How “Pharmacoresistant” is Cav2.3, the Major Component of Voltage-Gated R-type Ca2+ Channels?
Abstract
:1. The Cav2.3 Voltage-Gated Ca2+ Channel
Nomenclature, splice variant | Structure related to alternate exons expressed (+) | Expression (tissue and species) | Ref. | |||
---|---|---|---|---|---|---|
Novel terms | Old terms | Exon 19 (57 nts) | Segment (21 nts) in exon 20 | Exon 45 (129 nts) | ||
Cav2.3a | alpha1E-1 | - | + | - | Rat cerebellum | [100] |
Cav2.3b | alpha1E-2 | + | - | - | Less important in CNS | [3] |
Cav2.3c | alpha1E-3 | + | + | - | Dominant in CNS | [3] |
Cav2.3d | alpha1Ed | + | + | + | Human fetal brain | [4] |
Cav2.3e | alpha1Ee | - | + | + | Pancreas, kidney, heart | [70,101] |
Cav2.3f | alpha1Ef | + | - | + | Rat cerebellum | [100] |
Brain region (mouse) | Major splice variant | Miscellaneous |
---|---|---|
Neocortex | Cav2.3c | Minor amounts of Cav2.3e |
Hippocampus | Cav2.3c | Minor amounts of Cav2.3e |
Thalamus | Cav2.3c | Substantial amounts of Cav2.3e and Cav2.3f |
Cerebellum, mesencephalon, medulla oblongata | Cav2.3e | minor amounts of Cav2.3a |
2. Selective and Non-Selective Antagonists of Cav2.3
3. Physiological Functions, in Which Cav2.3 may be Involved, as Deduced from Cav2.3-Deficient Mice
Substance | Application | IC50 or Kd [µM] | Amount of max. Inhibition | Selectivity | Ref. |
---|---|---|---|---|---|
SNX-482 | Peptide toxin | 0.015–0.030 | > 80 % | Cav2.3-prevalent | [107,108,128,129,130] |
ω-Aga-IVA | Peptide toxin | 0.051 | 80% | non-selective | [116] |
ω-Aga-IIIA | Peptide toxin | 0.003–0.010 | 100% | non-selective | [107] |
Ni2+ | Unphysiological | 27.4/303 | 100% | non-selective | [3,131] |
Cd2+ | Unphysiological | 0.8 | 100% | non-selective | [3] |
Zn2+ | Trace element | 31.8 | >90% | non-selective | [132] |
Zn2+ (calibrated) | Trace element | 1.3 | 100% | non-selective | [10] |
Cu2+ | Trace element | 0.018 | 100% | non-selective | [10] |
Topiramate | Anticonvulsive | 50.9 | >70% | non-selective | [133] |
Lamotrigine | Anticonvulsive | >10 | non-selective | [134] | |
Sipatrigine | Anticonvulsive | 10 | 100% | non-selective | [134] |
202W92 | Anticonvulsive | 56 | 100% | [134] | |
Ethosuximide | Anticonvulsive | 20000 | 100% | non-selective | [135] |
MPS (α-methylphenylsuccinimide) | Anticonvulsive | 2300 | 100% | [135] | |
Phenytoin | Anticonvulsive | 360 | 100% | [135] | |
Phenobarbital | Anticonvulsive | 2700 | >80% | [135] | |
Pentobarbital | Anticonvulsive | 600 | 100% | [135] | |
Halothane | Inhalation anaesthetic | [136,137] | |||
Isoflurane | Inhalation anaesthetic | 206 | 100% | [136,138,139] | |
Fomocaine | Local anaestetic | 95 | 100% | [140] | |
Procaine | Local anaestetic | [140] | |||
Octanol | Organic solvent | 206 | 100% | [135] | |
(+)-ACN | Steroid anaestetic | 5.3–10.2 | 100% | [141] | |
(+)-ECN | Steroid anaestetic | 9.9–16.1 | >70% | [141] | |
Flecainide | Antiarrhythmic | 320 | [140] | ||
Penfluridol | Antipsychotic | 13 | [140] | ||
Verapamil | Antihypertensive | 100 | 100% | non-selective | [142] |
Diltiazem | Antihypertensive | 220 | 100% | non-selective | [4,142] |
Isradipine | Antihypertensive | 9.1 | 100% | non-selective | [87] |
Nicardipine | Antihypertensive | 1 | n.t. | non-selective | [116] |
Mibefradil | Antihypertensive | 0.4/6.5 | 100% | non-selective | [143] |
Amiloride | Diuretic | 7400 | 100% | non-selective | [135] |
Ethoxyzolamide | Carboanhydrase inhibitor/anticonvulsive | 1 | 70% | [144] | |
Eugenol | Analgetic | [145] | |||
Bisphenol A | Environmental pollutant | 26 | 50% | non-selective | [146] |
Acknowledgments
Conflict of Interest
References
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Schneider, T.; Dibué, M.; Hescheler, J. How “Pharmacoresistant” is Cav2.3, the Major Component of Voltage-Gated R-type Ca2+ Channels? Pharmaceuticals 2013, 6, 759-776. https://doi.org/10.3390/ph6060759
Schneider T, Dibué M, Hescheler J. How “Pharmacoresistant” is Cav2.3, the Major Component of Voltage-Gated R-type Ca2+ Channels? Pharmaceuticals. 2013; 6(6):759-776. https://doi.org/10.3390/ph6060759
Chicago/Turabian StyleSchneider, Toni, Maxine Dibué, and Jürgen Hescheler. 2013. "How “Pharmacoresistant” is Cav2.3, the Major Component of Voltage-Gated R-type Ca2+ Channels?" Pharmaceuticals 6, no. 6: 759-776. https://doi.org/10.3390/ph6060759