Bertha K. Madras, Alan Davis, Betty Chan, Philip Seeman
{"title":"溶解多巴胺/抗精神病药物受体(d2型)","authors":"Bertha K. Madras, Alan Davis, Betty Chan, Philip Seeman","doi":"10.1016/0364-7722(81)90043-6","DOIUrl":null,"url":null,"abstract":"<div><p></p><ul><li><span>1.</span><span><p>1. Dopamine (D<sub>2</sub>-type) receptors were solubilized from striatum of three species (human, canine, calf) using digitonin.</p></span></li><li><span>2.</span><span><p>2. The receptors were labeled with <sup>3</sup>H-spiperone and assayed by Sephadex G-50 columns or polyethylene glycol precipitation.</p></span></li><li><span>3.</span><span><p>3. The soluble receptors from canine and human tissue had similar K<sub>d</sub>'s and rank order of drug affinities to the membrane-bound sites.</p></span></li><li><span>4.</span><span><p>4. Soluble calf receptors showed reduced affinity for spiperone and chlorpromazine (12-fold). Non-specific binding also increased.</p></span></li><li><span>5.</span><span><p>5. Solubilized canine binding was insensitive to ascorbate, Mn<sup>++</sup>, and ethylenediamine tetracetic acid (EDTA) in contrast to the membrane binding sites.</p></span></li><li><span>6.</span><span><p>6. Solubilized canine striatum serves as an excellent source of D<sub>2</sub> receptors because these receptors are stable in solution and are a prototype of human D<sub>2</sub> receptors.</p></span></li></ul></div>","PeriodicalId":20801,"journal":{"name":"Progress in neuro-psychopharmacology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1981-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0364-7722(81)90043-6","citationCount":"7","resultStr":"{\"title\":\"Solubilized dopamine/neuroleptic receptors (D2-type)\",\"authors\":\"Bertha K. Madras, Alan Davis, Betty Chan, Philip Seeman\",\"doi\":\"10.1016/0364-7722(81)90043-6\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p></p><ul><li><span>1.</span><span><p>1. Dopamine (D<sub>2</sub>-type) receptors were solubilized from striatum of three species (human, canine, calf) using digitonin.</p></span></li><li><span>2.</span><span><p>2. The receptors were labeled with <sup>3</sup>H-spiperone and assayed by Sephadex G-50 columns or polyethylene glycol precipitation.</p></span></li><li><span>3.</span><span><p>3. The soluble receptors from canine and human tissue had similar K<sub>d</sub>'s and rank order of drug affinities to the membrane-bound sites.</p></span></li><li><span>4.</span><span><p>4. Soluble calf receptors showed reduced affinity for spiperone and chlorpromazine (12-fold). Non-specific binding also increased.</p></span></li><li><span>5.</span><span><p>5. Solubilized canine binding was insensitive to ascorbate, Mn<sup>++</sup>, and ethylenediamine tetracetic acid (EDTA) in contrast to the membrane binding sites.</p></span></li><li><span>6.</span><span><p>6. Solubilized canine striatum serves as an excellent source of D<sub>2</sub> receptors because these receptors are stable in solution and are a prototype of human D<sub>2</sub> receptors.</p></span></li></ul></div>\",\"PeriodicalId\":20801,\"journal\":{\"name\":\"Progress in neuro-psychopharmacology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1981-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0364-7722(81)90043-6\",\"citationCount\":\"7\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Progress in neuro-psychopharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/0364772281900436\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in neuro-psychopharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0364772281900436","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
1. Dopamine (D2-type) receptors were solubilized from striatum of three species (human, canine, calf) using digitonin.
2.
2. The receptors were labeled with 3H-spiperone and assayed by Sephadex G-50 columns or polyethylene glycol precipitation.
3.
3. The soluble receptors from canine and human tissue had similar Kd's and rank order of drug affinities to the membrane-bound sites.
4.
4. Soluble calf receptors showed reduced affinity for spiperone and chlorpromazine (12-fold). Non-specific binding also increased.
5.
5. Solubilized canine binding was insensitive to ascorbate, Mn++, and ethylenediamine tetracetic acid (EDTA) in contrast to the membrane binding sites.
6.
6. Solubilized canine striatum serves as an excellent source of D2 receptors because these receptors are stable in solution and are a prototype of human D2 receptors.
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