<Suppliers Price>

Linopirdine(DuP-996)

Names

[ CAS No. ]:
105431-72-9

[ Name ]:
Linopirdine(DuP-996)

[Synonym ]:
linopiridine
Dup 996
Linopirdine

Biological Activity

[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 Channel
Research Areas >> Neurological Disease
Signaling 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

MSDS

Click to get detail MSDS

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

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933790090

[ Summary ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

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...


More Articles

Related Compounds