INT26707

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Context Info
Confidence 0.35
First Reported 1983
Last Reported 2005
Negated 0
Speculated 0
Reported most in Abstract
Documents 21
Total Number 21
Disease Relevance 6.01
Pain Relevance 7.43

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

small molecule metabolic process (PPAP2A) plasma membrane (PPAP2A) lipid metabolic process (PPAP2A)
Anatomy Link Frequency
fat cells 4
blood platelet 1
cavity 1
central nervous system 1
ovary 1
PPAP2A (Homo sapiens)
Pain Link Frequency Relevance Heat
Clonidine 54 100.00 Very High Very High Very High
agonist 40 100.00 Very High Very High Very High
antagonist 17 100.00 Very High Very High Very High
Potency 11 100.00 Very High Very High Very High
adenocard 4 100.00 Very High Very High Very High
opiate 1 98.44 Very High Very High Very High
Central nervous system 2 97.60 Very High Very High Very High
depression 2 95.16 Very High Very High Very High
Catecholamine 4 93.64 High High
noradrenaline 6 91.84 High High
Disease Link Frequency Relevance Heat
Obesity 39 100.00 Very High Very High Very High
Irritable Bowel Syndrome /

Irritable Bowel Syndrome Super

5 99.24 Very High Very High Very High
Thyroid Disease 4 97.88 Very High Very High Very High
Depression 3 96.68 Very High Very High Very High
Heart Rate Under Development 13 95.96 Very High Very High Very High
Adhesions 127 94.40 High High
Hypotension 14 91.12 High High
Cognitive Disorder 2 87.32 High High
Sleep Disorders 8 83.16 Quite High
Bordatella Infection 1 74.44 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Specific high-affinity binding of the alpha 2 agonist 3H-clonidine and the alpha 2 antagonist 3H-yohimbine was used to determine the number (Bmax) of alpha 2 receptors and the dissociation constant (KD) for the 2 ligands.
alpha 2 Binding (binding) of associated with antagonist, agonist and clonidine
1) Confidence 0.35 Published 1983 Journal Am. J. Cardiol. Section Abstract Doc Link 6305182 Disease Relevance 0.32 Pain Relevance 0.39
Specific high-affinity binding of the alpha 2 agonist 3H-clonidine and the alpha 2 antagonist 3H-yohimbine was used to determine the number (Bmax) of alpha 2 receptors and the dissociation constant (KD) for the 2 ligands.
alpha 2 Binding (binding) of associated with antagonist, agonist and clonidine
2) Confidence 0.35 Published 1983 Journal Am. J. Cardiol. Section Abstract Doc Link 6305182 Disease Relevance 0.32 Pain Relevance 0.40
Clonidine had a higher affinity for alpha-2 sites in femoral fat cells and was equipotent in the omental and abdominal ones.
alpha-2 Binding (affinity) of in fat cells associated with obesity and clonidine
3) Confidence 0.34 Published 1987 Journal Eur. J. Clin. Invest. Section Abstract Doc Link 3034620 Disease Relevance 0.68 Pain Relevance 0.26
For alpha-2 antagonists, the potency order was: yohimbine greater than idazoxan greater than SK&F-86,466 much greater than benextramine; 3) a description of the impact of benextramine (irreversible alpha-1/alpha-2 antagonist) on human fat cell alpha-2 adrenergic receptors and on human fat cell function; the drug inactivates the alpha-2 adrenergic receptors with a minor impact on beta adrenergic receptors and without noticeable alterations of fat cell function as assessed by preservation of beta adrenergic and Al-adenosine receptor-mediated lipolytic responses; and 4) a definition of the relationship existing between alpha-2 adrenergic receptor occupancy, inhibition of adenylate cyclase activity and antilipolysis with full and partial agonists.
alpha-2 Binding (definition) of in fat cell associated with adenocard, antagonist, obesity, agonist and potency
4) Confidence 0.32 Published 1989 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 2566681 Disease Relevance 0.70 Pain Relevance 0.51
Heterogeneous distribution of beta and alpha-2 adrenoceptor binding sites in human fat cells from various fat deposits: functional consequences.
alpha-2 Binding (binding) of in fat cells associated with obesity
5) Confidence 0.30 Published 1987 Journal Eur. J. Clin. Invest. Section Title Doc Link 3034620 Disease Relevance 0.50 Pain Relevance 0.22
Comparative studies on the antihypertensive potency of selective alpha 2 agonists like rilmenidine, guanfacine, clonidine and lofexidine suggest that the relative ability to bind to alpha 1 and alpha 2 adrenoceptors is not critical but the ability to enter the central nervous system is essential for antihypertensive efficacy.
alpha 2 Binding (bind) of in central nervous system associated with agonist, central nervous system, clonidine and potency
6) Confidence 0.30 Published 1988 Journal Am. J. Cardiol. Section Abstract Doc Link 2894151 Disease Relevance 0 Pain Relevance 0.40
The specific binding of the alpha2-subtype-selective [3H]-RX 821002 confirms the presence of alpha2-adrenoceptors in the human placenta, while [3H]-idazoxan binds to non-adrenergic IBS.
alpha2-adrenoceptors Binding (binds) of in placenta
7) Confidence 0.25 Published 1998 Journal Mol. Hum. Reprod. Section Abstract Doc Link 9620839 Disease Relevance 0 Pain Relevance 0.08
