“Compound 9” is the first potent M3-selective positive allosteric modulator, with potential utility as a biological tool compound. It does have secondary activity against M5 at high doses though. It’s quite a large zwitterion, which is somewhat unusual for GPCRs.
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Sep. 17, 2021
Compound 9: M3-Selective Positive Allosteric Modulator
“Compound 9”
M3-selective positive allosteric modulator oral bioavailability in rodent from HTS and optimization Bioorg. Med. Chem. Apr. 23, 2020 Astellas Pharma, Tsukuba, JP
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