INT37219

Context Info Confidence 0.78 First Reported 1987 Last Reported 2011 Negated 1 Speculated 6 Reported most in Abstract Documents 56 Total Number 62 Disease Relevance 32.40 Pain Relevance 54.16

plasma membrane (TACR1) cytoplasm (TACR1) signal transducer activity (TACR1)

Anatomy Link Frequency neurons 11 dorsal horn 7 spinal 3 blood vessels 2 spinal cord 2 TACR1 (Homo sapiens)

Pain Link Frequency Relevance Heat substance P 324 100.00 Pain 198 100.00 antagonist 70 100.00 agonist 31 100.00 Neuropeptide 24 100.00 opioid receptor 19 100.00 Opioid 19 100.00 Glutamate receptor 4 100.00 gABA 2 100.00 Dorsal horn neuron 19 99.98

Disease Link Frequency Relevance Heat INFLAMMATION 123 99.84 Pain 135 99.80 Pancreatitis 94 99.76 Complex Regional Pain Syndromes 20 99.52 Hyperalgesia 56 99.12 Gastrointestinal Disease 1 99.04 Nervous System Injury 9 98.92 Enteropathy 9 98.44 Hypertension 3 98.24 Asthma 7 97.80

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

In the present study, the human Achilles and patellar tendons were examined concerning immunohistochemical expression of the NK-1 receptor.

Spec (examined) Gene_expression (expression) of NK-1 receptor in tendons

1) Confidence 0.78 Published 2005 Journal Regul. Pept. Section Abstract Doc Link 15664664 Disease Relevance 0.18 Pain Relevance 0.26

The immunohistochemical expression of various neuropeptides, including substance P (SP), and the substance P receptor (SPR), was examined in irradiation-induced enteropathy in man.

Spec (examined) Gene_expression (expression) of SPR associated with enteropathy, neuropeptide and substance p

2) Confidence 0.77 Published 2000 Journal Regul. Pept. Section Abstract Doc Link 10706946 Disease Relevance 0.42 Pain Relevance 0.34

The immunohistochemical expression of various neuropeptides, including substance P (SP), and the substance P receptor (SPR), was examined in irradiation-induced enteropathy in man.

Spec (examined) Gene_expression (expression) of substance P receptor associated with enteropathy, neuropeptide and substance p

3) Confidence 0.77 Published 2000 Journal Regul. Pept. Section Abstract Doc Link 10706946 Disease Relevance 0.42 Pain Relevance 0.34

Human monocytes and macrophages express substance P and neurokinin-1 receptor.

Gene_expression (express) of neurokinin-1 receptor in macrophages associated with qutenza and substance p

4) Confidence 0.75 Published 1997 Journal J. Immunol. Section Title Doc Link 9548509 Disease Relevance 0 Pain Relevance 0.49

Spinal NK-1 receptor expressing neurons mediate opioid-induced hyperalgesia and antinociceptive tolerance via activation of descending pathways.

Gene_expression (expressing) of NK-1 receptor in neurons associated with pain, hyperalgesia, tolerance, antinociceptive and opioid

5) Confidence 0.70 Published 2007 Journal Pain Section Title Doc Link 17123731 Disease Relevance 0.49 Pain Relevance 1.76

Thus, NK-1 receptor expressing neurons play a critical role in sustained morphine-induced neuroplastic changes which underlie spinal excitability reflected as thermal and tactile hypersensitivity to peripheral stimuli, and to reduced antinociceptive actions of spinal morphine (i.e., antinociceptive tolerance).

Gene_expression (expressing) of NK-1 receptor in spinal associated with hypersensitivity, tolerance, antinociceptive and morphine

6) Confidence 0.70 Published 2007 Journal Pain Section Abstract Doc Link 17123731 Disease Relevance 0.54 Pain Relevance 1.95

Ablation of NK-1 receptor expressing cells prevented (a) morphine-induced thermal and mechanical hypersensitivity, (b) increased touch-evoked spinal FOS expression, (c) upregulation of spinal dynorphin content and (d) the rightward displacement of the spinal morphine antinociceptive dose-response curve (i.e., tolerance).

Gene_expression (expressing) of NK-1 receptor in spinal associated with dynorphin, hypersensitivity, tolerance, antinociceptive and morphine

7) Confidence 0.70 Published 2007 Journal Pain Section Abstract Doc Link 17123731 Disease Relevance 0.55 Pain Relevance 1.73

Here, the role of NK-1 receptor expressing cells in the spinal dorsal horn in morphine-induced hyperalgesia and spinal antinociceptive tolerance was assessed by ablating these cells with intrathecal injection of SP-saporin (SP-SAP).

