A neurotransmitter release enhancer
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Linopirdine

Item No. 19547

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one
CAS Number
105431-72-9
Synonyms
  • DuP-996
Molecular Formula
C26H21N3O
Formula Weight
391.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 25 mg/mLEthanol: 30 mg/mLEthanol:PBS (pH 7.2) (1:30): 0.03 mg/mL
λmax
248 nm
SMILES
O=C1C(CC2=CC=NC=C2)(CC3=CC=NC=C3)C4=CC=CC=C4N1C5=CC=CC=C5
InChi Code
InChI=1S/C26H21N3O/c30-25-26(18-20-10-14-27-15-11-20,19-21-12-16-28-17-13-21)23-8-4-5-9-24(23)29(25)22-6-2-1-3-7-22/h1-17H,18-19H2
InChi Key
YEJCDKJIEMIWRQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $36

    Add

    5 mg

    $134

    Add

    10 mg

    $215

    Add
    Product Description

    Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 µM.1,2 Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release.3 Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory.4 Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV).5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schnee, M.E., and Brown, B.S. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J. Pharmacol. Exp. Ther. 286(2), 709-717 (1998).

    2. Kristufek, D., Koth, G., Motejlek, A., et al. Modulation of spontaneous and stimulation-evoked transmitter release from rat sympathetic neurons by the cognition enhancer linopirdine: Insights into its mechanisms of action. J. Neurochem. 72(50), 2083-2091 (1999).

    3. Sun, J., and Kapur, J. M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission. J. Physiol. 590(16), 3953-3964 (2012).

    4. Tam, S.W., and Zaczek, R. Linopirdine. A depolarization-activated releaser of transmitters for treatment of dementia. Adv. Exp. Med. Biol. 363, 47-56 (1995).

    5. Neacsu, C., and Babes, A. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J. Pharmacol. Sci. 114(3), 332-340 (2010).