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E-55888: Difference between revisions

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IUPHAR_ligand
 
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{{Short description|Chemical compound}}
{{Drugbox
{{Drugbox
| verifiedrevid = 449673561
| verifiedrevid = 451118186
| 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
| 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 -->
| legal_status =
| legal_status =
| routes_of_administration =
| routes_of_administration =


<!--Pharmacokinetic data-->
<!--Pharmacokinetic data-->
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| metabolism =
| metabolism =
| elimination_half-life =
| elimination_half-life =
| excretion =
| excretion =


<!--Identifiers-->
<!--Identifiers-->
| CAS_number =
| CAS_number = 1034142-33-0
| ATC_prefix =
| ATC_prefix =
| ATC_suffix =
| ATC_suffix =
| PubChem =
| PubChem = 24825775
| ChemSpiderID = 34980845
| UNII = 4KQ7F7PL4L
| ChEMBL = 4205349
| IUPHAR_ligand = 3929


<!--Chemical data-->
<!--Chemical data-->
| C=16 | H=23 | N=3
| C=16 | H=23 | N=3
| molecular_weight = 257.373 g/mol
| smiles = Cn1nc(C)c(c1C)-c(c2)cccc2CCN(C)C
| smiles = Cn1nc(C)c(c1C)-c(c2)cccc2CCN(C)C
| 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
| StdInChIKey = MFUWRMRKXKCSPL-UHFFFAOYSA-N
}}
}}


'''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 |author=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 |year=2009 |month=February |pmid=19118950 |doi=10.1016/j.pain.2008.11.009 |url=}}</ref><ref name="pmid21778664">{{cite journal |author=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 |year=2011 |month=August |pmid=21778664 |doi= |url=}}</ref>
'''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>


==See also==
==See also==
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==References==
==References==
{{reflist}}
{{Reflist}}


{{Serotonin receptor modulators}}
{{Serotonergics}}
{{Phenethylamines}}


[[Category:Serotonin receptor agonists]]
[[Category:5-HT7 agonists]]
[[Category:Pyrazoles]]
[[Category:Pyrazoles]]
[[Category:Phenethylamines]]
[[Category:Phenethylamines]]
[[Category:Dimethylamino compounds]]