Human myometrial adrenergic receptors: Identification of the beta-adrenergic receptor by [3H] dihydroalprenolol binding
The radioactive beta-adrenergic antagonist [3H] dihydroalprenolol (DHA) binds to particulate preparations of human myometrium in a manner compatible with binding to the beta-adrenergic receptor. The binding of DHA is rapid (attaining equilibrium in 12minutes), readily reversible (half time=16minutes...
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| Veröffentlicht in: | American journal of obstetrics and gynecology 1982-02, Vol.142 (4), p.389-393 |
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| container_end_page | 393 |
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| container_issue | 4 |
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| container_title | American journal of obstetrics and gynecology |
| container_volume | 142 |
| creator | Hayashida, David N. Leung, Raymond Goldfien, Alan Roberts, James M. |
| description | The radioactive beta-adrenergic antagonist [3H] dihydroalprenolol (DHA) binds to particulate preparations of human myometrium in a manner compatible with binding to the beta-adrenergic receptor. The binding of DHA is rapid (attaining equilibrium in 12minutes), readily reversible (half time=16minutes), high affinity (KD=0.50 nM), low capacity (Bmax=70 fmoles/mg of protein), and stereoselective ([−]-propranolol is 100 times as potent as [+] -propranolol in inhibiting DHA binding). Adrenergic agonists competed for DHA binding sites in a manner compatible with beta-adrenergic interactions and mirrored β2 pharmacologic potencies: isoproterenol>epinephrine≫norepinephrine. Studies in which zinterol, a β2-adrenergic agonist, competed for DHA binding sites in human myometrial particulate indicated that at least 87% of the beta-adrenergic receptors present are β2-adrenergic receptors. Binding of DHA to human myometrial beta-adrenergic receptors provides a tool which may be used in the examination of gonadal hormonal modification of adrenergic response in human uterus as well as in the analysis of beta-adrenergic agents as potentially useful tocolytic agents. |
| doi_str_mv | 10.1016/S0002-9378(16)32378-X |
| format | Article |
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The binding of DHA is rapid (attaining equilibrium in 12minutes), readily reversible (half time=16minutes), high affinity (KD=0.50 nM), low capacity (Bmax=70 fmoles/mg of protein), and stereoselective ([−]-propranolol is 100 times as potent as [+] -propranolol in inhibiting DHA binding). Adrenergic agonists competed for DHA binding sites in a manner compatible with beta-adrenergic interactions and mirrored β2 pharmacologic potencies: isoproterenol>epinephrine≫norepinephrine. Studies in which zinterol, a β2-adrenergic agonist, competed for DHA binding sites in human myometrial particulate indicated that at least 87% of the beta-adrenergic receptors present are β2-adrenergic receptors. 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The binding of DHA is rapid (attaining equilibrium in 12minutes), readily reversible (half time=16minutes), high affinity (KD=0.50 nM), low capacity (Bmax=70 fmoles/mg of protein), and stereoselective ([−]-propranolol is 100 times as potent as [+] -propranolol in inhibiting DHA binding). Adrenergic agonists competed for DHA binding sites in a manner compatible with beta-adrenergic interactions and mirrored β2 pharmacologic potencies: isoproterenol>epinephrine≫norepinephrine. Studies in which zinterol, a β2-adrenergic agonist, competed for DHA binding sites in human myometrial particulate indicated that at least 87% of the beta-adrenergic receptors present are β2-adrenergic receptors. Binding of DHA to human myometrial beta-adrenergic receptors provides a tool which may be used in the examination of gonadal hormonal modification of adrenergic response in human uterus as well as in the analysis of beta-adrenergic agents as potentially useful tocolytic agents.</description><subject>Adrenergic beta-Agonists - metabolism</subject><subject>Adrenergic beta-Antagonists - metabolism</subject><subject>Alprenolol - analogs & derivatives</subject><subject>Binding, Competitive</subject><subject>Dihydroalprenolol - metabolism</subject><subject>Ethanolamines - metabolism</subject><subject>Female</subject><subject>Humans</subject><subject>Myometrium - metabolism</subject><subject>Postural Balance</subject><subject>Propranolol - metabolism</subject><subject>Receptors, Adrenergic - metabolism</subject><subject>Receptors, Adrenergic, beta - metabolism</subject><subject>Uterus - metabolism</subject><issn>0002-9378</issn><issn>1097-6868</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1982</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LxDAQhoMoun78BCEn0UM1H9s28SIi6gqCBxUEkZAmE420zZpklf33dt3Fk-BpZpj3nZd5ENqn5JgSWp3cE0JYIXktDml1xNnQFE9raESJrItKVGIdjX4lW2g7pffFyCTbRJsVZaQq2Qh9TWad7nE3Dx3k6HWLtY3QQ3z1BkcwMM0hplN8Y6HP3nmjsw89Dg7nN8ANZF38YcDNHD_zyQu2_m1uY9DtdNCENrS48b31_esu2nC6TbC3qjvo8ery4WJS3N5d31yc3xaG1WUuHIyFbbjQtZS8GkunTcNBOCot1aakxjnNdWkbyZlgYzA157yunCCsNrIc8x10sLw7jeFjBimrzicDbat7CLOkai6FZIwMwnIpNDGkFMGpafSdjnNFiVoAVz_A1YKmGqYf4Opp8O2vAmZNB_bXtSI87M-Wexi-_PQQVTIeegPWD7SyssH_k_ANKF-S3Q</recordid><startdate>19820215</startdate><enddate>19820215</enddate><creator>Hayashida, David N.