JNJ-7777120

JNJ-7777120
Clinical data
Other names	1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine
Identifiers
	IUPAC name 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole;
CAS Number	459168-41-3 ;
PubChem CID	4908365;
IUPHAR/BPS	1278;
ChemSpider	4090750 ;
UNII	4H1AU2V37X;
ChEMBL	ChEMBL129198 ;
CompTox Dashboard (EPA)	DTXSID20963461 ;
ECHA InfoCard	100.164.683
Chemical and physical data
Formula	C14H16ClN3O
Molar mass	277.75 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C3CN(C)CCN3C(=O)c(cc1c2)[nH]c1ccc2Cl;
	InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 ; Key:HUQJRYMLJBBEDO-UHFFFAOYSA-N ;
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JNJ-7777120 was a drug being developed by Johnson & Johnson Pharmaceutical Research & Development which acts as a potent and selective antagonist at the histamine H₄ receptor.^[1] It has anti-inflammatory effects,^[2] and has been demonstrated to be superior to traditional (H1) antihistamines in the treatment of pruritus (itching).^[3] The drug was abandoned because of its short in vivo half-life and hypoadrenocorticism toxicity in rats and dogs, that prevented advancing it into clinical studies.^[4]

References

^ Jiang W, Lim HD, Zhang M, et al. (July 2008). "Cloning and pharmacological characterization of the dog histamine H(4) receptor". Eur. J. Pharmacol. 592 (1–3): 26–32. doi:10.1016/j.ejphar.2008.06.095. PMID 18639542.
^ Thurmond RL, Desai PJ, Dunford PJ, Fung-Leung WP, Hofstra CL, Jiang W, Nguyen S, Riley JP, Sun S, Williams KN, Edwards JP, Karlsson L (Apr 2004). "A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties". Journal of Pharmacology and Experimental Therapeutics. 309 (1): 404–13. doi:10.1124/jpet.103.061754. PMID 14722321. S2CID 8396875.
^ Dunford PJ, Williams KN, Desai PJ, Karlsson L, McQueen D, Thurmond RL (Jan 2007). "Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus". Journal of Allergy and Clinical Immunology. 119 (1): 176–83. doi:10.1016/j.jaci.2006.08.034. PMID 17208599.
^ Thurmond RL, Venable J, Savall B, La D, Snook S, Dunford PJ, Edwards JP (2017). "Clinical Development of Histamine H4 Receptor Antagonists". Histamine and Histamine Receptors in Health and Disease. Handbook of Experimental Pharmacology. Vol. 241. pp. 301–320. doi:10.1007/164_2016_130. ISBN 978-3-319-58192-7. PMID 28233185.

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