TABLE 4

Agonist activity of FE 202158 and AVP at the recombinant mouse, rat, dog, sheep, and pig vasopressin and oxytocin receptors

Species	Receptor	EC₅₀			E_max
Species	Receptor	Mean	95% CI	n	Mean	95% CI	n
		nM			%
FE 202158
Mouse	V_1aR	18	11–30	6	93	83–103	6
Mouse	V₂R	263	213–324	26	84	79–89	26
Rat	V_1aR	0.55	0.43–0.70	11	98	89–107	12
Rat	V₂R	447	359–556	25	82	76–88	25
Dog	V_1aR	0.13	0.09–0.19	5	97	81–112	5
Dog	V₂R	551	369–822	4	78	69–87	4
Sheep	V_1aR	3.8	1.1–13.0	5	102	87–117	5
Sheep	V₂R	489	325–735	8	78	70–85	8
Pig	V_1aR	2.2	1.0–4.5	5	92	75–109	5
Pig	V₂R	150	84–269	7	76	66–86	7
AVP
Mouse	V_1aR	10	9–12	48	100^*	100–100	48
Mouse	V₂R	0.13	0.10–0.16	10	102	88–115	14
Rat	V_1aR	0.07	0.06–0.07	282	100^*	100–100	305
Rat	V₂R	0.03	0.02–0.04	62	100	97–102	57
Dog	V_1aR	0.02	0.01–0.03	9	100^*	100–100	9
Dog	V₂R	0.39	0.13–1.17	8	103	96–110	7
Sheep	V_1aR	1.0	0.7–1.4	19	100^*	100–100	19
Sheep	V2R	0.5	0.3–0.9	5	84	77–91	5
Pig	V_1aR	1.1	0.7–1.7	21	100^*	100–100	21
Pig	V₂R	2.5		2	82		2

↵* Efficacy is expressed as E_max as a percentage of the relative maximal response to the reference agonist in each assay AVP for V_1aR, desmopressin for V₂R.