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HP-505 - 版本历史
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<p><b>新页面</b></p><div>{{Drugbox<br />
| IUPAC_name = 3-phenyl-3H-spiro[isobenzofuran-1,4'-piperidine]<br />
| image = HP_505.svg<br />
| width = 130<br />
<br />
<!--Clinical data--><br />
| tradename = <br />
| legal_status = <br />
| routes_of_administration =<br />
<br />
<!--Pharmacokinetic data--><br />
| metabolism = <br />
| elimination_half-life = <br />
| excretion =<br />
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<!--Identifiers--><br />
| IUPHAR_ligand = <br />
| CAS_number = 59142-94-8<br />
| CAS_number_Ref = {{cascite|correct|CAS}}<br />
| ChEMBL = 436281<br />
| UNII_Ref = {{fdacite|correct|FDA}}<br />
| UNII = <br />
| PubChem = 191510<br />
| ChemSpiderID = 166303<br />
<br />
<!--Chemical data--><br />
| C=18 | H=19 | N=1 | O=1 <br />
| smiles = C1(C2OC3(CCNCC3)C4=C2C=CC=C4)=CC=CC=C1<br />
| StdInChI = 1S/C18H19NO/c1-2-6-14(7-3-1)17-15-8-4-5-9-16(15)18(20-17)10-12-19-13-11-18/h1-9,17,19H,10-13H2<br />
| StdInChIKey = ZFJQWOMHWFYLPD-UHFFFAOYSA-N<br />
}}<br />
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'''HP-505'''是一种[[有机化合物]]，化学式为[[C18H19NO|C<sub>18</sub>H<sub>19</sub>NO]]。它是由{{le|赫美罗制药公司|Hoechst-Marion-Roussel}}研发的[[5-羟色胺、去甲肾上腺素和多巴胺再摄取抑制剂|三重再摄取抑制剂]]。<ref name="BETA">{{cite journal |last1=Meyerson |first1=Laurence R |last2=Ong |first2=Helen H |last3=Martin |first3=Lawrence L |last4=Ellis |first4=Daniel B |title=Effect of antidepressant agents on β-adrenergic receptor and neurotransmitter regulatory systems |url=https://archive.org/details/sim_pharmacology-biochemistry-and-behavior_1980-06_12_6/page/943 |journal=Pharmacology Biochemistry and Behavior |date=June 1980 |volume=12 |issue=6 |pages=943–948 |doi=10.1016/0091-3057(80)90457-8|pmid=6105676 |s2cid=45400599 }}</ref>HP-505在小鼠试验中发现是{{le|丁苯那嗪|tetrabenazine}}诱导的{{le|上睑下垂|ptosis}}的有效抑制剂，这表明它可能具有抗抑郁活性。<ref>{{cite journal |last1=Klioze |first1=SS |last2=Bauer |first2=VJ |last3=Geyer HM |first3=3rd |title=Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen. |journal=Journal of Medicinal Chemistry |date=April 1977 |volume=20 |issue=4 |pages=610–2 |doi=10.1021/jm00214a039 |pmid=850252}}</ref> <br />
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==药理学==<br />
{| class="wikitable"<br />
|+ HP-505 IC<sub>50</sub> (µM)<ref name="BETA" /><br />
|-<br />
! [[血清素轉運體|5-HT]] !! [[去甲腎上腺素轉運體|NE]] !! [[多巴胺轉運體|DA]] !! NE:5-HT !! DA:5-HT<br />
|- <br />
| 0.19 ± 0.04 || 0.34 ± 0.1 || 0.66 ± 0.15 || 1.8 || 3.5 <br />
|}<br />
<br />
==化学性质==<br />
HP-505在[[碳酸氢钠]]存在下，可以和2-氯-4-硝基吡啶-1-氧化物反应，得到''N''-(1-氧化-4-硝基吡啶-2-基)-HP-505。<ref>Allerton, Charlotte Moira Norfor; Owen, Dafydd Rhys; Ryckmans, Thomas; Stammen, Blanda Luzia Christa. Spiropiperidine derivatives, processes for preparing them, pharmaceutical compositions containing them, and their use as delta opioid receptor agonists. 2007 WO 2007057775 A1.</ref><br />
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== 参考文献 ==<br />
{{Reflist}}<br />
<br />
[[Category:血清素-去甲肾上腺素-多巴胺重摄取抑制剂]]<br />
[[Category:神經系統藥物小作品]]<br />
[[Category:未分配ATC的藥物]]<br />
[[Category:哌啶]]<br />
[[Category:异苯并呋喃]]<br />
[[Category:螺环化合物]]</div>
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