INT49521

Context Info Confidence 0.04 First Reported 1995 Last Reported 1998 Negated 2 Speculated 0 Reported most in Abstract Documents 5 Total Number 5 Disease Relevance 0.22 Pain Relevance 1.90

nucleus (Rtcd1) molecular_function (Rtcd1) ligase activity (Rtcd1)

Anatomy Link Frequency skin 1 Rtcd1 (Mus musculus)

Pain Link Frequency Relevance Heat Kappa opioid receptor 6 99.36 Neuropeptide 1 97.92 Central nervous system 1 97.48 antagonist 6 96.98 Dynorphin 1 96.80 Opioid 4 95.66 agonist 8 93.36 opioid receptor 5 92.56 Sumatriptan 1 92.54 Morphine 4 91.04

Disease Link Frequency Relevance Heat Thymoma 4 75.00 Hyperalgesia 1 68.64 Bordatella Infection 2 42.40 Nociception 1 5.00

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

To determine whether kappa opioid receptor function was maintained by spare receptors after agonist-induced down-regulation, membranes from untreated R1.1 cells were incubated with 400 nM of the irreversible opioid antagonist beta-chlornaltrexamine (beta-CNA) followed by extensive washing. beta-CNA produced a 50% reduction in the [3H]U69,593 binding and a 6-fold increase in the IC50 value for (-)-U50,488 inhibition of adenylyl cyclase activity, with no change in the maximal inhibition of cyclic AMP levels.

cyclase Binding (activity) of associated with antagonist, agonist, kappa opioid receptor and opioid

1) Confidence 0.04 Published 1995 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 7891351 Disease Relevance 0.07 Pain Relevance 0.44

The R1.1 cell line and its derivatives, R1.G1 and R1EGO, express a similar type of kappa opioid receptor, which exhibits differences in coupling to G-proteins and to adenylyl cyclase among cell lines.

cyclase Binding (coupling) of associated with kappa opioid receptor

2) Confidence 0.04 Published 1995 Journal Biochem. Pharmacol. Section Abstract Doc Link 7840787 Disease Relevance 0.07 Pain Relevance 0.23

Here we report the isolation, on the basis of its ability to inhibit the cyclase in a stable recombinant CHO(ORL1+) cell line, of a neuropeptide that resembles dynorphin A9 and whose amino acid sequence is Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln.

cyclase Neg (inhibit) Binding (inhibit) of associated with dynorphin and neuropeptide

3) Confidence 0.01 Published 1995 Journal Nature Section Abstract Doc Link 7566152 Disease Relevance 0.07 Pain Relevance 0.36

The effects of agonists and antagonists comprised: (i) agonist potencies in the order 5-carboxamidotryptamine > 5-HT > sumatriptan > 8-hydroxy-2-(di-n-propylamino)tetralin; (ii) inhibition of contractile action of 5-HT by the 5-HT1D antagonist GR 127935; (iii) a contractile response to methysergide; (iv) a lack of effect of tropisetron, an antagonist of 5-HT3 and 5-HT4 receptors; and (v) inhibition of forskolin-stimulated cAMP formation by 5-HT (in the presence of LY 53857), indicative of negative coupling to adenylate cyclase. 4.

cyclase Neg (negative) Binding (coupling) of associated with sumatriptan, antagonist and agonist

4) Confidence 0.00 Published 1998 Journal Clin. Exp. Pharmacol. Physiol. Section Abstract Doc Link 9590577 Disease Relevance 0 Pain Relevance 0.46

These results suggest that L-Arg increases transport in toad skin presumably acting through the formation of nitric oxide, which then stimulates cytoplasmic guanylate cyclase and leads to increased Na+ and K+ transport.

cyclase Binding (leads) of in skin

5) Confidence 0.00 Published 1996 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8982659 Disease Relevance 0 Pain Relevance 0.40

General Comments

This test has worked.