INT20715

Context Info Confidence 0.48 First Reported 1980 Last Reported 2007 Negated 3 Speculated 2 Reported most in Abstract Documents 45 Total Number 49 Disease Relevance 4.03 Pain Relevance 13.17

transport (Sigmar1) nuclear envelope (Sigmar1) lipid particle (Sigmar1) endoplasmic reticulum (Sigmar1) plasma membrane (Sigmar1) nucleus (Sigmar1)

Anatomy Link Frequency brain 8 pyramidal cells 1 liver 1 CSF 1 caudate putamen 1 Sigmar1 (Rattus norvegicus)

Pain Link Frequency Relevance Heat fortral 86 100.00 opiate 8 100.00 opioid receptor 6 100.00 Calcium channel 1 100.00 agonist 27 99.96 antagonist 12 99.48 Enkephalin 9 99.38 Dopamine 24 99.34 narcan 18 98.98 nMDA receptor 13 98.96

Disease Link Frequency Relevance Heat Myocardial Infarction 7 99.76 Cancer 5 99.30 Schizophrenia 3 99.24 Psychosis 9 99.16 Disease 6 98.00 Shock 1 97.76 Drug Induced Neurotoxicity 4 94.08 Cv Unclassified Under Development 1 93.40 Dystonia 5 91.28 Movement Disorders 4 90.40

Sentences Mentioned In

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The present study was undertaken to examine whether repeated exposure of rats to the psychostimulant drug, methamphetamine, induces changes in sigma receptor binding.

sigma receptor Binding (binding) of

1) Confidence 0.48 Published 1993 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8422906 Disease Relevance 0.16 Pain Relevance 0.14

Further, the prototypic sigma receptor ligands, such as 1,3-di-o-tolylguanidine (DTG), (+)3-PPP, and progesterone, bound poorly to the protein.

sigma receptor Binding (bound) of

2) Confidence 0.45 Published 1997 Journal Synapse Section Abstract Doc Link 9021892 Disease Relevance 0 Pain Relevance 0.64

MS-377 ((R)-(+)-1-(4-chlorophenyl)-3-[4-(2-methoxyethyl)piperazin-1-yl]methyl-2-pyrrolidinone L-tartrate) is a antipsychotic agent that binds to sigma-1 receptor.

sigma-1 receptor Binding (binds) of

3) Confidence 0.40 Published 2002 Journal Life Sci. Section Abstract Doc Link 11991251 Disease Relevance 0.09 Pain Relevance 0.04

Influence of trishomocubanes on sigma receptor binding of N-(1-benzyl-piperidin-4-yl)-4-[123I]iodobenzamide in vivo in the rat brain.

sigma receptor Binding (binding) of in brain

4) Confidence 0.40 Published 2005 Journal Medicinal chemistry (Sh?riqah (United Arab Emirates)) Section Title Doc Link 16789883 Disease Relevance 0.06 Pain Relevance 0.11

The interaction of these functionalised trishomocubanes on the binding of the known sigma receptor radioligand, 4-[123I]IBP, was evaluated in the rat brain.

sigma receptor Binding (binding) of in brain

5) Confidence 0.40 Published 2005 Journal Medicinal chemistry (Sh?riqah (United Arab Emirates)) Section Abstract Doc Link 16789883 Disease Relevance 0.09 Pain Relevance 0.15

The sigma receptor ligand (+)-3-hydroxyphenyl-N-(1-propyl)piperidine ((+)-3-PPP) binds with a Kd of 17.9 +/- 4.0 nM and a Bmax of 275 +/- 32.1 fmol/mg protein.

sigma receptor Binding (binds) of

6) Confidence 0.39 Published 1995 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8566148 Disease Relevance 0 Pain Relevance 0.09

Because a single population of binding sites (R(2) = 0.992) for [(125)I]IAF interaction with the sigma-1 receptor was identified by (+)-[(3)H]pentazocine competitive binding with nonradioactive [(127)I]IAF, it was concluded that SBDLI (amino acids 91-109) and SBDLII (amino acids 176-194) comprises, at least in part, regions of the sigma-1 receptor ligand binding site(s).

sigma-1 receptor Binding (interaction) of associated with fortral

7) Confidence 0.37 Published 2007 Journal Mol. Pharmacol. Section Abstract Doc Link 17622576 Disease Relevance 0 Pain Relevance 0.10

Because fenpropimorph has high-binding affinity to the sigma-1 receptor, we have synthesized a series of fenpropimorph-like derivatives with varying phenyl ring substituents and have characterized their binding affinities to the sigma-1 receptor.

