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Sodium leak channel, non-selective (NaVi) C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The sodium leak channel, non selective (NC-IUPHAR tentatively recommends the nomenclature NaVi2.1, W.A. Catterall, personal communication) is structurally a member of the family of voltage-gated sodium channel family (Nav1.1-Nav1.9) [1,9]. In contrast to the latter, NaVi2.1, is voltage-insensitive (denoted in the subscript 'vi' in the tentative nomenclature) and possesses distinctive ion selectivity and pharmacological properties. NaVi2.1, which is insensitive to tetrodotoxin (10 µM), has been proposed to mediate the tetrodotoxin-resistant and voltage-insensitive Na+ leak current (IL-Na) observed in many types of neurone [2]. However, whether NaVi2.1 is constitutively active has been challenged [7]. NaVi2.1 is widely distributed within the central nervous system and is also expressed in the heart and pancreas specifically, in rodents, within the islets of Langerhans [1-2]. Recently, NaVi2.1 has been proposed to be a core effector for the action of inhibitory G proteins [5].

Channels and Subunits

750
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Navi2.1 C Show summary »


Target Id 750
Nomenclature Navi2.1
Previous and unofficial names Nax | NALCN | Nav2.1 | Rb21 | voltage-gated channel like 1 (VGCNL1) | CanIon | brain voltage-gated cation channel | four domain-type voltage-gated ion channel alpha-1 subunit | sodium leak channel, non-selective | sodium leak channel, non selective | sodium leak channel
Genes NALCN (Hs), Nalcn (Mm), Nalcn (Rn)
Ensembl ID ENSG00000102452 (Hs), ENSMUSG00000000197 (Mm), ENSRNOG00000004752 (Rn)
UniProtKB AC Q8IZF0 (Hs), Q8BXR5 (Mm), Q6Q760 (Rn)
Activators Constitutively active (Lu et al., 2007), or activated downstream of Src family tyrosine kinases (SFKs) (Lu et al.,2009; Swayne et al., 2009); positively modulated by decreased extracellular Ca2+ concentration (Lu et al., 2010)  [2-4,7]
Channel blockers
Gd3+ pIC50 5.6
Cd2+ pIC50 3.8
Co2+ pIC50 3.6
verapamil pIC50 3.4
Functional characteristics γ = 27 pS (by fluctuation analysis), PNa/PCs = 1.3, PK/PCs = 1.2, PCa/PCs = 0.5, linear current voltage-relationship, voltage-independent and non-inactivating

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How to cite this family page

Database page citation:

Sodium leak channel, non-selective (NaVi). Accessed on 20/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=126.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Mathie A, Peters JA, Veale EL, Striessnig J, Kelly E, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Ion channels. Br J Pharmacol. 176 Issue S1: S142-228.