INT100722

Context Info Confidence 0.52 First Reported 2002 Last Reported 2009 Negated 0 Speculated 0 Reported most in Abstract Documents 7 Total Number 7 Disease Relevance 2.56 Pain Relevance 6.14

cell differentiation (YY1) chromosome organization (YY1) RNA binding (YY1) plasma membrane (YY1) nucleus (YY1) intracellular (YY1)

Anatomy Mention Frequency neurons 2 superior 1 spinal cord 1 nerve 1 brain 1 YY1 (Homo sapiens)

Pain Term Frequency Confidence Heat Neurotransmitter 7 100.00 pregabalin 48 100.00 Neuropathic pain 1 99.92 Gabapentin 8 99.90 gABA 5 99.24 Calcium channel 7 98.96 GABA receptor 2 98.60 Analgesic 3 98.08 anticonvulsant 3 97.04 Spinal cord 2 96.84

Disease Term Frequency Confidence Heat Anxiety Disorder 20 100.00 Neuropathic Pain 1 99.92 Depression 2 87.16 Pain 4 85.04 Generalized Anxiety Disorder 4 83.72 Epilepsy 1 82.72 Mental Disorders 1 81.12 Partial Seizures 1 75.00 Post Operative Pain 4 75.00 Convulsion 2 74.48

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Pain term

Disease term

Pregabalin, the pharmacologically active S-enantiomer of 3-aminomethyl-5-methyl-hexanoic acid, is a structural analogue of GABA, although it is not active at GABA receptors, nor does it acutely alter GABA uptake or degradation.black triangle Pregabalin binds with high affinity to the alpha2-delta subunit protein of voltage-gated calcium channels in CNS tissues and acts as a presynaptic modulator of the excessive release, in hyperexcited neurons, of various excitatory neurotransmitters.

Pregabalin Binding (binds) of delta in neurons associated with pregabalin, neurotransmitter, gaba, calcium channel and gaba receptor

1) Confidence 0.52 Published 2006 Journal CNS Drugs Section Abstract Doc Link 16863276 Disease Relevance 0.32 Pain Relevance 0.78

Pregabalin binds to the alpha2-delta subunit of a neuronal voltage-gated calcium channel and is believed to exert its anticonvulsant effect by modulating the release of specific neurotransmitters from hyperexcited presynaptic neurons.

Pregabalin Binding (binds) of delta in neurons associated with pregabalin, neurotransmitter, calcium channel and anticonvulsant

2) Confidence 0.52 Published 2008 Journal Expert Rev Neurother Section Abstract Doc Link 18590472 Disease Relevance 0.30 Pain Relevance 0.58

Gabapentin and pregabalin may bind to the Ca(2+) channel alpha 2 delta subunit to selectively attenuate depolarization-induced Ca(2+) influx of presynaptic P/Q-type Ca(2+) channels; this results in decreased glutamate/aspartate release from excitatory amino acid nerve terminals leading to a reduced activation of AMPA heteroreceptors on noradrenergic nerve terminals.

pregabalin Binding (bind) of delta in nerve associated with pregabalin, glutamate, gabapentin and excitatory amino acid

3) Confidence 0.40 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 11804619 Disease Relevance 0 Pain Relevance 1.16

Pregabalin is a new anxiolytic that acts as a presynaptic inhibitor of the release of excessive levels of excitatory neurotransmitters by selectively binding to the alpha2-delta subunit of voltage-gated calcium channels.

Pregabalin Binding (binding) of delta associated with pregabalin, neurotransmitter, calcium channel and anxiety disorder

4) Confidence 0.39 Published 2005 Journal J Clin Psychopharmacol Section Abstract Doc Link 15738746 Disease Relevance 0.59 Pain Relevance 0.43

BACKGROUND: Pregabalin inhibits release of excess excitatory neurotransmitters, presumably by binding to the alpha2-delta subunit protein of widely distributed voltage-dependent calcium channels in the brain and spinal cord.

Pregabalin Binding (binding) of delta in spinal cord associated with pregabalin, neurotransmitter, calcium channel and spinal cord

5) Confidence 0.39 Published 2005 Journal Arch. Gen. Psychiatry Section Abstract Doc Link 16143734 Disease Relevance 0.07 Pain Relevance 0.40

Binding of pregabalin to the alpha2-delta subunit appears necessary for its demonstrable anxiolytic, analgesic and anticonvulsant activities in animal models.black triangle Oral pregabalin, typically at dosages of 300-600 mg/day, was superior to placebo and similar to lorazepam 6 mg/day, alprazolam 1.5 mg/day and venlafaxine 75 mg/day in improving anxiety and depressive symptoms in patients with moderate-to-severe generalised anxiety disorder (GAD).

pregabalin Binding (Binding) of delta in superior associated with pregabalin, depression, generalized anxiety disorder, analgesic, anxiety disorder and anticonvulsant

6) Confidence 0.39 Published 2006 Journal CNS Drugs Section Abstract Doc Link 16863276 Disease Relevance 0.58 Pain Relevance 0.94

Pregabalin is thought to act by reducing the excessive release of several excitatory neurotransmitters by binding to the alpha(2)-delta protein subunit of voltage-gated calcium channels.

Pregabalin Binding (binding) of delta associated with pregabalin, neurotransmitter and calcium channel

7) Confidence 0.39 Published 2009 Journal Drugs Aging Section Abstract Doc Link 19761281 Disease Relevance 0.62 Pain Relevance 1.46

BACKGROUND: Pregabalin inhibits release of excess excitatory neurotransmitters, presumably by binding to the alpha2-delta subunit protein of widely distributed voltage-dependent calcium channels in the brain and spinal cord.

Pregabalin Binding (binding) of delta in brain associated with pregabalin, neurotransmitter, calcium channel and spinal cord

8) Confidence 0.13 Published 2005 Journal Arch. Gen. Psychiatry Section Abstract Doc Link 16143734 Disease Relevance 0.07 Pain Relevance 0.40

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