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 |