Receptor adrenérgico alfa 1A O receptor adrenérgico alfa 1A (adrenorreceptor α1A). também conhecido como ADRA1A, é um receptor adrenérgico alfa 1 e também denota o gene humano que o codifica.[1] É encontrado no trato urinário e na próstata.[2]
A tansulosina é um fármaco antagonista seletivo desse receptor, sendo utilizado para o tratamento de hiperplasia benigna de próstata. Diminui a obstrução do fluxo urinário (melhorando os sintomas obstrutivos) através do relaxamento da musculatura lisa na próstata e na uretra.[2]
Referências
- ↑ «α1A-adrenoceptor» (em inglês). IUPHAR DATABASE. Consultado em 1 de julho de 2010
- ↑ a b WHALEN, KAREN et. al (2016). Farmacologia Ilustrada. Porto Alegre: Artmed. 80 páginas
Leitura de apoio
- Mátyus P, Horváth K (1998). «Alpha-adrenergic approach in the medical management of benign prostatic hyperplasia.». Med Res Rev. 17 (6): 523–35. PMID 9359081. doi:10.1002/(SICI)1098-1128(199711)17:6<523::AID-MED2>3.0.CO;2-3
- Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT (1993). «A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C).». Hum. Mol. Genet. 1 (5): 349. PMID 1363873. doi:10.1093/hmg/1.5.349-a
- Schwinn DA, Lomasney JW, Lorenz W; et al. (1990). «Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype.». J. Biol. Chem. 265 (14): 8183–9. PMID 1970822
- Hirasawa A, Shibata K, Horie K; et al. (1995). «Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants.». FEBS Lett. 363 (3): 256–60. PMID 7737411. doi:10.1016/0014-5793(95)00330-C
- Diehl NL, Shreeve SM (1995). «Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction.». Eur. J. Pharmacol. 268 (3): 393–8. PMID 7805763
- Schwinn DA, Johnston GI, Page SO; et al. (1995). «Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.». J. Pharmacol. Exp. Ther. 272 (1): 134–42. PMID 7815325
- Weinberg DH, Trivedi P, Tan CP; et al. (1994). «Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c.». Biochem. Biophys. Res. Commun. 201 (3): 1296–304. PMID 8024574. doi:10.1006/bbrc.1994.1845
- Forray C, Bard JA, Wetzel JM; et al. (1994). «The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype.». Mol. Pharmacol. 45 (4): 703–8. PMID 8183249
- Hirasawa A, Horie K, Tanaka T; et al. (1993). «Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor.». Biochem. Biophys. Res. Commun. 195 (2): 902–9. PMID 8396931. doi:10.1006/bbrc.1993.2130
- Tseng-Crank J, Kost T, Goetz A; et al. (1996). «The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types.». Br. J. Pharmacol. 115 (8): 1475–85. PMID 8564208
- Shibata K, Hirasawa A, Moriyama N; et al. (1997). «Alpha 1a-adrenoceptor polymorphism: pharmacological characterization and association with benign prostatic hypertrophy.». Br. J. Pharmacol. 118 (6): 1403–8. PMID 8832064
- Chang DJ, Chang TK, Yamanishi SS; et al. (1998). «Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.». FEBS Lett. 422 (2): 279–83. PMID 9490024. doi:10.1016/S0014-5793(98)00024-6
- Daniels DV, Gever JR, Jasper JR; et al. (1999). «Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.». Eur. J. Pharmacol. 370 (3): 337–43. PMID 10334511. doi:10.1016/S0014-2999(99)00154-5
- Cogé F, Guenin SP, Renouard-Try A; et al. (1999). «Truncated isoforms inhibit [3H]prazosin binding and cellular trafficking of native human alpha1A-adrenoceptors.». Biochem. J. 343 Pt 1: 231–9. PMID 10493934. doi:10.1042/0264-6021:3430231
- Rudner XL, Berkowitz DE, Booth JV; et al. (1999). «Subtype specific regulation of human vascular alpha(1)-adrenergic receptors by vessel bed and age.». Circulation. 100 (23): 2336–43. PMID 10587338
- Ballou LM, Cross ME, Huang S; et al. (2000). «Differential regulation of the phosphatidylinositol 3-kinase/Akt and p70 S6 kinase pathways by the alpha(1A)-adrenergic receptor in rat-1 fibroblasts.». J. Biol. Chem. 275 (7): 4803–9. PMID 10671514. doi:10.1074/jbc.275.7.4803
- Keffel S, Alexandrov A, Goepel M, Michel MC (2000). «alpha(1)-adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells.». Biochem. Biophys. Res. Commun. 272 (3): 906–11. PMID 10860850. doi:10.1006/bbrc.2000.2850
