Skip to main content
. Author manuscript; available in PMC: 2016 Mar 7.
Published in final edited form as: Drug News Perspect. 2010 May;23(4):229–240. doi: 10.1358/dnp.2010.23.4.1416977

Table I.

Abbreviated summary of muscarinic acetylcholine receptor (mAChR) ligands discovered by Vanderbilt University.

Compound Type/mode Potency in cell-based
Ca2+ assay		 Efficacy in rodent
behavioral models		 Electrophysiology/
neurochemistry
TBPB (26) M1 agonist 158 nM at rat M1,
> 30 µM vs. all other
mAChRs		 Amphetamine-induced
hyperlocomotion,
apomorphine-induced PPI		 Potentiates NMDAR
current in CA1,
induces fos expression in
forebrain
VU-0357017 (31) M1 agonist 198 nM at rat M1,
> 30 µM vs. all other
mAChRs		 Scopolamine-induced
disruption of contextual fear
conditioning (acquisition)		 Potentiates NMDAR
current in CA1
VU-0366369 (20) M1 PAM 830 nM at rat M1,
> 30 µM vs. all other
mAChRs		 Not
determined/unpublished		 Not
determined/unpublished
VU-0152100 (34) M4 PAM 380 nM at rat M4,
> 30 µM vs. all other
mAChRs		 Amphetamine-induced
hyperlocomotion		 Not
determined/unpublished
VU-0238429 (38) M5 PAM 1.1 µM at human M5,
> 30 µM vs. all other
mAChRs		 Not
determined/unpublished		 Not
determined/unpublished