Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00090

Target Information
NameSubstance-K receptor    
Type of targetClinical trial target    
SynonymsNK-2 receptor    
NK-2R    
Neurokinin A receptor    
SKR    
Tachykinin neurokinin 2 receptor    
Tachykinin receptor 2    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1][2]
Anxiety Disorders
[ICD9: 300   ICD10: F40-F42]
[1][2]
Asthma
[ICD9: 493   ICD10: J45]
[3]
Depression
[ICD9: 311   ICD10: F32]
[4][5][6]
Generalized Anxiety Disorders (GAD)
[ICD9: 300   ICD10: F40-F42]
[4][5][6]
Pain, Acute or Chronic
[ICD9: 338,780   ICD10: R52, G89]
[1][2]
Urinary incontinence
[ICD9: 788.3   ICD10: N39.3, N39.4, R32]
[1][2]
Drug(s)NepadutantPhase I/IIInfantile colics; Postoperative ileus[7]
CS-003Discontinued in Phase IIChronic obstructive pulmonary disease[8]
DNK-333Discontinued in Phase IIIrritable Bowel Syndrome With Diarrhea (IBS-D), Asthma[8]
SR 144190DiscontinuedDepression, Acute or Chronic Pain, Anxiety Disorders, Urinary Incontinence[1][2]
SaredutantDiscontinued in Phase III (2009), Positive phase III result (2007)Depression, Generalized Anxiety Disorders[4][5][6]
SLV-332PreclinicalIrritable bowel syndrome[9]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
UniProt IDP21452
FunctionThis is a receptor for the tachykinin neuropeptide substance k (neurokinin a). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.    
SequenceMGTCDIVTEANISSGPESNTTGITAFSMPSWQLALWATAYLALVLVAVTGNAIVIWIILA HRRMRTVTNYFIVNLALADLCMAAFNAAFNFVYASHNIWYFGRAFCYFQNLFPITAMFVS IYSMTAIAADRYMAIVHPFQPRLSAPSTKAVIAGIWLVALALASPQCFYSTVTMDQGATK CVVAWPEDSGGKTLLLYHLVVIALIYFLPLAVMFVAYSVIGLTLWRRAVPGHQAHGANLR HLQAMKKFVKTMVLVVLTFAICWLPYHLYFILGSFQEDIYCHKFIQQVYLALFWLAMSST MYNPIIYCCLNHRFRSGFRLAFRCCPWVTPTKEDKLELTPTTSLSTRVNRCHTKETLFMA GDTAPSEATSGEAGRPQDGSGLWFGYGLLAPTKTHVEI
Related US Patent6,207,678
6,235,735
6,265,614
6,319,917
6,339,094
6,358,994
6,365,602
6,372,754
6,403,582
6,403,601
6,407,106
6,432,952
6,432,953
6,479,518
6,500,818
6,534,502
6,569,872
6,583,142
6,638,930
6,664,253
6,676,950
6,780,875
Target ValidationClick to Find Target Validation Information.    
Inhibitor4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[10]
A-987306[11]
Ac-Phe-[Orn-Pro-cha-Trp-Arg][12]
Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2[12]
L-732138[13]
MEN-14933[14]
WAY-207024[15]
AntagonistCS-003[8]
DNK-333[8]
MEN13510[16]
Nepadutant[7]
SLV-332[9]
SR 144190[1][2]
SR48,968[17]
Saredutant[4][5][6]
MultitargetCS-003[8]
DNK-333[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Pharmacologic evaluation of neurokinin-2 receptor antagonists in the guinea pig respiratory tract. Am J Vet Res. 2004 Jul;65(7):984-91. To Reference
Ref 2Antagonists at the neurokinin receptors--recent patent literature. IDrugs. 2003 Aug;6(8):758-72. To Reference
Ref 3The role of neuroeffector mechanisms in the pathogenesis of asthma. Curr Allergy Asthma Rep. 2001 Mar;1(2):134-43. To Reference
Ref 4Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochem Pharmacol. 2009 May 1;77(9):1522-30. Epub 2009 Feb 6. To Reference
Ref 5Multifaceted approach to determine the antagonist molecular mechanism and interaction of ibodutant ([1-(2-phenyl-1R-[[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl]-ethylcarbamoyl)-cyclopentyl]-amide) at the human tachykinin NK2 receptor. J Pharmacol Exp Ther. 2009 May;329(2):486-95. Epub 2009 Feb 13. To Reference
Ref 6Occurrence and pharmacological characterization of four human tachykinin NK2 receptor variants. Biochem Pharmacol. 2008 Aug 15;76(4):476-81. Epub 2008 Jun 13. To Reference
Ref 7Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26. To Reference
Ref 8Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. To Reference
Ref 9Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. To Reference
Ref 10J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 11J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 12Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. Epub 2006 Jul 28.Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. To Reference
Ref 13J Med Chem. 2010 Aug 12;53(15):5491-501.Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. To Reference
Ref 14Bioorg Med Chem Lett. 2005 Feb 1;15(3):585-8.Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'. To Reference
Ref 15J Med Chem. 2009 Apr 9;52(7):2148-52.Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). To Reference
Ref 16Pharmacology of an original and selective nonpeptide antagonist ligand for the human tachykinin NK2 receptor. Eur J Pharmacol. 2005 Jun 1;516(2):104-11. To Reference
Ref 17Cigarette smoke increases mucosal permeability in guinea pig trachea via tachykinin NK2 receptor activation. Eur J Pharmacol. 2005 Jan 10;507(1-3):223-8. Epub 2004 Dec 24. To Reference



 

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