- Richman JG, Brady AE, Wang Q; et al. (2001). «Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin.». J. Biol. Chem. 276 (18): 15003–8. PMID 11154706. doi:10.1074/jbc.M011679200
- Shibata K, Katsuma S, Koshimizu T; et al. (2003). «alpha 1-Adrenergic receptor subtypes differentially control the cell cycle of transfected CHO cells through a cAMP-dependent mechanism involving p27Kip1.». J. Biol. Chem. 278 (1): 672–8. PMID 12409310. doi:10.1074/jbc.M201375200
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Classe A: Tipo rodopsina | Neurotransmissor | Adrenérgico | |
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Purinérgico | Adenosina ( A1, A2A, A2B, A3) · P2Y ( 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14) |
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Serotonina | (todos, exceto 5-HT3) 5-HT1 ( A, B, D, E, F) · 5-HT2 ( A, B, C) · 5-HT ( 4, 5A, 6, 7) |
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Outros | Acetilcolina ( M1, M2, M3, M4, M5) · Dopamina ( D1, D2, D3, D4, D5) · Histamina ( H1, H2, H3, H4) · Melatonina ( 1A, 1B, 1C) · TAAR ( 1, 2, 3, 5, 6, 8, 9) |
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Metabólitos e moléculas de sinalização | Eicosanoide | CysLT ( 1, 2) · LTB4 ( 1, 2) · FPRL ( 1, 2, 3) · OXE · Prostaglandina ( DP ( 1, 2), EP ( 1, 2, 3, 4), FP) · Prostaciclina · Tromboxano |
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Outros | Ácido biliar · Ácido graxo livre ( 1, 2, 3, 4) · Ácido hidroxicarboxilíco ( 1, 2, 3) · Ácido lisofosfatídico ( 1, 2, 3, 4, 5, 6) · Canabinoide ( CB1, CB2, GPR ( 18, 55, 119)) · EBI2 · Estrogênio · Lisofosfolipídeo ( 1, 2, 3) · Oxoglutarato · PAF · Esfingosina-1-fosfato ( 1, 2, 3, 4, 5) · Succinato |
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Peptídeos | Neuropeptídeo | |
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Outros | Anafilatoxina ( C3a, C5a) · Angiotensina ( 1, 2) · Apelina · Bombesina ( BRS3, GRPR, NMBR) · Bradicinina ( B1, B2) · Quimiocina · Colecistoquinina ( A, B) · Endotelina ( A, B) · Formil peptídeo ( 1, 2, 3) · FSH · Galanina ( 1, 2, 3) · Receptor GHB · Hormônio liberador de gonadotrofina ( 1, 2) · Ghrelina · Kisspeptina · Hormônio luteinizante/coriogonadotropina · MAS ( 1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortina ( 1, 2, 3, 4, 5) · MCHR ( 1, 2) · Motilina · Opioide ( δ, κ, μ, Nociceptina & ζ, mas não σ) · Orexina ( 1, 2) · Oxitocina · Procineticina ( 1, 2) · Peptídeo liberador de prolactina · Relaxina ( 1, 2, 3, 4) · Somatostatina ( 1, 2, 3, 4, 5) · Taquicinina ( 1, 2, 3) · Tirotrofina · Hormônio liberador de tirotropina · Urotensina-II · Vasopressina ( 1A, 1B, 2) |
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Miscelânea | Órfão | GPR ( 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183) |
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Outros | Olfatório · Opsina ( 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Ativado por protease ( 1, 2, 3, 4) · SREB ( 1, 2, 3) |
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Classe B: Tipo secretina | Órfãos | GPR ( 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157) |
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Outros | ADCYAP1R1 · Caderina ( 1, 2, 3) · Calcitonina · CALCRL · CD97 · EMR ( 1, 2, 3) · Glucagon ( GR, GIPR, GLP1R, GLP2R) · Hormônio liberador de corticotrofina ( 1, 2) · Hormônio liberador do hormônio do crescimento · Hormônio paratireoide ( 1, 2) · GPR · Inibidor de angiogênese específico do cérebro ( 1, 2, 3) · Latrofilina ( 1, 2, 3, ELTD1 · Peptídeo intestinal vasoativo ( 1, 2) · Proteínas tipo-Matusalém · Secretina |
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Classe C: Metabotrópico glutamato / feromona | Sabor | TAS1R ( 1, 2, 3) · TAS2R ( 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50) |
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Outros | Sensor de cálcio · GABA B ( 1, 2) · Glutamato ( Metabotrópico de glutamato ( 1, 2, 3, 4, 5, 6, 7, 8)) · GPRC6A · GPR ( 156, 158, 179) · RAIG ( 1, 2, 3, 4) |
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Class F: Frizzled / Smoothened | |
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