CAS 105431-72-9|Linopirdine(DuP-996)
| Common Name | Linopirdine(DuP-996) | ||
|---|---|---|---|
| CAS Number | 105431-72-9 | Molecular Weight | 391.46400 |
| Density | 1.255 g/cm3 | Boiling Point | 655.9ºC at 760 mmHg |
| Molecular Formula | C26H21N3O | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 350.5ºC |
Names
| Name | 1-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one |
|---|---|
| Synonym | More Synonyms |
Linopirdine(DuP-996) BiologicalActivity
| Description | Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3]. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>TRP ChannelResearch Areas >>Neurological DiseaseSignaling Pathways >>Membrane Transporter/Ion Channel >>Potassium Channel |
| Target | IC50: 2.4 μM (M-type K+ current)[1] |
| In Vitro | Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K+ leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na+/K+ inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC50>300 μM)[1]. Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1)[3]. |
| In Vivo | Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%[2]. Animal Model: Male Sprague-Dawley rats (300-350 g)[2] Dosage: 0.1, 0.5, 1, 3, 6 mg/kg Administration: 5 intravenous bolus injections of increasing doses Result: Transiently and dose-dependently increases MAP by up to 15%. |
| References | [1]. Schnee ME, et al. 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. 1998 Aug;286(2):709-17. [2]. Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8. [3]. Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40. |
Chemical & Physical Properties
| Density | 1.255 g/cm3 |
|---|---|
| Boiling Point | 655.9ºC at 760 mmHg |
| Molecular Formula | C26H21N3O |
| Molecular Weight | 391.46400 |
| Flash Point | 350.5ºC |
| Exact Mass | 391.16800 |
| PSA | 46.09000 |
| LogP | 4.94310 |
| Vapour Pressure | 4.45E-17mmHg at 25°C |
| Index of Refraction | 1.669 |
| InChIKey | YEJCDKJIEMIWRQ-UHFFFAOYSA-N |
| SMILES | O=C1N(c2ccccc2)c2ccccc2C1(Cc1ccncc1)Cc1ccncc1 |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Hazard Codes | Xi |
| RIDADR | NONH for all modes of transport |
| HS Code | 2933790090 |
Customs
| HS Code | 2933790090 |
|---|---|
| Summary | 2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0% |
Articles40
More Articles| Ion channel expression in the developing enteric nervous system. PLoS ONE 10(3) , e0123436, (2015) The enteric nervous system arises from neural crest-derived cells (ENCCs) that migrate caudally along the embryonic gut. The expression of ion channels by ENCCs in embryonic mice was investigated usin... | |
| Low expression of Kv7/M channels facilitates intrinsic and network bursting in the developing rat hippocampus. J. Physiol. 586(Pt 22) , 5437-53, (2008) Early in development, network activity in the hippocampus is characterized by recurrent synchronous bursts, whose cellular correlates are giant depolarizing potentials (GDPs). The propensity for gener... | |
| Role of Kv7 channels in responses of the pulmonary circulation to hypoxia. Am. J. Physiol. Lung Cell. Mol. Physiol. 308(1) , L48-57, (2015) Hypoxic pulmonary vasoconstriction (HPV) is a beneficial mechanism that diverts blood from hypoxic alveoli to better ventilated areas of the lung, but breathing hypoxic air causes the pulmonary circul... |
Synonyms
| linopiridine |
| Dup 996 |
| Linopirdine |
