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. 2013 Dec 17;170(8):1582–1606. doi: 10.1111/bph.12446
Nomenclature α1* α2* α3*
HGNC, UniProt CHRNA1, P02708 CHRNA2, Q15822 CHRNA3, P32297
Commonly used antagonists (α1)2β1γδ and (α1)2β1δε: α-bungarotoxin > pancuronium > vecuronium > rocuronium > (+)-tubocurarine (IC50 = 43 - 82 nM) α2β2: DHβE (KB = 0.9 μM), (+)-tubocurarine (KB = 1.4 μM); α2β4: DHβE (KB = 3.6 μM), (+)-tubocurarine (KB = 4.2 μM) α3β2: DHβE (KB = 1.6 μM, IC50 = 2.0 μM), (+)-tubocurarine (KB = 2.4 μM); α3β4: DHβE (KB = 19 μM, IC50 = 26 μM), (+)-tubocurarine (KB = 2.2 μM)
Selective agonists succinylcholine (Full agonist, selective for (α1)2β1γδ) – –
Selective antagonists α-bungarotoxin, α-conotoxin GI, α-conotoxin MI, pancuronium, waglerin-1 (selective for (α1)2β1δε) – α-conotoxin AuIB (α3β4), α-conotoxin-GIC (α3β2), α-conotoxin MII (α3β2), α-conotoxin PnIA (α3β2), α-conotoxin TxIA (α3β2)
Selective channel blockers (IC50) gallamine ((α1)2β1γδ and (α1)2β1δε) (∼1x10-6 M), mecamylamine ((α1)2β1δε) (∼1.5x10-6 M) hexamethonium, mecamylamine A-867744(α3β4) 227, hexamethonium (α3β2), hexamethonium (α3β4), NS1738(α3β4) 237, mecamylamine (α3β4) (3.9x10-7 M), mecamylamine (α3β2) (7.6x10-6 M)
Selective allosteric regulators – LY2087101(Positive) 206 –
Radioligands (Kd) [125I]α-bungarotoxin, [3H]α-bungarotoxin [3H]cytisine, [125I]epibatidine (α2β2) (1x10-11 – 2.1x10-11 M - Rat), [3H]epibatidine (α2β2) (1x10-11 – 2.1x10-11 M - Rat), [125I]epibatidine (α2β4) (4.2x10-11 M), [3H]epibatidine (α2β4) (4.2x10-11 M), [125I]epibatidine (α2β4) (8.4x10-11 – 8.7x10-11 M - Rat), [3H]epibatidine (α2β4) (8.4x10-11 – 8.7x10-11 M - Rat) [3H]cytisine, [125I]epibatidine (α3β2) (7x10-12 M), [3H]epibatidine (α3β2) (7x10-12 M), [125I]epibatidine (α3β2) (1.4x10-11 – 3.4x10-11 M - Rat), [3H]epibatidine (α3β2) (1.4x10-11 – 3.4x10-11 M - Rat), [125I]epibatidine (α3β4) (2.3x10-10 M), [3H]epibatidine (α3β4) (2.3x10-10 M), [125I]epibatidine (α3β4) (2.9x10-10 – 3.04x10-10 M - Rat), [3H]epibatidine (α3β4) (2.9x10-10 – 3.04x10-10 M - Rat)
Functional characteristics (α1)2βγδ: PCa/PNa = 0.16 - 0.2, Pf = 2.1 – 2.9%; (α1)2βδε: PCa/PNa = 0.65 – 1.38, Pf = 4.1 – 7.2% α2β2: PCa/PNa ∼ 1.5 α3β2: PCa/PNa = 1.5; α3β4: PCa/PNa = 0.78 - 1.1, Pf = 2.7 – 4.6%