INT16194

Context Info Confidence 0.48 First Reported 1991 Last Reported 2011 Negated 3 Speculated 2 Reported most in Abstract Documents 82 Total Number 84 Disease Relevance 20.75 Pain Relevance 39.59

aging (CNR1) plasma membrane (CNR1) response to stress (CNR1) signal transducer activity (CNR1)

Anatomy Link Frequency brain 14 neuron 3 CNS 2 cerebellum 2 nerves 2 CNR1 (Homo sapiens)

Pain Link Frequency Relevance Heat Cannabinoid 579 100.00 Cannabinoid receptor 400 100.00 agonist 254 100.00 antagonist 236 100.00 Analgesic 119 100.00 Central nervous system 59 100.00 intrathecal 30 100.00 Opioid 20 100.00 Hippocampus 13 100.00 GABAergic 3 100.00

Disease Link Frequency Relevance Heat Cancer 282 100.00 Disease 224 100.00 Pancreatitis 128 99.96 Hypothermia 14 99.80 Pain 265 99.76 Glioma 6 99.70 Neuroblastoma 4 99.52 Appetite Loss 41 99.04 INFLAMMATION 189 98.56 Obesity 238 98.40

Sentences Mentioned In

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Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

The present investigation examines several series of CP-47,497 analogs for their binding affinity at the cannabinoid receptor and their ability to evoke analgesia in rodents.

cannabinoid receptor Binding (affinity) of associated with cannabinoid receptor and analgesia

1) Confidence 0.48 Published 1993 Journal Mol. Pharmacol. Section Abstract Doc Link 8246904 Disease Relevance 0 Pain Relevance 1.05

This structure-activity relationship investigation was initiated to determine which effects might correspond to binding affinity for the cannabinoid receptor, as well as to explore the binding requirements of this site.

cannabinoid receptor Spec (might) Binding (affinity) of associated with cannabinoid receptor

2) Confidence 0.47 Published 1993 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8474008 Disease Relevance 0 Pain Relevance 0.22

In turn, the activated post-synaptic neuron releases endocannabinoids such as anandamide (Freund et al 2003; Navari 2003; Piomelli 2003) These endogenous CB1 ligands then diffuse back and bind to the pre-synaptic CB1 receptor (Piomelli 2003).

CB1 receptor Binding (bind) of in neuron associated with endocannabinoid

3) Confidence 0.47 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2503671 Disease Relevance 0.34 Pain Relevance 0.89

AJA binds weakly to CB1 only at concentrations many fold higher than its therapeutic range, and is, therefore, completely free of psychotropic effects in both normal subjects and pain patients suggesting the involvement of a target site other than CB1.

CB1 Binding (binds) of associated with pain

4) Confidence 0.47 Published 2005 Journal Life Sci. Section Abstract Doc Link 16005906 Disease Relevance 0.26 Pain Relevance 0.41

Most of the agonists exhibit nonselective affinity for CB1/CB2 receptors, and delta9-THC and anandamide probably act as partial agonists.

CB1 Binding (affinity) of associated with agonist

5) Confidence 0.47 Published 1999 Journal Crit Rev Neurobiol Section Abstract Doc Link 10803637 Disease Relevance 0 Pain Relevance 0.61

To this date, it has been documented the presence in the CNS of specific lipids that bind naturally to the CB1/CB2 receptors.

CB1 Binding (bind) of in CNS associated with central nervous system

6) Confidence 0.46 Published 2008 Journal Prog. Neuropsychopharmacol. Biol. Psychiatry Section Abstract Doc Link 18514375 Disease Relevance 0.06 Pain Relevance 0.44

Anandamide (arachidonylethanolamide), isolated from porcine brain, has been shown to bind to the cannabinoid receptor and also to produce cannabimimetic activity in pharmacological assays.

cannabinoid receptor Binding (bind) of in brain associated with cannabinoid receptor

7) Confidence 0.45 Published 1995 Journal Life Sci. Section Abstract Doc Link 7776830 Disease Relevance 0 Pain Relevance 0.11

Structure-activity relationships for cannabinoid receptor-binding and analgesic activity: studies of bicyclic cannabinoid analogs.

cannabinoid receptor Binding (binding) of associated with cannabinoid receptor, cannabinoid and analgesic

8) Confidence 0.41 Published 1993 Journal Mol. Pharmacol. Section Title Doc Link 8246904 Disease Relevance 0 Pain Relevance 1.20

The cannabinoid receptor mediating this response has been characterized by its ability to bind the cannabinoid agonist [3H]CP-55,940 and to inhibit adenylyl cyclase via Gi.

cannabinoid receptor Binding (bind) of associated with cannabinoid receptor, cannabinoid and agonist

9) Confidence 0.41 Published 1993 Journal Mol. Pharmacol. Section Abstract Doc Link 8246904 Disease Relevance 0 Pain Relevance 0.72

Two CB receptors have been identified in humans (CB1 and CB2) which are recognized exclusively by cannabinoids.

