Alpha-1 adrenergic receptor
alpha-1 (
Effects
[edit]The
Smooth muscle
[edit]In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. Blood vessels with
It also induces contraction of the internal urethral sphincter[7] of the urinary bladder,[8][9] although this effect is minor compared to the relaxing effect of
- Ureter
- Uterus (when pregnant): this is minor compared to the relaxing effects of the
β 2 receptor, agonists of which—notably albuterol/salbutamol—were formerly[citation needed] used to inhibit premature labor. - Urethral sphincter
- Bronchioles (although minor to the relaxing effect of
β 2 receptor on bronchioles) - Iris dilator muscle[4]
- Seminal tract,[4] resulting in ejaculation
Neuronal
[edit]Activation of
Other
[edit]- Both positive and negative inotropic effects on heart muscle[8][14]
- Secretion from salivary gland[8]
- Increase salivary potassium levels
- Glycogenolysis and gluconeogenesis in liver.
- Secretion from sweat glands[8]
- Contraction of the urinary bladder urothelium and lamina propria [15]
- Na+ reabsorption from kidney[8]
- Stimulate proximal tubule NHE3[16]
- Stimulate proximal tubule basolateral Na-K ATPase[16]
- Activate mitogenic responses and regulate growth and proliferation of many cells
- Involved in the detection of mechanical feedback on the hypoglossal motor neurons which allow a long-term facilitation in respiration in response to repeated apneas.[17]
Signaling cascade
[edit]Activity during exercise
[edit]During exercise,
Note that only active muscle
Ligands
[edit]Various heterocyclic antidepressants and antipsychotics are
See also
[edit]References
[edit]- ^ Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular structure, function, and signaling". Circulation Research. 78 (5): 737–49. doi:10.1161/01.RES.78.5.737. PMID 8620593.
- ^ Deluigi M, Morstein L, Schuster M, Klenk C, Merklinger L, Cridge RR, de Zhang LA, Klipp A, Vacca S, Vaid TM, Mittl PR, Egloff P, Eberle SA, Zerbe O, Chalmers DK, Scott DJ, Plückthun A (January 2022). "Crystal structure of the
α 1B-adrenergic receptor reveals molecular determinants of selective ligand recognition". Nature Communications. 13 (1): 382. Bibcode:2022NatCo..13..382D. doi:10.1038/s41467-021-27911-3. PMC 8770593. PMID 35046410. - ^ Piascik MT, Perez DM (August 2001). "Alpha1-adrenergic receptors: new insights and directions". The Journal of Pharmacology and Experimental Therapeutics. 298 (2): 403–10. PMID 11454900.
- ^ a b c Rang HP (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 978-0-443-07145-4. Page 163
- ^ Schmitz JM, Graham RM, Sagalowsky A, Pettinger WA (November 1981). "Renal alpha-1 and alpha-2 adrenergic receptors: biochemical and pharmacological correlations". The Journal of Pharmacology and Experimental Therapeutics. 219 (2): 400–6. PMID 6270306.
- ^ Circulation & Lung Physiology I Archived 2011-07-26 at the Wayback Machine M.A.S.T.E.R. Learning Program, UC Davis School of Medicine
- ^ Le, Tao; Bhushan, Vikas; Sochat, Matthew (2021). First Aid for the USMLE Step 1 2021:A Student to Student Guide. McGraw Hill. p. 240. ISBN 978-1-260-46752-9.
- ^ a b c d e Fitzpatrick D, Purves D, Augustine G (2004). "Table 20:2". Neuroscience (3rd ed.). Sunderland, Mass: Sinauer. ISBN 978-0-87893-725-7.
- ^ Chou EC, Capello SA, Levin RM, Longhurst PA (December 2003). "Excitatory alpha1-adrenergic receptors predominate over inhibitory beta-receptors in rabbit dorsal detrusor". The Journal of Urology. 170 (6 Pt 1): 2503–7. doi:10.1097/01.ju.0000094184.97133.69. PMID 14634460.
- ^ Cheng JT, Kuo DY (August 2003). "Both alpha1-adrenergic and D(1)-dopaminergic neurotransmissions are involved in phenylpropanolamine-mediated feeding suppression in mice". Neuroscience Letters. 347 (2): 136–8. doi:10.1016/S0304-3940(03)00637-2. PMID 12873745. S2CID 24284964.
- ^ Dinh L, Nguyen T, Salgado H, Atzori M (November 2009). "Norepinephrine homogeneously inhibits alpha-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate- (AMPAR-) mediated currents in all layers of the temporal cortex of the rat". Neurochemical Research. 34 (11): 1896–906. doi:10.1007/s11064-009-9966-z. PMID 19357950. S2CID 25255160.
- ^ Stahl, S. M. (2008). Essential Psychopharmacology Online. Retrieved October 20, 2020 from https://stahlonline-cambridge-org.offcampus.lib.washington.edu/essential_4th_chapter.jsf?page=chapter7.htm&name=Chapter%207&title=Antidepressant%20classes#c02598-7-76
- ^ Zimnik NC, Treadway T, Smith RS, Araneda RC (April 2013). "
α (1A)-Adrenergic regulation of inhibition in the olfactory bulb". The Journal of Physiology. 591 (7): 1631–43. doi:10.1113/jphysiol.2012.248591. PMC 3624843. PMID 23266935. - ^ Wang GY, McCloskey DT, Turcato S, Swigart PM, Simpson PC, Baker AJ (October 2006). "Contrasting inotropic responses to alpha1-adrenergic receptor stimulation in left versus right ventricular myocardium". American Journal of Physiology. Heart and Circulatory Physiology. 291 (4): H2013-7. doi:10.1152/ajpheart.00167.2006. PMID 16731650. S2CID 20464280.
- ^ Moro C, Tajouri L, Chess-Williams R (January 2013). "Adrenoceptor function and expression in bladder urothelium and lamina propria". Urology. 81 (1): 211.e1–7. doi:10.1016/j.urology.2012.09.011. PMID 23200975.
- ^ a b Boron WF (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 978-1-4160-2328-9. Page 787
- ^ Tadjalli A, Duffin J, Peever J (December 2010). "Identification of a novel form of noradrenergic-dependent respiratory motor plasticity triggered by vagal feedback". The Journal of Neuroscience. 30 (50): 16886–95. doi:10.1523/JNEUROSCI.3394-10.2010. PMC 6634916. PMID 21159960.
- ^ a b Buckwalter JB, Naik JS, Valic Z, Clifford PS (January 2001). "Exercise attenuates alpha-adrenergic-receptor responsiveness in skeletal muscle vasculature". Journal of Applied Physiology. 90 (1): 172–8. doi:10.1152/jappl.2001.90.1.172. PMID 11133908. S2CID 71048990.
- ^ Fahed S, Grum DF, Papadimos TJ (May 2008). "Labetalol infusion for refractory hypertension causing severe hypotension and bradycardia: an issue of patient safety". Patient Safety in Surgery. 2: 13. doi:10.1186/1754-9493-2-13. PMC 2429901. PMID 18505576.
- ^ Timmermans PB, de Jonge A, Thoolen MJ, Wilffert B, Batink H, van Zwieten PA (April 1984). "Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal of Medicinal Chemistry. 27 (4): 495–503. doi:10.1021/jm00370a011. PMID 6142954.
External links
[edit]- "Adrenoceptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.