JNJ-7777120: Difference between revisions

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+{{Short description|Chemical compound}}
-{{Drugbox|
+{{Drugbox
-|IUPAC_name = 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1''H''-indole
+| Verifiedfields = changed
-| synonyms=<small>1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine</small>
+| verifiedrevid = 394360889
-| image=JNJ7777120.png
+| IUPAC_name = 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1''H''-indole
-| CAS_number= 459168-41-3
+| image = JNJ-7777120.svg
-| ATC_prefix=
+| alt = Skeletal formula of JNJ-7777120
-| ATC_suffix=
+| image2 = JNJ-7777120-3D-spacefill.png
-| PubChem= 4908365
+| alt2 = Ball-and-stick model of the JNJ-7777120 molecule
-| IUPHAR_ligand = 1279
+<!--Clinical data-->
+| tradename =
+| routes_of_administration =
+<!--Identifiers-->
+| CAS_number_Ref = {{cascite|correct|??}}
+| CAS_number = 459168-41-3
+| UNII_Ref = {{fdacite|correct|FDA}}
+| UNII = 4H1AU2V37X
+| PubChem = 4908365
 | IUPHAR_ligand = 1278
+| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
-| DrugBank=
+| ChEMBL_Ref = {{ebicite|changed|EBI}}
-| C=14 | H=16 | Cl=1 | N=3 | O=1
+| ChEMBL = 129198
-| molecular_weight = 277.749 g/mol
+| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
-| smiles = C3CN(C)CCN3C(=O)c(cc1c2)nc1ccc2Cl
+| ChemSpiderID = 4090750
-| bioavailability=
-| metabolism =
+<!--Chemical data-->
-| elimination_half-life=
+| C=14 | H=16 | Cl=1 | N=3 | O=1
-| excretion =
+| smiles = C3CN(C)CCN3C(=O)c(cc1c2)[nH]c1ccc2Cl
-| pregnancy_category =
+| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
-| legal_status =
+| StdInChI = 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
-| routes_of_administration=
+| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
+| StdInChIKey = HUQJRYMLJBBEDO-UHFFFAOYSA-N
+| synonyms = <small>1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine</small>
 }}
-'''JNJ-7777120''' is a drug being developed by [[Johnson & Johnson Pharmaceutical Research & Development]] which acts as a potent and selective [[Receptor antagonist|antagonist]] at the [[histamine H4 receptor]].<ref name="pmid18639542">{{cite journal |author=Jiang W, Lim HD, Zhang M, ''et al.'' |title=Cloning and pharmacological characterization of the dog histamine H(4) receptor |journal=Eur. J. Pharmacol. |volume= |issue= |pages= |year=2008 |month=July |pmid=18639542 |doi=10.1016/j.ejphar.2008.06.095 |url=http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(08)00709-7}}</ref> It has [[antiinflammatory]] effects,<ref>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. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. ''Journal of Pharmacology and Experimental Therapeutics''. 2004 Apr;309(1):404-13. PMID 14722321</ref> and has been demonstrated to be superior to traditional antihistamines in the treatment of [[pruritus]] (itching).<ref>Dunford PJ, Williams KN, Desai PJ, Karlsson L, McQueen D, Thurmond RL. Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus. ''Journal of Allergy and Clinical Immunology''. 2007 Jan;119(1):176-83. PMID 17208599</ref>
+'''JNJ-7777120''' was a drug being developed by [[Johnson & Johnson Pharmaceutical Research & Development]] which acts as a potent and selective [[Receptor antagonist|antagonist]] at the [[histamine H4 receptor|histamine H<sub>4</sub> receptor]].<ref name="pmid18639542">{{cite journal  |vauthors=Jiang W, Lim HD, Zhang M, etal |title=Cloning and pharmacological characterization of the dog histamine H(4) receptor |journal=Eur. J. Pharmacol. |volume= 592|issue= 1–3|pages= 26–32|date=July 2008 |pmid=18639542 |doi=10.1016/j.ejphar.2008.06.095 }}</ref> It has [[anti-inflammatory]] effects,<ref>{{cite journal | vauthors = 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 | date = Apr 2004 | title = A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 309 | issue = 1| pages = 404–13 | pmid = 14722321 | doi = 10.1124/jpet.103.061754 | s2cid = 8396875 }}</ref> and has been demonstrated to be superior to traditional (H1) antihistamines in the treatment of [[pruritus]] (itching).<ref>{{cite journal | vauthors = Dunford PJ, Williams KN, Desai PJ, Karlsson L, McQueen D, Thurmond RL | date = Jan 2007 | title = Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus | journal = Journal of Allergy and Clinical Immunology | volume = 119 | issue = 1| pages = 176–83 | pmid = 17208599 | doi = 10.1016/j.jaci.2006.08.034 }}</ref> The drug was abandoned because of its short ''[[in vivo]]'' [[Biological half-life|half-life]] and [[hypoadrenocorticism]] toxicity in rats and dogs, that prevented advancing it into clinical studies.<ref>{{cite book | vauthors = Thurmond RL, Venable J, Savall B, La D, Snook S, Dunford PJ, Edwards JP | title = Histamine and Histamine Receptors in Health and Disease | date = 2017 | chapter = Clinical Development of Histamine H4 Receptor Antagonists | series = Handbook of Experimental Pharmacology | volume = 241 | pages = 301–320 | pmid = 28233185 | doi = 10.1007/164_2016_130 | isbn = 978-3-319-58192-7 }}</ref>
+== See also ==
+* [[VUF-6002]]
 ==References==
@@ Line 30: / Line 47: @@
 {{Piperazines}}
+[[Category:Carboxamides]]
+[[Category:Chloroarenes]]
+[[Category:H4 receptor antagonists]]
 [[Category:Indoles]]
+[[Category:Drugs developed by Johnson & Johnson]]
 [[Category:Piperazines]]
-[[Category:Amides]]
+[[Category:Abandoned drugs]]
-[[Category:Organochlorides]]
-[[Category:H4 receptor antagonists]]
 {{pharma-stub}}
-[[sv:JNJ-7777120]]