Two TRPV1 receptor antagonists are effective in two different experimental models of migraine

Table 1 Pharmacological selectivity of JNJ compounds

	JNJ-38893777	JNJ-17203212
pIC₅₀ (capsaicin)	8.08	7.19
pIC₅₀ (low pH)	8.13	7.8
pK _i (hTRPV1)	8.0	7.3
Activity against related TRP channels^a	no activity (pIC₅₀ < 5)	weak activity against cTRPM8 (pIC₅₀ < 6)
Activity against non-related channels or receptors	weak activity against:	no activity
	human Cholecystokinin 1 receptor (pK _i 6.1)
	human Adenosine 3 receptor (pK _i 6.2)
	rat cerebral cortex sodium channel (pK _i 6.1)

pIC₅₀ values were determined using the recombinant hTRPV1 in a Ca²⁺ influx in vitro assay (FLIPR) [58]. pK _i values were determined by radioligand binding to a broad panel of receptors, channels and transporters at CEREP (Paris, France) [43]
^aActivity was tested against the following related TRP channels: rTRPV2, hTRPV4, hTRPA1, cTRPM8

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