YM 230888

Pricing Availability Delivery Time Qty
Cat.No. 2986 - YM 230888 | C19H28N4OS | CAS No. 446257-23-4
Description: Selective mGlu1 antagonist
Chemical Name: 4-(Cycloheptylamino)-N-[[(2R)-tetrahydro-2-furanyl]methyl]-thieno[2,3-d]pyrimidine-6-methanamine
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Selective mGlu1 antagonist (Ki = 13 nM). Inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells (IC50 = 13 nM). Displays antinociceptive and analgesic effects in vitro; exhibits no significant sedative effect on locomotor activity.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Technical Data

M. Wt 360.52
Formula C19H28N4OS
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 446257-23-4
PubChem ID 11682007
InChI Key SASNRPJKZVJWQW-OAHLLOKOSA-N
Smiles C1(NC4CCCCCC4)=C(C=C(CNC[C@H]3CCCO3)S2)C2=NC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.05 100
ethanol 36.05 100

Preparing Stock Solutions

The following data is based on the product molecular weight 360.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.77 mL 13.87 mL 27.74 mL
5 mM 0.55 mL 2.77 mL 5.55 mL
10 mM 0.28 mL 1.39 mL 2.77 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kohara et al (2007) Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models. Eur.J.Pharmacol. 571 8 PMID: 17597604

Satow et al (2008) Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost J.Pharmacol.Exp.Ther. 326 577 PMID: 18487514


If you know of a relevant reference for YM 230888, please let us know.

View Related Products by Product Action

View all Glutamate (Metabotropic) Group I Receptor Antagonists

Keywords: YM230888 mGlu1 metabotropic glutamate receptors group I 1 antagonist antagonists mGlu selective Glutamate (Metabotropic) Group I Receptors

Citations for YM 230888

Citations are publications that use Tocris products.

Currently there are no citations for YM 230888. Do you know of a great paper that uses YM 230888 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Metabotropic Glutamate Receptors

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

Addiction

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

Huntington's Disease

Huntington's Disease Poster

Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.

Learning & Memory

Learning & Memory Poster

Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Parkinson's

Parkinson's Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.

Pathways for YM 230888

Protocols

TODO: Add Protocols