jan 13;530(1-2):136-43. doi: 10.1016/j.ejphar.2005.10.049. Epub 2005 Dec 20. PMID: 16364290.


20: Walkembach J, Brüss M, Urban BW, Barann M. Interactions of metoclopramide and ergotamine with human 5-HT(3A) receptors and human 5-HT reuptake carriers. Br J Pharmacol. 2005 Oct;146(4):543-52. doi: 10.1038/sj.bjp.0706351. Erratum in: Br J Pharmacol. 2005 Dec;146(8):1156. PMID: 16041395; PMCID: PMC1751187.