TABLE 1

Summary of effects of LY593093 and reference muscarinic agonist compounds on stimulation of calcium mobilization in whole cells (CHO) stably expressing human M1, M3, or M5 muscarinic receptors

Data were analyzed using nonlinear regression for a sigmoidal concentration-response curve (Prism version 4.0) and are expressed as mean ± S.E.M. from n ≥ 3 separate experiments. Potency data are expressed in log₁₀ molar (M) units, and efficacy data are expressed as a percentage of response at 10 μM oxotremorine M.

Compound	M1AChR		M3AChR		M5AChR
Compound	EC₅₀	E_max	EC₅₀	E_max	EC₅₀	E_max
	log₁₀ M	%	log₁₀ M	%	log₁₀ M	%
LY593093	−7.30 ± −8.20	85.3 ± 2.86	−5.21 ± −5.60	43.9 ± 0.98	>−4.00	^*
Acetylcholine	−7.62 ± −8.64	130 ± 3.90	−8.77 ± −9.82	124 ± 10.0	−7.39 ± −7.76	124 ± 18.8
Alvameline	−6.36 ± −7.28	46.9 ± 7.72	−5.82 ± −6.43	44.0 ± 8.99	>−4.00	^*
Sabcomeline	−8.27 ± −9.30	87.1 ± 4.41	−8.39 ± −9.30	99.3 ± 3.96	−7.44 ± −8.19	27.6 ± 3.03
Talsaclidine	−6.57 ± −7.42	104 ± 4.37	−5.96 ± −6.64	97.5 ± 8.17	>−4.00	^*
Xanomeline	−7.22 ± −7.76	115 ± 4.32	−6.58 ± −7.42	92.4 ± 9.20	−5.86 ± −6.26	64.2 ± 8.77

↵* Indicates <20% efficacy at the highest doses tested (100 nM).