JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinityhistamineH₄receptorantagonist, withK_is of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamineH₄receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity^[1][2].

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H₄receptor antagonist with a K_iof 12.5 nM versus the human H₄receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H₄R, the K_i=5.3 nM and the pA2=8.3. At the monkey H₄R, the K_i=25 nM and the pA2=7.5. The affinity for the rat (K_i=188 nM, pA2 = 7.2) and guinea pig H₄R (K_i=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H₄R (K_i≥10 μM). The compound is highly selective for H₄R, as it exhibits low affinity for the H₁, H₂, and H₃receptors^[1].
JNJ-39758979 dihydrochloride is metabolically stable (t_1/2>120 min) when incubatedin vitrowith human, rat, dog, or monkey liver microsomes^[1].

JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the C_max, t_1/2and F values are 0.3 μM, 7.5 hours, 36%, respectively^[1].
JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t_1/2were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively^[1].

294.22

C₁₁H₂₁Cl₂N₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.