INT33463

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Context Info
Confidence 0.31
First Reported 1986
Last Reported 2003
Negated 0
Speculated 1
Reported most in Abstract
Documents 3
Total Number 6
Disease Relevance 0.16
Pain Relevance 3.27

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cell differentiation (DMRT1) nucleus (DMRT1)
Anatomy Link Frequency
brain 1
DMRT1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Enkephalin 6 99.82 Very High Very High Very High
Analgesic 6 99.52 Very High Very High Very High
antagonist 4 99.30 Very High Very High Very High
MU agonist 3 99.04 Very High Very High Very High
Opioid 13 98.50 Very High Very High Very High
mu opioid receptor 9 98.28 Very High Very High Very High
Kappa opioid receptor 8 94.60 High High
intrathecal 4 94.60 High High
opioid receptor 5 87.68 High High
Morphine 4 86.68 High High
Disease Link Frequency Relevance Heat
Mental Disorders 1 81.88 Quite High
Schizophrenia 1 80.80 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Dissociation of [3H][Dmt1]DALDA was also rapid (K(-1) = 0.032 min(-1)) and indicated binding to a single site. [3H][Dmt1]DALDA binds with very high affinity to human mu opioid receptor (hMOR) (Kd = 0.199 nM), and Kd and Bmax were reduced by sodium but not Gpp(NH)p [guanosine 5'-(beta,gamma-imido)triphosphate].
Dmt1 Binding (binding) of associated with mu opioid receptor
1) Confidence 0.31 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 14534366 Disease Relevance 0 Pain Relevance 0.50
The Ki values for a number of opioid ligands were generally higher when determined by competitive displacement binding against [3H][Dmt1]DALDA compared with [3H]DAMGO, with the exception of Dmt1-substituted peptide analogs.
Dmt1 Spec (determined) Binding (binding) of associated with opioid
2) Confidence 0.31 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 14534366 Disease Relevance 0 Pain Relevance 0.56
[Dmt1]DALDA (H-Dmt-d-Arg-Phe-Lys-NH2; Dmt = 2',6'-dimethyltyrosine) binds with high affinity and selectivity to the mu opioid receptor and is a surprisingly potent and long-acting analgesic, especially after intrathecal administration.
Dmt1 Binding (binds) of associated with analgesic, mu opioid receptor and intrathecal
3) Confidence 0.31 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 14534366 Disease Relevance 0 Pain Relevance 0.30
Kinetic studies revealed rapid association of [3H][Dmt1]DALDA when incubated with mouse brain membranes (K+1 = 0.155 nM(-1) min(-1)).
Dmt1 Binding (association) of in brain
4) Confidence 0.31 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 14534366 Disease Relevance 0 Pain Relevance 0.41
Characterization of the binding of [3H][Dmt1]H-Dmt-D-Arg-Phe-Lys-NH2, a highly potent opioid peptide.
Dmt1 Binding (binding) of associated with analgesic and opioid
5) Confidence 0.30 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 12663687 Disease Relevance 0 Pain Relevance 0.69
Several mu opioid agonists, antagonists, and synthetic enkephalin analogs interacted with DMT and LSD.
DMT Binding (interacted) of associated with mu agonist, antagonist and enkephalin
6) Confidence 0.25 Published 1986 Journal Pharmacol. Biochem. Behav. Section Abstract Doc Link 3006089 Disease Relevance 0.16 Pain Relevance 0.81

General Comments

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