sigma-1 receptor Binding (affinity) of

8) Confidence 0.37 Published 2007 Journal Mol. Pharmacol. Section Abstract Doc Link 17622576 Disease Relevance 0 Pain Relevance 0.04

To further examine the nature of the interaction between sigma receptor ligands and the dopamine transporter, the effects of sigma receptor ligands on amphetamine-stimulated [3H]dopamine release were examined in slices prepared from rat caudate putamen.

sigma receptor Spec (examine) Binding (interaction) of in caudate putamen associated with dopamine

9) Confidence 0.35 Published 1998 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9652359 Disease Relevance 0 Pain Relevance 0.63

Sigma receptor ligands caused changes in beating frequencies which were followed by irregular contractions.

Sigma receptor Binding (ligands) of

10) Confidence 0.34 Published 1994 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8014874 Disease Relevance 0 Pain Relevance 0

Some sigma receptor ligands have been shown to bind with low affinity to the dopamine transporter and to inhibit [3H]dopamine uptake.

sigma receptor Binding (bind) of associated with dopamine

11) Confidence 0.34 Published 1998 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9652359 Disease Relevance 0 Pain Relevance 0.47

However, the protein was not the sigma receptor. [3H](+)SKF-10047 binding to the protein was inhibited by the following compounds in the order of decreasing potency: (+)pentazocine > (-) pentazocine > (+/-)cyclazocine > (-)morphine > (-)naloxone > haloperidol > (+)SKF-10047 > DADLE > (-)SKF-10047.

sigma receptor Binding (binding) of associated with fortral, narcan, morphine and potency

12) Confidence 0.33 Published 1997 Journal Synapse Section Abstract Doc Link 9021892 Disease Relevance 0 Pain Relevance 0.53

In search of a mechanism of action we observed that procaine is a ligand for the sigma1 receptor, a protein which ligands have been shown to protect mitochondrial function and to exert antidepressant properties.

sigma1 receptor Binding (ligand) of associated with antidepressant

13) Confidence 0.33 Published 2005 Journal Pharmacology Section Abstract Doc Link 15687733 Disease Relevance 0.87 Pain Relevance 0.30

Therefore, it cannot be attributed to sigma receptor interactions with certainty.

sigma receptor Binding (interactions) of

14) Confidence 0.32 Published 1990 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2155804 Disease Relevance 0.09 Pain Relevance 0.35

These effects of MS-377 may depend on its affinity for the sigma-1 receptor, because MS-377 is a selective sigma-1 receptor ligand without any affinity for NMDA receptor ion-channel complex.

sigma-1 receptor Binding (ligand) of associated with nmda receptor

15) Confidence 0.31 Published 2002 Journal Life Sci. Section Abstract Doc Link 11991251 Disease Relevance 0.05 Pain Relevance 0.22

These effects of MS-377 may depend on its affinity for the sigma-1 receptor, because MS-377 is a selective sigma-1 receptor ligand without any affinity for NMDA receptor ion-channel complex.

sigma-1 receptor Binding (affinity) of associated with nmda receptor

16) Confidence 0.31 Published 2002 Journal Life Sci. Section Abstract Doc Link 11991251 Disease Relevance 0.06 Pain Relevance 0.22

These anti-psychotic activities of MS-377 are attributable to association with sigma-1 receptor.

sigma-1 receptor Binding (association) of associated with psychosis

17) Confidence 0.31 Published 2002 Journal Life Sci. Section Abstract Doc Link 11991251 Disease Relevance 0.10 Pain Relevance 0.04

A sigma-opioid receptor ligand, N-allylnormetazocine (SKF 10047), binds specifically and reversibly to rat liver membranes.

sigma-opioid receptor Binding (binds) of in liver associated with opioid receptor

18) Confidence 0.31 Published 1985 Journal Bioorg. Khim. Section Abstract Doc Link 3000388 Disease Relevance 0 Pain Relevance 0.48

These data suggest that sigma-related (+)-benzomorphans and non-benzomorphans interact either with distinct, allosterically coupled sites on the same sigma receptor macromolecule or with different populations of sigma receptor types.

sigma receptor Binding (interact) of

19) Confidence 0.31 Published 1989 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2542066 Disease Relevance 0 Pain Relevance 0.23

These data suggest that sigma-related (+)-benzomorphans and non-benzomorphans interact either with distinct, allosterically coupled sites on the same sigma receptor macromolecule or with different populations of sigma receptor types.

sigma receptor Binding (interact) of

20) Confidence 0.31 Published 1989 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2542066 Disease Relevance 0 Pain Relevance 0.23

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