Table 3. Profiles of Disubstituted Imidazoyl β-Carbolines^a.

	human SSTR3		mouse SSTR3
compd no.	binding IC50 (nM)	functional cAMP antagonism IC50 (nM) (% inh.)	binding IC50 (nM)	functional cAMP antagonism IC50 (nM) (% inh.)	MK-499 binding assay, Ki (nM)	reduction of glucose excursion in mouse oGTT at 1 mg/kg oral doseb
7	0.76	7.3 (91%)	ND	2.4 (101%)	44	NDc
8	0.66	0.95 (83%)	0.36	0.46 (87%)	1701	109%
9	1.1	1.1 (107%)	0.61	3.7 (130%)	1638	63%
10	2.3	3.6 (77%)	1.2	4.8 (92%)	462	81%
11	0.94	0.78 (75%)	0.50	0.14 (68%)	543	80%
12	0.74	0.70 (103%)	0.46	0.48 (113%)	2616	68%
13	0.97	1.2 (69%)	0.59	1.3 (133%)	1403	71%

^aAssay protocols are provided in the Supporting Information. In vitro assay results are the average of at least three duplicates.

^bMice were challenged with oral dose of 5 g/kg dextrose.

^cNot determined.