JNJ-39393406 is an experimental medication which is under development by Janssen Pharmaceutica, a division of Johnson & Johnson, for the treatment of depressive disorders and smoking withdrawal.[1] It acts as a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR).[1] It does not act on the α4β2 or α3β4 nAChRs or the serotonin 5-HT3 receptor, and does not interact with a panel of 62 other receptors and enzymes.[2] The drug has been found to lower the agonist and nicotine threshold for activation of the α7 nAChR by 10- to 20-fold and to increase the maximum agonist response of the α7 nAChR by 17- to 20-fold.[2]

JNJ-39393406
Clinical data
Routes of
administration
By mouth[1]
Drug classAntinicotinic
Identifiers
  • 3-[3-[(2,2-Difluoro-1,3-benzodioxol-5-yl)amino]-5-pyridin-4-yl-1,2,4-triazol-1-yl]-N,N-dimethylpropanamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H18F2N6O3
Molar mass416.389 g·mol−1
3D model (JSmol)
  • CN(C)C(=O)CCN1C(=NC(=N1)NC2=CC3=C(C=C2)OC(O3)(F)F)C4=CC=NC=C4
  • InChI=1S/C19H18F2N6O3/c1-26(2)16(28)7-10-27-17(12-5-8-22-9-6-12)24-18(25-27)23-13-3-4-14-15(11-13)30-19(20,21)29-14/h3-6,8-9,11H,7,10H2,1-2H3,(H,23,25)
  • Key:IURMHZBQEYNQOH-UHFFFAOYSA-N

As of February 2018, JNJ-39393406 is in phase II clinical trials for both depressive disorders and smoking withdrawal.[1] It was also under investigation for the treatment of schizophrenia and Alzheimer's disease, but development for these indications was discontinued.[1]

See also

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References

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  1. ^ a b c d e "JNJ-39393406". Adis Insight.
  2. ^ a b Winterer G, Gallinat J, Brinkmeyer J, Musso F, Kornhuber J, Thuerauf N, Rujescu D, Favis R, Sun Y, Franc MA, Ouwerkerk-Mahadevan S, Janssens L, Timmers M, Streffer JR (2013). "Allosteric alpha-7 nicotinic receptor modulation and P50 sensory gating in schizophrenia: a proof-of-mechanism study". Neuropharmacology. 64: 197–204. doi:10.1016/j.neuropharm.2012.06.040. PMID 22766391. S2CID 29118435.