</creator><creator>Leung, Raymond</creator><creator>Goldfien, Alan</creator><creator>Roberts, James M.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19820215</creationdate><title>Human myometrial adrenergic receptors: Identification of the beta-adrenergic receptor by [3H] dihydroalprenolol binding</title><author>Hayashida, David N. ; Leung, Raymond ; Goldfien, Alan ; Roberts, James M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c275t-fe48db38a7993649facb3e8f19d1ac51cffa3a5db932824ec733376f8027c9543</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1982</creationdate><topic>Adrenergic beta-Agonists - metabolism</topic><topic>Adrenergic beta-Antagonists - metabolism</topic><topic>Alprenolol - analogs & derivatives</topic><topic>Binding, Competitive</topic><topic>Dihydroalprenolol - metabolism</topic><topic>Ethanolamines - metabolism</topic><topic>Female</topic><topic>Humans</topic><topic>Myometrium - metabolism</topic><topic>Postural Balance</topic><topic>Propranolol - metabolism</topic><topic>Receptors, Adrenergic - metabolism</topic><topic>Receptors, Adrenergic, beta - metabolism</topic><topic>Uterus - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hayashida, David N.</creatorcontrib><creatorcontrib>Leung, Raymond</creatorcontrib><creatorcontrib>Goldfien, Alan</creatorcontrib><creatorcontrib>Roberts, James M.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>American journal of obstetrics and gynecology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hayashida, David N.</au><au>Leung, Raymond</au><au>Goldfien, Alan</au><au>Roberts, James M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Human myometrial adrenergic receptors: Identification of the beta-adrenergic receptor by [3H] dihydroalprenolol binding</atitle><jtitle>American journal of obstetrics and gynecology</jtitle><addtitle>Am J Obstet Gynecol</addtitle><date>1982-02-15</date><risdate>1982</risdate><volume>142</volume><issue>4</issue><spage>389</spage><epage>393</epage><pages>389-393</pages><issn>0002-9378</issn><eissn>1097-6868</eissn><abstract>The radioactive beta-adrenergic antagonist [3H] dihydroalprenolol (DHA) binds to particulate preparations of human myometrium in a manner compatible with binding to the beta-adrenergic receptor. The binding of DHA is rapid (attaining equilibrium in 12minutes), readily reversible (half time=16minutes), high affinity (KD=0.50 nM), low capacity (Bmax=70 fmoles/mg of protein), and stereoselective ([−]-propranolol is 100 times as potent as [+] -propranolol in inhibiting DHA binding). Adrenergic agonists competed for DHA binding sites in a manner compatible with beta-adrenergic interactions and mirrored β2 pharmacologic potencies: isoproterenol>epinephrine≫norepinephrine. Studies in which zinterol, a β2-adrenergic agonist, competed for DHA binding sites in human myometrial particulate indicated that at least 87% of the beta-adrenergic receptors present are β2-adrenergic receptors. Binding of DHA to human myometrial beta-adrenergic receptors provides a tool which may be used in the examination of gonadal hormonal modification of adrenergic response in human uterus as well as in the analysis of beta-adrenergic agents as potentially useful tocolytic agents.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>6120652</pmid><doi>10.1016/S0002-9378(16)32378-X</doi><tpages>5</tpages></addata></record> |
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| identifier | ISSN: 0002-9378 |
| ispartof | American journal of obstetrics and gynecology, 1982-02, Vol.142 (4), p.389-393 |
| issn | 0002-9378 1097-6868 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Adrenergic beta-Agonists - metabolism Adrenergic beta-Antagonists - metabolism Alprenolol - analogs & derivatives Binding, Competitive Dihydroalprenolol - metabolism Ethanolamines - metabolism Female Humans Myometrium - metabolism Postural Balance Propranolol - metabolism Receptors, Adrenergic - metabolism Receptors, Adrenergic, beta - metabolism Uterus - metabolism |
| title | Human myometrial adrenergic receptors: Identification of the beta-adrenergic receptor by [3H] dihydroalprenolol binding |
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