View source for Chemistry:Opiranserin

{{Short description|Chemical compound}}
{{Drugbox
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| IUPAC_name = 4-Butoxy-''N''-([4-(dimethylamino)oxan-4-yl]methyl)-3,5-dimethoxybenzamide
| image = Opiranserin.svg
| width = 250px

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| routes_of_administration = [[Chemistry:Intravenous therapy|Intravenous]]

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<!-- Identifiers -->
| CAS_number_Ref = 
| CAS_number = 1441000-45-8
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| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = AP031EC2NI
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| PubChem = 71566778
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| synonyms = VVZ-149; VVZ-000149

<!--Chemical data-->
| C=21 | H=34 | N=2 | O=5
| SMILES = O=C(NCC1(N(C)C)CCOCC1)C2=CC(OC)=C(OCCCC)C(OC)=C2
| StdInChI_Ref = 
| StdInChI = 1S/C21H34N2O5/c1-6-7-10-28-19-17(25-4)13-16(14-18(19)26-5)20(24)22-15-21(23(2)3)8-11-27-12-9-21/h13-14H,6-12,15H2,1-5H3,(H,22,24)
| StdInChIKey_Ref = 
| StdInChIKey = JQUVQWMHZSYCRQ-UHFFFAOYSA-N
}}

'''Opiranserin''' ({{abbrlink|INN|International Nonproprietary Name}}; developmental code name '''VVZ-149''') is a [[Chemistry:Binding selectivity|selective]] and combined [[Chemistry:Glycine|glycine]] [[Biology:Glycine transporter 2|GlyT2]] [[Biology:Glycine transporter|transporter]] blocker ({{abbrlink|IC<sub>50</sub>|Half-maximal inhibitory concentration}} = 0.86&nbsp;μM), purine P2X<sub>3</sub> receptor [[Biology:Receptor antagonist|antagonist]] ({{abbr|IC<sub>50</sub>|Half-maximal inhibitory concentration}} = 0.87&nbsp;μM), and [[Chemistry:Serotonin receptor|serotonin]] [[Biology:5-HT2A receptor|5-HT<sub>2A</sub> receptor]] antagonist ({{abbrlink|IC<sub>50</sub>|Half-maximal inhibitory concentration}} = 1.3&nbsp;μM) which is under development by Vivozon for the [[Chemistry:Intravenous therapy|intravenous]] treatment of postoperative pain.<ref name="pmid22269134">{{cite journal | vauthors = Pang MH, Kim Y, Jung KW, Cho S, Lee DH | title = A series of case studies: practical methodology for identifying antinociceptive multi-target drugs | journal = Drug Discov. Today | volume = 17 | issue = 9–10 | pages = 425–34 | year = 2012 | pmid = 22269134 | doi = 10.1016/j.drudis.2012.01.003 }}</ref><ref name="WHO2017">[http://apps.who.int/medicinedocs/documents/s23256en/s23256en.pdf ] </ref><ref name="AdisInsight">{{Cite web|url=https://adisinsight.springer.com/drugs/800038462|title=Opiranserin - Vivozon - AdisInsight|website=adisinsight.springer.com}}</ref><ref name="pmid28213593">{{cite journal | vauthors = Nedeljkovic SS, Correll DJ, Bao X, Zamor N, Zeballos JL, Zhang Y, Young MJ, Ledley J, Sorace J, Eng K, Hamsher CP, Maniam R, Chin JW, Tsui B, Cho S, Lee DH | title = Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery | journal = BMJ Open | volume = 7 | issue = 2 | pages = e011035 | year = 2017 | pmid = 28213593 | pmc = 5318554 | doi = 10.1136/bmjopen-2016-011035 }}</ref> As of April 2017, it is in [[Medicine:Phases of clinical research#Phase II|phase II]] [[Engineering:Clinical trial|clinical trial]]s for this indication.<ref name="AdisInsight" /> The {{abbrlink|INN|International Nonproprietary Name}} of the drug was issued in 2017.<ref name="WHO2017"/>

==References==
{{Reflist}}


{{Glycine receptor modulators}}
{{Serotonin receptor modulators}}

[[Category:5-HT2A antagonists]]
[[Category:Dimethylamino compounds]]
[[Category:Analgesics]]
[[Category:Benzamides]]
[[Category:Experimental drugs]]

{{Sourceattribution|Opiranserin}}