CB1 Binding (recognized) of associated with cannabinoid

10) Confidence 0.41 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2503671 Disease Relevance 0.82 Pain Relevance 0.73

Anandamide (arachidonylethanolamide) is a brain constituent which binds to the cannabinoid receptor.

cannabinoid receptor Binding (binds) of in brain associated with cannabinoid receptor

11) Confidence 0.39 Published 1993 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8384116 Disease Relevance 0 Pain Relevance 0.29

A new class of cannabinoid ligands was rationally designed from known aminoalkylindole agonists and showed good binding and functional activities at human CB1 and CB2 receptors.

CB1 Binding (binding) of associated with cannabinoid and agonist

12) Confidence 0.37 Published 2007 Journal J. Med. Chem. Section Abstract Doc Link 17630726 Disease Relevance 0.09 Pain Relevance 0.53

In addition, recent evidence indicates a more general role of CB1 receptors in reward-related memories, which is consistent with the proposed role of endocannabinoids in memory-related plasticity.

CB1 Binding (role) of associated with endocannabinoid

13) Confidence 0.37 Published 2005 Journal Trends Pharmacol. Sci. Section Abstract Doc Link 15992935 Disease Relevance 0.44 Pain Relevance 0.44

Unlike NADA, OLDA was only a weak ligand for rat CB1 receptors; but like NADA, it was recognized by the anandamide membrane transporter while being a poor substrate for fatty-acid amide hydrolase.

CB1 Binding (ligand) of

14) Confidence 0.36 Published 2003 Journal J. Biol. Chem. Section Abstract Doc Link 12569099 Disease Relevance 0.24 Pain Relevance 0.54

This compound displays nanomolar affinity (Ki = 0.56 and 3.5 nM) for both the rat brain and human CB1 recombinant receptors, respectively.

CB1 Binding (affinity) of in brain

15) Confidence 0.36 Published 2004 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15131245 Disease Relevance 0 Pain Relevance 0.12

CB1A, Ki = 298 nM), these agonists bound to CB1A (CP 55,940, WIN 55212-2 and delta 9-THC, Ki = 7.24,345 and 26.7 nM, respectively) with about 3-fold less affinity than to CB1 (CP 55,940, WIN 55212-2 and delta 9-THC, Ki = 2.26, 93 and 7.1 nM, respectively).

CB1A Binding (bound) of associated with agonist

16) Confidence 0.36 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8768742 Disease Relevance 0 Pain Relevance 0.45

CB1A, Ki = 298 nM), these agonists bound to CB1A (CP 55,940, WIN 55212-2 and delta 9-THC, Ki = 7.24,345 and 26.7 nM, respectively) with about 3-fold less affinity than to CB1 (CP 55,940, WIN 55212-2 and delta 9-THC, Ki = 2.26, 93 and 7.1 nM, respectively).

CB1A Binding (bound) of associated with agonist

17) Confidence 0.36 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8768742 Disease Relevance 0 Pain Relevance 0.45

In turn, the activated post-synaptic neuron releases endocannabinoids such as anandamide (Freund et al 2003; Navari 2003; Piomelli 2003) These endogenous CB1 ligands then diffuse back and bind to the pre-synaptic CB1 receptor (Piomelli 2003).

CB1 Binding (bind) of in neuron associated with endocannabinoid

18) Confidence 0.35 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2503671 Disease Relevance 0.34 Pain Relevance 0.91

We observed that LASSBio-881 (3c) was able to bind to CB1 receptors (71% at 100microM) and also to inhibit T-cell proliferation (66% at 10microM) probably by binding to CB2 receptors, in a non-proapoptotic manner, different from anandamide (1).

CB1 Binding (bind) of in T-cell

19) Confidence 0.35 Published 2007 Journal Bioorg. Med. Chem. Section Abstract Doc Link 17275312 Disease Relevance 0.09 Pain Relevance 0.18

In direct binding assays on isolated membranes the agonist [3H]CP 55,940 bound in a saturable and highly specific manner to both cannabinoid receptor isoforms.

cannabinoid receptor Binding (bound) of associated with cannabinoid receptor and agonist

20) Confidence 0.32 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8768742 Disease Relevance 0 Pain Relevance 0.37

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