581809-67-8Relevant academic research and scientific papers
N-Isoquinolin-5-yl-N′-aralkyl-urea and -amide antagonists of human vanilloid receptor 1
Jetter, Michele C.,Youngman, Mark A.,McNally, James J.,Zhang, Sui-Po,Dubin, Adrienne E.,Nasser, Nadia,Dax, Scott L.
, p. 3053 - 3056 (2004)
Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N′-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described.
Design, synthesis, and evaluation of isoquinoline ureas as trpv1 antagonists
Gujarati, Nehaben A.,Korlipara, Vijaya L.,Undem, Bradley J.
, p. 202 - 211 (2020/03/06)
Background: The inhibition of transient receptor potential vanilloid receptor 1 (TRPV1) has emerged as a novel approach for the treatment of various pain states. Pyrrolidinyl urea, SB 705498 with pKb = 7.3 in guinea pig TRPV1 receptor has been
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain; Structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaliue, and cinnoline moieties
Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Guo, Zhu Zheng,Perner, Richard J.,Didomenico, Stanley,Koenig, John R.,Turner, Sean,Jinkerson, Tammie,Drizin, Irene,Hannick, Steven M.,Macri, Bryan S.,McDonald, Heath A.,Honore, Prisca,Wismer, Carol T.,Marsh, Kennan C.,Wetter, Jill,Stewart, Kent D.,Oie, Tetsuro,Jarvis, Michael F.,Surowy, Carol S.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 744 - 752 (2007/10/03)
Novel transient receptor potential vanilloid 1 (TRPV1) receptor antagonists with various bicyclic heteroaromatic pharmacophores were synthesized, and their in vitro activity in blocking capsaicin activation of TRPV1 was assessed. On the basis of the contribution of these pharmacophores to the in vitro potency, they were ranked in the order of 5-isoquinoline > 8-quinoline = 8-quinazoline > 8-isoquinoline ≥ cinnoline ≈ phthalazine ≈ quinoxaline ≈ 5-quinoline. The 5-isoquinoline-containing compound 14a (hTRPV1 IC50 = 4 nM) exhibited 46% oral bioavailability and in vivo activity in animal models of visceral and inflammatory pain. Pharmacokinetic and pharmacological properties of 14a are substantial improvements over the profile of the high-throughput screening hit 1 (hTRPV1 IC50 = 22 nM), which was not efficacious in animal pain models and was not orally bioavailable.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2 and L are as defined in the description.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Page/Page column 23, (2010/02/11)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
NAPHTHOL, QUINOLINE AND ISOQUINOLINE-DERIVED UREA MODULATORS OF VANILLOID VR1 RECEPTOR
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Page 137, (2008/06/13)
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
-
, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
-
, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
