Previous names |
Muscle-type, muscle |
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Autonomic, ganglionic |
Selective agonists |
Succinylcholine (selective for (α1)2β1γδ) |
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Positive allosteric modulators |
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LY-2087101 (Broad et al., 2006, also potentiates α4β2 and α4β4) |
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Selective antagonists |
Waglerin-1 (selective for α(1)2β1δε), α-bungarotoxin, α-conotoxin GI, α-conotoxin MI, pancuronium |
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α3β2: α-conotoxin MII (also blocks α6-containing), α-conotoxin-GIC, α-conotoxin PnIA, α-conotoxin TxIA |
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α3β4: α-conotoxin AuIB |
Commonly used antagonists |
(α1)2β1γδ and (α1)2β1δε: α-bungarotoxin, > pancuronium > vecuronium > rocuronium > (+)-Tc (IC50 = 43–82 nM) |
α2β2: DHβE (KB = 0.9 µM), (+)-Tc (KB = 1.4 µM) |
α3β2: DHβE (KB = 1.6 µM, IC50 = 2.0 µM), (+)-Tc (KB = 2.4 µM) |
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α2β4: DHβE (KB = 3.6 µM), (+)-Tc (KB = 4.2 µM) |
α3β4: DHβE (KB = 19 µM, IC50 = 26 µM), (+)-Tc (KB = 2.2 µM) |
Channel blockers |
α(1)2β1δε and α(1)2β1yδ: gallamine (IC50∼ 1 µM) |
mecamylamine, hexamethonium |
α3β2: mecamylamine (IC50 = 7.6 µM), hexamethonium |
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α(1)2β1δε: mecamylamine (IC50∼ 1.5 µM) |
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α3β4: mecamylamine (IC50 = 0.39 µM), hexamethonium |
Radioligands (Kd) |
[3H]/[125I]-α-bungarotoxin |
[3H]/[125I]-epibatidine (hα2β4, 42 pM; rα2β2, 10–21 pM; rα2β4, 84–87 pM), [3H]-cytisine |
[3H]/[125I]-epibatidine (hα3β2, 7 pM; hα3β4, 230 pM; rα3β2, 14–34 pM, rα3β4, 290–304 pM), [3H]-cytisine |
Functional characteristics |
α(1)2βγδ: PCa/PNa = 0.16–0.2, Pf = 2.1–2.9%; α(1)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% |