First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain

Journal of Medicinal Chemistry

Volumn 55, Issue 7, 2012, Pages 3488-3501

  Mladenova, Gabriela ^a   Annedi, Subhash C ^a   Ramnauth, Jailall ^a   Maddaford, Shawn P ^a   Rakhit, Suman ^a   Andrews, John S ^a   Zhang, Dongqin ^b   Porreca, Frank ^b  

^a NeurAxon Inc   (Canada)

^b UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANALGESIC AGENT; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; ENDOTHELIAL NITRIC OXIDE SYNTHASE; INDOLE DERIVATIVE; INDUCIBLE NITRIC OXIDE SYNTHASE; N(G) METHYLARGININE; N3 [4 (METHYLAMINO)CYCLOHEX 1 ENYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [3 (ETHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMINE; N[3 [3 (METHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [3 (METHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMINE; N[3 [4 (DIMETHYLAMINO)CYCLOHEX 1 ENYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [4 (DIMETHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [4 (ETHYLAMINO)CYCLOHEX 1 ENYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [4 (ETHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; N[3 [4 (METHYLAMINO)CYCLOHEXYL] 1H INDOL 5 YL]THIOPHENE 2 CARBOXIMIDAMIDE; NEURONAL NITRIC OXIDE SYNTHASE; NITRIC OXIDE SYNTHASE INHIBITOR; NORADRENALIN TRANSPORTER; NORADRENALIN UPTAKE INHIBITOR; PROTRIPTYLINE; UNCLASSIFIED DRUG;

ALLODYNIA; ANALGESIC ACTIVITY; ANIMAL CELL; ARTICLE; CONTROLLED STUDY; CORONARY ARTERY CONSTRICTION; CORONARY ARTERY DILATATION; DRUG DESIGN; DRUG METABOLISM; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN TISSUE; HYPERALGESIA; IC 50; NERVE LIGATION; NEUROPATHIC PAIN; NONHUMAN; POTENCY DISORDER; SPINAL NERVE; STRUCTURE ACTIVITY RELATION;

ADRENERGIC UPTAKE INHIBITORS; ANALGESICS; ANIMALS; CHO CELLS; CORONARY VESSELS; CRICETINAE; CRICETULUS; CYCLOHEXANES; ETHER-A-GO-GO POTASSIUM CHANNELS; HEK293 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INDOLES; MUSCLE CONTRACTION; MUSCLE, SMOOTH, VASCULAR; NEURALGIA; NITRIC OXIDE SYNTHASE TYPE I; NOREPINEPHRINE PLASMA MEMBRANE TRANSPORT PROTEINS; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; VASCULAR RESISTANCE;

EID: 84859787097     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300138g     Document Type: Article

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