E-55888: Difference between revisions
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IUPHAR_ligand |
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{{Short description|Chemical compound}} |
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{{Drugbox |
{{Drugbox |
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| verifiedrevid = |
| verifiedrevid = 451118186 |
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| IUPAC_name = N,N-dimethyl-3-(1,3,5-trimethyl-1H-pyrazol-4-yl)phenethylamine |
| IUPAC_name = N,N-dimethyl-3-(1,3,5-trimethyl-1H-pyrazol-4-yl)phenethylamine |
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| image = E-55888_structure.png |
| image = E-55888_structure.png |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = |
| legal_status = |
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| routes_of_administration = |
| routes_of_administration = |
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<!--Pharmacokinetic data--> |
<!--Pharmacokinetic data--> |
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| metabolism = |
| metabolism = |
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| elimination_half-life = |
| elimination_half-life = |
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| excretion = |
| excretion = |
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<!--Identifiers--> |
<!--Identifiers--> |
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| CAS_number = |
| CAS_number = 1034142-33-0 |
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| ATC_prefix = |
| ATC_prefix = |
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| ATC_suffix = |
| ATC_suffix = |
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| PubChem = |
| PubChem = 24825775 |
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| ChemSpiderID = 34980845 |
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| UNII = 4KQ7F7PL4L |
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| ChEMBL = 4205349 |
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| IUPHAR_ligand = 3929 |
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<!--Chemical data--> |
<!--Chemical data--> |
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| C=16 | H=23 | N=3 |
| C=16 | H=23 | N=3 |
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| molecular_weight = 257.373 g/mol |
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| smiles = Cn1nc(C)c(c1C)-c(c2)cccc2CCN(C)C |
| smiles = Cn1nc(C)c(c1C)-c(c2)cccc2CCN(C)C |
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| StdInChI = 1S/C16H23N3/c1-12-16(13(2)19(5)17-12)15-8-6-7-14(11-15)9-10-18(3)4/h6-8,11H,9-10H2,1-5H3 |
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| StdInChIKey = MFUWRMRKXKCSPL-UHFFFAOYSA-N |
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'''E-55888''' is a drug developed by [[Esteve]], which acts as a potent and selective [[full agonist]] at the [[5-HT7 receptor|5HT<sub>7</sub>]] [[serotonin]] [[Receptor (biochemistry)|receptor]], and is used for investigating the role of 5-HT<sub>7</sub> receptors in the perception of [[pain]]. When administered by itself, E-55888 is anti-[[hyperalgesia|hyperalgesic]] but not [[analgesic]], but when administered alongside [[morphine]], E-55888 was found to significantly increase the analgesic effects.<ref name="pmid19118950">{{cite journal | |
'''E-55888''' is a drug developed by [[Esteve]], which acts as a potent and selective [[full agonist]] at the [[5-HT7 receptor|5HT<sub>7</sub>]] [[serotonin]] [[Receptor (biochemistry)|receptor]], and is used for investigating the role of 5-HT<sub>7</sub> receptors in the perception of [[pain]]. When administered by itself, E-55888 is anti-[[hyperalgesia|hyperalgesic]] but not [[analgesic]], but when administered alongside [[morphine]], E-55888 was found to significantly increase the analgesic effects.<ref name="pmid19118950">{{cite journal |vauthors=Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, Hamon M, Baeyens JM, Buschmann H, Zamanillo D, Vela JM |title=5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice |journal=Pain |volume=141 |issue=3 |pages=239–47 |date=February 2009 |pmid=19118950 |doi=10.1016/j.pain.2008.11.009 |s2cid=27144262 }}</ref><ref name="pmid21778664">{{cite journal |vauthors=Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L |title=Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT(7) Receptors |journal=Journal of Pharmacological Sciences |volume=116 |issue=4 |pages=388–91 |date=August 2011 |pmid=21778664 |doi= 10.1254/jphs.11039sc|doi-access=free }}</ref> |
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==See also== |
==See also== |
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==References== |
==References== |
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{{ |
{{Reflist}} |
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{{Serotonin receptor modulators}} |
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{{Serotonergics}} |
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{{Phenethylamines}} |
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[[Category: |
[[Category:5-HT7 agonists]] |
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[[Category:Pyrazoles]] |
[[Category:Pyrazoles]] |
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[[Category:Phenethylamines]] |
[[Category:Phenethylamines]] |
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[[Category:Dimethylamino compounds]] |