Gene_expression (expressing) of NK-1 receptor in dorsal horn associated with hyperalgesia, spinal dorsal horn, tolerance, antinociceptive, intrathecal and morphine

8) Confidence 0.70 Published 2007 Journal Pain Section Abstract Doc Link 17123731 Disease Relevance 0.48 Pain Relevance 1.56

A novel neurokinin-1 receptor antagonist, (+/-)-(1R( *),3S( *),4S( *),5S( *))-4-[(N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-3-phenyl-2-aza-7-oxabicyclo[3.3.0]octane (1), was synthesized stereoselectively using Padwa's intramolecular 1,3-dipolar cycloaddition methodology as the key step.

Gene_expression (synthesized) of neurokinin-1 receptor associated with antagonist

9) Confidence 0.67 Published 2007 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 17967540 Disease Relevance 0 Pain Relevance 0.16

Immunoprecipitation of SPR from 32Pi-labeled Chinese hamster ovary cells stably expressing human SPR (CHO-hSPR) indicates that substance P (SP) causes a rapid (T1/2 < 1 min), dose-dependent (EC50 = 2 nM), and pronounced (5-fold over basal) phosphorylation of SPR.

Gene_expression (expressing) of SPR in ovary associated with substance p

10) Confidence 0.67 Published 1999 Journal Mol. Pharmacol. Section Abstract Doc Link 10220564 Disease Relevance 0.09 Pain Relevance 0.46

Effects of tachykinin receptor antagonists on cumulative additions of hHK-1 to guinea pig airways

Gene_expression (antagonists) of tachykinin receptor associated with antagonist

11) Confidence 0.64 Published 2010 Journal Respir Res Section Body Doc Link PMC2959027 Disease Relevance 0 Pain Relevance 0.51

Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.

Gene_expression (synthesis) of neurokinin-1 receptor associated with antagonist

12) Confidence 0.60 Published 2007 Journal Bioorg. Med. Chem. Lett. Section Title Doc Link 17967540 Disease Relevance 0 Pain Relevance 0.18

Accordingly, numerous NK1 receptor antagonists have either been synthesized and are under clinical development, or have already been tested in clinical trials.

Gene_expression (synthesized) of NK1 receptor associated with antagonist

13) Confidence 0.59 Published 2006 Journal Med Monatsschr Pharm Section Abstract Doc Link 16792196 Disease Relevance 0.52 Pain Relevance 0.62

In contrast with the results in human bronchi, SP and the specific NK1-receptor agonist produced maximal responses similar to those of NKA and hHK-1 in guinea pig airways providing evidence of the higher involvement of NK1 receptors in this animal species than in humans as already reported [23,40].

Gene_expression (produced) of NK1-receptor associated with agonist and substance p

14) Confidence 0.58 Published 2010 Journal Respir Res Section Body Doc Link PMC2959027 Disease Relevance 0 Pain Relevance 0.58

We also analyzed whether an association exists between NK-1R mRNA expression and pain and inflammation.

Gene_expression (expression) of NK-1R mRNA associated with pain and inflammation

15) Confidence 0.54 Published 2001 Journal Pain Section Abstract Doc Link 11275376 Disease Relevance 1.52 Pain Relevance 1.50

Quantitative PCR was used to determine the NK-1R mRNA expression levels and in situ hybridization and immunohistochemistry were used to localize expression sites of NK-1R mRNA and protein, respectively.

Gene_expression (expression) of NK-1R mRNA

16) Confidence 0.54 Published 2001 Journal Pain Section Abstract Doc Link 11275376 Disease Relevance 1.39 Pain Relevance 1.39

NK-1 receptor gene expression is related to pain in chronic pancreatitis.

Gene_expression (expression) of NK-1 receptor gene associated with pain and chronic pancreatitis

17) Confidence 0.54 Published 2001 Journal Pain Section Title Doc Link 11275376 Disease Relevance 1.30 Pain Relevance 1.53

In CP samples, in situ hybridization and immunohistochemistry localized NK-1R mRNA expression and protein mainly in the nerves, ganglia, blood vessels, inflammatory cells and occasionally in fibroblasts.

Gene_expression (expression) of NK-1R mRNA in blood vessels associated with inflammation and chronic pancreatitis

18) Confidence 0.54 Published 2001 Journal Pain Section Abstract Doc Link 11275376 Disease Relevance 1.75 Pain Relevance 1.67

Quantitative PCR was used to determine the NK-1R mRNA expression levels and in situ hybridization and immunohistochemistry were used to localize expression sites of NK-1R mRNA and protein, respectively.

Spec (determine) Gene_expression (expression) of NK-1R mRNA

19) Confidence 0.54 Published 2001 Journal Pain Section Abstract Doc Link 11275376 Disease Relevance 1.28 Pain Relevance 1.29

This study analyzed the expression and localization of neurokinin 1 receptor (NK-1R), which binds SP, and its association with pain and inflammation in CP.

Spec (analyzed) Gene_expression (expression) of NK-1R associated with pain, inflammation, chronic pancreatitis and substance p

20) Confidence 0.54 Published 2001 Journal Pain Section Abstract Doc Link 11275376 Disease Relevance 1.16 Pain Relevance 1.24

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