Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 345, Issue 3, 1992, Pages 264-269

  Dumuis, A ^a   Gozlan, H ^b   Sebben, M ^a   Ansanay, H ^a   Rizzi, C A ^c   Turconi, M ^c   Monferini, E ^c   Giraldo, E ^c   Schiantarelli, P ^c   Ladinsky, H ^c   Bockaert, J ^b  

^a INSERM   (France)

^b PITIÉ SALPÊTRIÈRE HOSPITAL   (France)

^c Boehringer Ingelheim Italia SpA   (Italy)

Author keywords

5 HT3 receptor antagonist; 5 HT4 receptor antagonist; Azabicycloalkyl benzimidazolone derivatives

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 2,3 DIHYDRO 2 OXO 1 BENZIMIDAZOLECARBOXYLIC ACID 6 METHOXY 3ALPHA TROPANYL ESTER; 2,3 DIHYDRO 3 ISOPROPYL 2 OXO 1 BENZIMIDAZOLECARBOXYLIC ACID 3ALPHA TROPANYLAMIDE; 8 CHLORO 2,3,4,5 TETRAHYDRO 3 METHYL 5 PHENYL 1H 3 BENZAZEPIN 7 OL HYDROGEN MALEATE; ADENYLATE CYCLASE; BENZIMIDAZOLE DERIVATIVE; CLONIDINE; CYCLIC AMP; KETANSERIN; MESULERGINE; METHYLSCOPOLAMINE; METHYSERGIDE; MIANSERIN; NEUROTRANSMITTER RECEPTOR; ONDANSETRON; PINDOLOL; PIRENZEPINE; PRAZOSIN; QUINUCLIDINYL BENZILATE; RADIOLIGAND; RECEPTOR SUBTYPE; RENZAPRIDE; SEROTONIN; SEROTONIN 3 RECEPTOR; SEROTONIN 4 RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR; SPIPERONE; TROPISETRON; ZACOPRIDE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRADYCARDIA; BRAIN; CELL CULTURE; CONCENTRATION RESPONSE; CONTROLLED STUDY; EMBRYO; INTRAVENOUS DRUG ADMINISTRATION; MEMBRANE BINDING; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; REFLEX;

ANIMAL; BENZAMIDES; BENZIMIDAZOLES; BICYCLO COMPOUNDS; BRAIN; CELLS, CULTURED; COMPARATIVE STUDY; CYCLIC AMP; EMBRYO; HEART RATE; INDOLES; KINETICS; MESENCEPHALON; MICE; RATS; RECEPTORS, SEROTONIN; REFLEX; SEROTONIN; SEROTONIN ANTAGONISTS; STIMULATION, CHEMICAL; SUPPORT, NON-U.S. GOV'T;

EID: 0026581581     PISSN: 00281298     EISSN: 14321912     Source Type: Journal    
DOI: 10.1007/BF00168685     Document Type: Article

References (46)

1. Some quantitative uses of drug antagonists
2. 5-hydroxytryptamine 4 receptors mediate relaxation of the rat oesophageal tunica muscularis mucosae
3. Characterisation of the binding of [3H]-SCH 23390, a selective D1 receptor antagonist ligand in rat striatum
4. Pharmacological characterization of 5-HT4 receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: Effect of substituted benzamide derivatives
5. Common pharmacological and physicochemical properties of 5-HT3 binding sites in the rat cerebral cortex and NG-108-15 cloned cells
6. Anxiolytic effects of a new structural class of 5-HT3 antagonists
7. Study of the contractile effect of 5-hydroxytryptamine (5-HT) in the isolated longitudinal muscle strip from guinea pig ileum. Evidence for two distinct release mechanisms
8. SDZ 205-557, a selective antagonist at 5-HT4 receptors in the isolated guinea pig ileum
9. The 5-HT4 receptor: naughty, but nice
10. Pharmacological characterization of a neuronal receptor for 5-hydroxytryptamine in guinea pig ileum with properties similar to the 5-HT4 receptor
11. 5-Methoxytryptamine and 2-methyl-5-hydroxytryptamine induced desensitization as discriminative tools for the 5-HT3 and putative 5-HT4 receptors in guinea pig ileum
12. Dopamine receptor binding: differenciation of agonist and antagonist states with [3H]-dopamine and [3H]-haloperidol
13. A 5-HT receptor in the central nervous system positively coupled with adenylate cyclase is antagonized by ICS 205–930
14. A non classical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system
15. BRL 24924, a potent agonist at a non classical 5-HT receptor positively coupled with adenylate cyclase in colliculi neurons
16. The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate acylase in neurons
17. Azabicycloalkyl benzimidazolone derivatives as a novel class of potent agonists at the 5-HT4 receptor positively coupled to adenylate cyclase in brain
18. Identification of putative 5-HT4 receptors in guinea pig ascending colon
19. MDL 72222: A potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors
20. α-noradrenergic receptor binding in mammalian brain: differential labeling of agonist and antagonist stated
21. Binding characteristics of [3H] prazosin to rat brain α-adrenergic receptors
22. Aging associated changes in serotoninergic and dopaminergic pre- and postsynaptic neurochemical markers in the rat brain
23. Binding profile of a novel cardioselective muscarine receptor antagonist, AF-DX 116 to membranes of peripheral tissues and brain in the rat
24. A 5-hydroxytryptamine receptor in human atrium
25. Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors
26. Ouadid H, Seguin J, Frapier JM, Dumuis A, Bockaert J, Nargeot J (1991) 5-hydroxytryptamine increases CA++ current in human atrial cells via a 5-HT4 receptor positively coupled to adenylate cyclase. J Physiol (Lond) 435:93P
27. Investigation of the 5-hydroxytryptamine receptor mediatin smooth muscle relaxation in the rat oesophagus
28. Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs
29. Increased gut cholinergic activity and antagonism of 5-hydroxytryptamine M-receptors by BRL 24924: potential clinical importance of BRL 24924
30. Activation of a myenteric 5-hydroyxytryptamine-like receptor by metoclopramide
31. The prokinetic properties of new benzimidazolone derivatives are related to 5-HT4 agonism
32. Zacopride, a potent 5-HT3 antagonist
33. Synthesis of a new class of 2–3 dihydro-2-oxo-1-H-benzamidazolone-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists
34. Mediation of 5-hydroxytryptamine induced tachycardia in the pig by the putative 5-HT4 receptor
35. Further characterization, by use of tryptamine and benzamide derivatives, of the putative 5-HT4 receptor mediating tachycardia in the pig
36. 5-HT1D receptors in guinea pig and pigeon brain. Radioligand binding and biochemical studies
37. Synaptogenesis of cultured striatal neurons in serum-free medium: A morphological and biochemical study