Adrenoceptor antagonists displaced binding in a simple monomolecular fashion with an order of affinity rauwolscine greater than yohimbine greater than phentolamine greater than corynanthine greater than prazosin indicating binding to alpha-2-adrenoceptors.
alpha-2-adrenoceptors Binding (binding) of associated with antagonist
8) Confidence 0.21 Published 1983 Journal Life Sci. Section Abstract Doc Link 6136881 Disease Relevance 0 Pain Relevance 0.48
Specific binding of 3H-clonidine to alpha 2 adrenoreceptors upon human blood platelet membranes is increased in patients with major depressive disorder (endogenous depression).
alpha 2 Binding (binding) of in blood platelet associated with depression and clonidine
9) Confidence 0.19 Published 1983 Journal Prog. Neuropsychopharmacol. Biol. Psychiatry Section Abstract Doc Link 6310693 Disease Relevance 0.32 Pain Relevance 0.28
Alpha 2- and beta-adrenergic receptor binding and action in gluteal adipocytes from patients with hypothyroidism and hyperthyroidism.
Alpha 2 Binding (binding) of in adipocytes associated with thyroid disease and obesity
10) Confidence 0.09 Published 1987 Journal Metab. Clin. Exp. Section Title Doc Link 2823049 Disease Relevance 0.77 Pain Relevance 0.22
However, these substances also interacted in differing degrees with alpha-1, alpha-2, beta-adrenergic, 5-HT-1, 5-HT-2, and opiate sites.
alpha-2 Binding (interacted) of associated with opiate
11) Confidence 0.05 Published 1988 Journal J. Pharm. Pharmacol. Section Abstract Doc Link 2901473 Disease Relevance 0 Pain Relevance 0.28
These differences in rank order potency are consistent with the recent proposal of alpha-2 receptor subtypes, a rauwolscine-sensitive site (Rs) that binds clonidine greater than B-HT920 greater than guanfacine and a rauwolscine-insensitive site (Ri) that binds guanfacine greater than clonidine greater than B-HT920 (Boyajian and Leslie, 1987).
alpha-2 Binding (binds) of associated with clonidine and potency
12) Confidence 0.05 Published 1988 Journal J. Neurosci. Section Abstract Doc Link 2903226 Disease Relevance 0.62 Pain Relevance 0.96
Interactions between the presynaptic alpha2-autoreceptor and presynaptic inhibitory heteroreceptors on noradrenergic neurones.
alpha2-autoreceptor Binding (Interactions) of
13) Confidence 0.04 Published 1998 Journal Brain Res. Bull. Section Title Doc Link 9820729 Disease Relevance 0 Pain Relevance 0.74
These differences in rank order potency are consistent with the recent proposal of alpha-2 receptor subtypes, a rauwolscine-sensitive site (Rs) that binds clonidine greater than B-HT920 greater than guanfacine and a rauwolscine-insensitive site (Ri) that binds guanfacine greater than clonidine greater than B-HT920 (Boyajian and Leslie, 1987).
alpha-2 Binding (binds) of associated with clonidine and potency
14) Confidence 0.04 Published 1988 Journal J. Neurosci. Section Abstract Doc Link 2903226 Disease Relevance 0.63 Pain Relevance 0.97
Chloroethylclonidine, an alkylating derivative of the alpha2-adrenergic agonist clonidine, binds irreversibly to alpha2A-ARs by forming a covalent bond with the sulfhydryl side chain of a cysteine residue exposed in the binding cavity, leading to inactivation of the receptor.
alpha2A Binding (binds) of in cavity associated with agonist and clonidine
15) Confidence 0.03 Published 1998 Journal Mol. Pharmacol. Section Abstract Doc Link 9495800 Disease Relevance 0 Pain Relevance 0.15
Chloroethylclonidine binds irreversibly to exposed cysteines in the fifth membrane-spanning domain of the human alpha2A-adrenergic receptor.
alpha2A Binding (binds) of
16) Confidence 0.03 Published 1998 Journal Mol. Pharmacol. Section Title Doc Link 9495800 Disease Relevance 0 Pain Relevance 0.10
Competition studies with several imidazoli(di)ne/guanidine drugs and other nonrelated structures were performed in cortical membranes against [3H]idazoxan (4 nM in the presence of 10(-6) M I-epinephrine to prevent binding to alpha-2 adrenoceptors) or [3H]RX821002 (1 nM).
alpha-2 Binding (binding) of
17) Confidence 0.02 Published 1993 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8095548 Disease Relevance 0 Pain Relevance 0.13
In contrast, the 2-methoxy derivative of idazoxan, 2-methoxy idazoxan (RX821002), binds almost exclusively to alpha-2 adrenoceptors.
alpha-2 Binding (binds) of
18) Confidence 0.02 Published 1993 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8095548 Disease Relevance 0 Pain Relevance 0.10
Gene filter data from two patients also showed similar pattern of collagen, type 1 (alpha 2), fibronectin 1, MMP-1, TGF-?
alpha 2 Binding (pattern) of
19) Confidence 0.02 Published 2005 Journal Reprod Biol Endocrinol Section Body Doc Link PMC548295 Disease Relevance 0.68 Pain Relevance 0.03
Ligand- and subtype-selective coupling of human alpha-2 adrenoceptors to Ca++ elevation in Chinese hamster ovary cells.
alpha-2 Binding (coupling) of in ovary
20) Confidence 0.01 Published 1998 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 9808694 Disease Relevance 0.07 Pain Relevance 0.33

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