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. 2017 Oct 21;174(Suppl Suppl 1):S17–S129. doi: 10.1111/bph.13878
Nomenclature M 1 receptor M 2 receptor
HGNC, UniProt CHRM1, P11229 CHRM2, P08172
Agonists carbachol [350, 888, 2129], pilocarpine (Partial agonist) [888], bethanechol [888] bethanechol [888]
Antagonists glycopyrrolate (pIC50 9.9) [1874], umeclidinium (pK i 9.8) [1090, 1705], AE9C90CB (pK i 9.7) [1818], propantheline (pK i 9.7) [837], atropine (pK i 8.5–9.6) [350, 582, 797, 837, 1555, 1831], tiotropium (pK i 9.6) [452], 4‐DAMP (pK i 9.2) [486] tiotropium (pK i 9.9) [452], umeclidinium (pK i 9.8) [1090, 1705], propantheline (pK i 9.5) [837], glycopyrrolate (Full agonist) (pIC50 9.3) [1874], atropine (pK i 7.8–9.2) [245, 325, 797, 837, 1046, 1437, 1555], AE9C90CB (pK i 8.6) [1818], tolterodine (Inverse agonist) (pK i 8.4–8.6) [642, 1437, 1818]
Selective antagonists biperiden (pK d 9.3) [175], VU0255035 (pK i 7.8) [1786], guanylpirenzepine (pK i 7.3–7.6) [23, 2050] – Rat tripitramine (pK i 9.6) [1240]
Allosteric modulators muscarinic toxin 7 (Negative) (pK i 11–11.1) [1480], benzoquinazolinone 12 (Positive) (pK B 6.6) [4], KT 5720 (Positive) (pK d 6.4) [1110], brucine (Positive) (pK d 4.5–5.8) [888, 1109], BQCA (Positive) (pK B 4–4.8) [4, 5, 271, 1225], VU0029767 (Positive) [1270], VU0090157 (Positive) [1270] W‐84 (Negative) (pK d 6–7.5) [1353, 1983], C7 /3‐phth (Negative) (pK d 7.1) [351], alcuronium (Negative) (pK d 6.1–6.9) [888, 1983], gallamine (Negative) (pK d 5.9–6.3) [363, 1107], LY2119620 (Positive) (pK d 5.7) [399, 1057], LY2033298 (Positive) (pK d 4.4) [2009]
Labelled ligands [3 H]QNB (Antagonist) (pK d 10.6–10.8) [352, 1555], Cy3B‐telenzepine (Antagonist) (pK d 10.5) [777], [3 H]N‐methyl scopolamine (Antagonist) (pK d 9.4–10.3) [294, 350, 352, 797, 888, 889, 918, 977, 1107], [3 H](+)telenzepine (Antagonist) (pK i 9.4) [526] – Rat, Alexa‐488‐telenzepine (Antagonist) (pK d 9.3) [777], [3 H]pirenzepine (Antagonist) (pK d 7.9) [2083], BODIPY‐pirenzepine (Antagonist) (pK i 7) [860], [11 C]butylthio‐TZTP (Agonist) [530], [11 C]xanomeline (Agonist) [530], [18 F](R,R)‐quinuclidinyl‐4‐fluoromethyl‐benzilate (Antagonist) [982] – Rat [3 H]QNB (Antagonist) (pK d 10.1–10.6) [1555], Cy3B‐telenzepine (Antagonist) (pK i 10.4) [1444], [3 H]tiotropium (Antagonist) (pK d 10.3) [1705], [3 H]N‐methyl scopolamine (Antagonist) (pK d 9.3–9.9) [294, 325, 797, 888, 889, 918, 977, 1107, 2072], Alexa‐488‐telenzepine (Antagonist) (pK i 8.8) [1444], [3 H]acetylcholine (Agonist) [1108], [3 H]oxotremorine‐M (Agonist) [141], [3 H]dimethyl‐W84 (Allosteric modulator, Positive) (pK d 8.5) [1983], [18 F]FP‐TZTP (Agonist) [887] – Mouse