BIOMAT Database Logo BIOMAT Database Logo

Biochemical and pharmacological activities of SR 144190, a new potent non-peptide tachykinin NK2 receptor antagonist. 1997

X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
Sanofi Recherche, Montpellier, France.

(R)-3-(1-[2-(4-benzoyl-2-(3,4-difluorophenyl)-morpholin-2-yl)- ethyl]-4-phenylpiperidin-4-yl)-1-dimethylurea (SR 144190) is a new non-peptide antagonist of tachykinin NK2 receptors. SR 144190 potently and selectively inhibited neurokinin A binding to NK2 receptors from various species, including humans. In in vitro functional assays, it was a potent, selective and competitive antagonist of NK2 receptors with apparent affinities (pA2 values) between 9.08 and 10.10. In vivo, SR 144190 blocked [Nle10]neurokinin A-(4-10)-induced bronchoconstriction in guinea pigs (ID50 = 21 micrograms kg-1 i.v. and 250 micrograms kg-1 i.d.) and [beta Ala8]neurokinin A-(4-10)-induced urinary bladder contraction in rats (ID50 = 11 micrograms kg-1 i.v. and 190 micrograms kg-1 i.d.). It prevented citric acid-induced cough and airway hyperresponsiveness to acetylcholine in guinea pigs (1 mg kg-1 i.p.) as well as castor oil-induced diarrhoea in rats (0.01-10 micrograms kg-1 s.c. or p.o). Finally, it blocked the turning behaviour induced by intrastriatal injections of [Nle10]neurokinin A-(4-10) in mice (ID50 = 3 micrograms kg-1 i.v. and 16 micrograms kg-1 p.o.).

UI MeSH Term Description Entries
D008297 Male Males
D008782 Methylurea Compounds Urea compounds which are substituted with one or more methyl groups. Compounds, Methylurea
D009025 Morpholines Tetrahydro-1,4-Oxazines,Tetrahydro 1,4 Oxazines
D012137 Respiratory System The tubular and cavernous organs and structures, by means of which pulmonary ventilation and gas exchange between ambient air and the blood are brought about. Respiratory Tract,Respiratory Systems,Respiratory Tracts,System, Respiratory,Tract, Respiratory
D002490 Central Nervous System The main information-processing organs of the nervous system, consisting of the brain, spinal cord, and meninges. Cerebrospinal Axis,Axi, Cerebrospinal,Axis, Cerebrospinal,Central Nervous Systems,Cerebrospinal Axi,Nervous System, Central,Nervous Systems, Central,Systems, Central Nervous
D004064 Digestive System A group of organs stretching from the MOUTH to the ANUS, serving to breakdown foods, assimilate nutrients, and eliminate waste. In humans, the digestive system includes the GASTROINTESTINAL TRACT and the accessory glands (LIVER; BILIARY TRACT; PANCREAS). Ailmentary System,Alimentary System
D005260 Female Females
D005849 Gerbillinae A subfamily of the Muridae consisting of several genera including Gerbillus, Rhombomys, Tatera, Meriones, and Psammomys. Gerbils,Jird,Meriones,Psammomys,Rats, Sand,Gerbil,Jirds,Merione,Rat, Sand,Sand Rat,Sand Rats
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006224 Cricetinae A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS. Cricetus,Hamsters,Hamster

Related Publications

X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
February 1997, The Journal of pharmacology and experimental therapeutics,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors.
January 1995, European journal of pharmacology,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
In vivo and in vitro pharmacology of SR 48,968, a non-peptide tachykinin NK2 receptor antagonist.
March 1993, European journal of pharmacology,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.
September 1995, Journal of medicinal chemistry,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.
January 1995, Life sciences,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
The non-peptide tachykinin NK2 receptor antagonist SR 48968 interacts with human, but not rat, cloned tachykinin NK3 receptors.
February 1994, Biochemical and biophysical research communications,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist.
October 1991, The Journal of pharmacology and experimental therapeutics,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist.
August 1992, The Journal of pharmacology and experimental therapeutics,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
MEN 11420 (Nepadutant), a novel glycosylated bicyclic peptide tachykinin NK2 receptor antagonist.
January 1998, British journal of pharmacology,
X Emonds-Alt, and C Advenier, and C Cognon, and T Croci, and S Daoui, and J P Ducoux, and M Landi, and E Naline, and G Neliat, and M Poncelet, and V Proietto, and D Van Broeck, and P Vilain, and P Soubrié, and G Le Fur, and J P Maffrand, and J C Brelière
MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist.
November 2006, European journal of pharmacology,
Copied contents to your clipboard!