Structure-activity relationships of inverse agonists for G-protein-coupled receptors

Medicinal Research Reviews

Volumn 25, Issue 4, 2005, Pages 398-426

  Soudijn, Willem ^a,b   Van Wijngaarden, Ineke ^a   Ijzerman, Adriaan P ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Constitutive activity; G protein coupled receptors; Inverse agonists; Structure activity relationships

Indexed keywords

1 [2,3 DIHYDRO 1 (2' METHYLPHENACYL) 2 OXO 5 PHENYL 1H 1,4 BENZODIAZEPIN 3 YL] 3 (3 METHYLPHENYL)UREA; 1 [5 (3 AZABICYCLO[3.2.2]NON 3 YL) 2,3 DIHYDRO 1 METHYL 2 OXO 1H 1,4 BENZODIAZEPIN 3 YL] 3 (3 METHYLPHENYL)UREA; 1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 2 (2 ETHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; 2 (2 METHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; 2 (2,3 DIHYDRO 2 PENTYLBENZOFURAN 2 YL) 2 IMIDAZOLINE; 2 [[2 (2,6 DIMETHOXYPHENOXY)ETHYL]AMINOMETHYL] 1,4 BENZODIOXAN; 2 DIPROPYLAMINO 5 METHOXY 1 METHYLTETRALIN; 2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; 2,3,6,7 TETRAHYDRO 1' METHYL 5 [[2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL) 4 BIPHENYLYL]CARBONYL]SPIRO[FURO[2,3 F]INDOLE 3,4' PIPERIDINE]; 3 [2 [2 (4 METHYL 1 PIPERIDINYL)ETHYL] 1 PYRROLIDINESULFONYL]PHENOL; 3 ISOPROPYLAMINO 1 (7 METHYL 4 INDANYLOXY) 2 BUTANOL; 3' DEOXY N 6 CYCLOPENTYLADENOSINE; 3,N DIMETHYL N [1 METHYL 3 (4 METHYL 1 PIPERIDINYL)PROPYL]BENZENESULFONAMIDE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; 4 CARBOXY 2 METHYLPHENYLGLYCINE; 5 (4 CHLORO 3 METHYLPHENYL) 1 (4 METHYLBENZYL) N (1,3,3 TRIMETHYLBICYCLO[2.2.1]HEPTAN 2 YL) 3 PYRAZOLECARBOXAMIDE; 5 [2 [[2 HYDROXY 3 [4 (1 METHYL 4 TRIFLUOROMETHYL 2 IMIDAZOLYL)PHENOXY]PROPYL]AMINO]ETHOXY]SALICYLAMIDE; 5 CHLORO N [2 (2 CYCLOPROPYLMETHOXYPHENOXY)ETHYL] ALPHA,ALPHA DIMETHYL 1H INDOLE 3 ETHANAMINE; 5 FLUORO 2 METHOXY 1H INDOLE 3 CARBOXYLIC ACID 1 [2 (METHYLSULFONAMIDO)ETHYL] 4 PIPERIDINYLMETHYL ESTER; 5 METHOXY 1 METHYL 2 PROPYLAMINOTETRALIN; 6 N (5 HYDROXYNORBORNAN 2 YL) 8 (N ISOPROPYL N METHYLAMINO) 9 METHYLADENINE; 8 [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] 8 AZASPIRO[4.5]DECANE 7,9 DIONE; 8 [2 [4 (5 CHLORO 2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] 8 AZASPIRO[4.5]DECANE 7,9 DIONE; 8 [3 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]PROPYLCARBAMOYL] 3 METHYLFLAVONE; 8 [3 [4 (5 CHLORO 2 METHOXYPHENYL) 1 PIPERAZINYL]PROPYLCARBAMOYL] 2 CYCLOHEXYL 3 METHYL 4H 1 BENZOPYRAN 4 ONE; 8 [3 [4 (5 CHLORO 2 METHOXYPHENYL) 1 PIPERAZINYL]PROPYLCARBAMOYL] 3 METHYLFLAVONE; 8 AMINO 7 CHLORO 1,4 BENZODIOXAN 5 CARBOXYLIC ACID 1 BUTYL 4 PIPERIDINYLMETHYL ESTER; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; 9 CHLORO 2 (2 FURYL) 5,6 DIHYDRO 5 IMINO 1,2,4 TRIAZOLO[2,3 C]QUINAZOLINE; ADENOSINE A1 RECEPTOR ANTAGONIST; ADENOSINE A3 RECEPTOR ANTAGONIST; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; ALFUZOSIN; ALPHA 2 ADRENERGIC RECEPTOR BLOCKING AGENT; ALPRENOLOL; ATROPINE; BAY 36 7620; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; BETAXOLOL; CANNABINOID RECEPTOR ANTAGONIST; CETIRIZINE; CHOLECYSTOKININ B RECEPTOR ANTAGONIST; CLOBENPROPIT; CLOZAPINE; DOPAMINE 1 RECEPTOR BLOCKING AGENT; DOPAMINE 2 RECEPTOR BLOCKING AGENT; DOPAMINE 3 RECEPTOR BLOCKING AGENT; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR BLOCKING AGENT; GCS 15943; HISTAMINE H1 RECEPTOR ANTAGONIST; HISTAMINE H2 RECEPTOR ANTAGONIST; HISTAMINE H3 RECEPTOR ANTAGONIST; HORMONE RECEPTOR BLOCKING AGENT; IDAZOXAN; IODOPHENPROPIT; LUF 5603; LUF 5608; LUF 5644; MEDETOMIDINE; MELATONIN RECEPTOR BLOCKING AGENT; MEPYRAMINE; METABOTROPIC RECEPTOR ANTAGONIST; METOPROLOL; MIZOLASTINE; MUSCARINIC RECEPTOR BLOCKING AGENT; N 6 CYCLOPENTYLADENOSINE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; OLANZAPINE; OTENZEPAD; PIBOSEROD; PRAZOSIN; PROPRANOLOL; PSB 10; PSB 11; RACLOPRIDE; RAUWOLSCINE; REC 15 2615; RIMONABANT; RISPERIDONE; RO 116 0086; RO 116 1148; RS 100235; RX 831001; RX 851057; RX 851062; SB 258741; SEROTONIN ANTAGONIST; TAMSULOSIN; TIMOLOL; TIOTIDINE; TROPAPRIDE; UNCLASSIFIED DRUG; VUF 4903; VUF 4904; VUF 5202; YOHIMBINE; ZIPRASIDONE;

DRUG BINDING; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; HEART FAILURE; HUMAN; NONHUMAN; RECEPTOR AFFINITY; REVIEW; STRUCTURE ACTIVITY RELATION;

ADRENERGIC BETA-AGONISTS; ANIMALS; DOPAMINE AGONISTS; HISTAMINE AGONISTS; HUMANS; MUSCARINIC AGONISTS; RECEPTOR, ADENOSINE A1; RECEPTOR, ADENOSINE A3; RECEPTORS, ADRENERGIC, ALPHA-1; RECEPTORS, ADRENERGIC, ALPHA-2; RECEPTORS, CANNABINOID; RECEPTORS, G-PROTEIN-COUPLED; SEROTONIN AGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 21744441782     PISSN: 01986325     EISSN: None     Source Type: Journal    
DOI: 10.1002/med.20031     Document Type: Review

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