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Receptor adrenérgico alfa 1 مستقبلات ألفا-1 الأدرينالية Α1-Adrenozeptor Receptor adrenérgico alfa 1 Alpha-1 adrenergic receptor
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O receptor adrenérgico α1 é um dos tipos de receptores adrenérgicos, que constituem receptores metabotrópicos (proteínas associadas à proteína G, com sete domínios transmembrana). Ele está presente na membrana plasmática de certas células e sua função principal é a de promover a ativação da enzima fosfolipase C, que atua clivando um lipídeo de membrana, o fosfatidilinositol 4,5 bifosfato (PIP 2), em seus subprodutos trifosfato de inositol (IP3) e diacilglicerol (DAG). O trifosfato de inositol está relacionado a liberação do íon cálcio do retículo sarcoplasmático das células musculares lisas, enquanto o diacilglicerol propicia a ativação da proteíno quinase C (PKC), uma importante enzima reguladora. Entre suas principais ações estão a vasoconstrição, broncoconstrição, secreção salivar, cont مستقبلات ألفا-1 (α1) الأدرينالية هي مستقبلات مقترنة بالبروتين ج وهي مرتبطة بالبروتين ج كيو. وهو يتألف من ثلاثة أنواع فرعية متماثلة، بما في ذلك مستقبلات α1A- ،α1B- ،α1D الأدرينالية. الكاتيكولامينات مثل النورإبينفرين (النورأدرينالين) أبينفرين (الأدرينالين) يرسلون الإشارات خلال مستقبلات α1 الأدرينالية في الجهاز العصبي المركزي والجهاز العصبي المحيطي. لا يوجد مستقبلات α1C. في وقت ما كان هناك نوع فرعي باسم α1C، ولكن وجد أنه مطابق للنوع α1A الذي تم اكتشافه سابقًا. لتجنب الارتباك، استمرت التسمية باستخدام الحرف D. Die α1-Adrenozeptoren sind Gq/11-Protein-gekoppelte Rezeptoren, die durch die Signalstoffe Adrenalin und Noradrenalin aktiviert werden. Sie werden auf Grund ihrer pharmakologischen Eigenschaften in vier Subtypen unterteilt: α1A, α1B, α1D und „α1L“. Während die ersten drei Subtypen auch auf genomischer Ebene eigenständige Rezeptoren verkörpern, scheint der „α1L“-Adrenozeptor lediglich eine Konformationsvariante des α1A-Subtyps darzustellen. alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1-adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α1A-, α1B-, and α1D-adrenergic receptor subtypes. There is no α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptors in the central and peripheral nervous systems. The crystal structure of the α1B-adrenergic receptor subtype has been determined in complex with the inverse agonist (+)-cyclazosin. El receptor adrenérgico α1 es uno de los tipos de receptores adrenérgicos presentes en la membrana plasmática de ciertas células, cuya función principal es la vasoconstricción. Existen varios subtipos de receptores α, los cuales tienen funciones en común con el receptor α1, pero este tiene sus funciones que le son específicas.
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Die α1-Adrenozeptoren sind Gq/11-Protein-gekoppelte Rezeptoren, die durch die Signalstoffe Adrenalin und Noradrenalin aktiviert werden. Sie werden auf Grund ihrer pharmakologischen Eigenschaften in vier Subtypen unterteilt: α1A, α1B, α1D und „α1L“. Während die ersten drei Subtypen auch auf genomischer Ebene eigenständige Rezeptoren verkörpern, scheint der „α1L“-Adrenozeptor lediglich eine Konformationsvariante des α1A-Subtyps darzustellen. مستقبلات ألفا-1 (α1) الأدرينالية هي مستقبلات مقترنة بالبروتين ج وهي مرتبطة بالبروتين ج كيو. وهو يتألف من ثلاثة أنواع فرعية متماثلة، بما في ذلك مستقبلات α1A- ،α1B- ،α1D الأدرينالية. الكاتيكولامينات مثل النورإبينفرين (النورأدرينالين) أبينفرين (الأدرينالين) يرسلون الإشارات خلال مستقبلات α1 الأدرينالية في الجهاز العصبي المركزي والجهاز العصبي المحيطي. لا يوجد مستقبلات α1C. في وقت ما كان هناك نوع فرعي باسم α1C، ولكن وجد أنه مطابق للنوع α1A الذي تم اكتشافه سابقًا. لتجنب الارتباك، استمرت التسمية باستخدام الحرف D. El receptor adrenérgico α1 es uno de los tipos de receptores adrenérgicos presentes en la membrana plasmática de ciertas células, cuya función principal es la vasoconstricción. Existen varios subtipos de receptores α, los cuales tienen funciones en común con el receptor α1, pero este tiene sus funciones que le son específicas. O receptor adrenérgico α1 é um dos tipos de receptores adrenérgicos, que constituem receptores metabotrópicos (proteínas associadas à proteína G, com sete domínios transmembrana). Ele está presente na membrana plasmática de certas células e sua função principal é a de promover a ativação da enzima fosfolipase C, que atua clivando um lipídeo de membrana, o fosfatidilinositol 4,5 bifosfato (PIP 2), em seus subprodutos trifosfato de inositol (IP3) e diacilglicerol (DAG). O trifosfato de inositol está relacionado a liberação do íon cálcio do retículo sarcoplasmático das células musculares lisas, enquanto o diacilglicerol propicia a ativação da proteíno quinase C (PKC), uma importante enzima reguladora. Entre suas principais ações estão a vasoconstrição, broncoconstrição, secreção salivar, contração dos esfíncteres gastrointestinais, contração da íris (midríase), glicogenólise hepática e relaxamento da musculatura lisa do trato gastrointestinal. Os fármacos atuantes nesse receptor podem possuir ação específica (fármacos seletivos) ou também atuarem em outros receptores adrenérgicos (não-seletivos). Os agonistas dos receptoresα1 são medicamentos simpatomiméticos, tendo sua ação principalmente de vasoconstrição na pele e nas vísceras. Exemplos de agonistas são os descongestionantes nasais (oximetazolina, por exemplo), que atuam combatendo a característica passagem do plasma para a região sub-mucosa por meio da vasoconstrição. Outros exemplos são a fenilefrina e metoxamina. Os antagonistas estão relacionados à vasodilatação, queda de pressão arterial e relaxamento do músculo detrusor da bexiga. São exemplos destes a prazosina e doxazozina. alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1-adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α1A-, α1B-, and α1D-adrenergic receptor subtypes. There is no α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptors in the central and peripheral nervous systems. The crystal structure of the α1B-adrenergic receptor subtype has been determined in complex with the inverse agonist (+)-cyclazosin.
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