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Carvedilol
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Carvedilol, sold under the brand name Coreg among others, is a medication used to treat high blood pressure, congestive heart failure (CHF), and left ventricular dysfunction in people who are otherwise stable. For high blood pressure, it is generally a second-line treatment.<ref name="a1">[https://www.drugs.com/monograph/carvedilol.html "Carvedilol Monograph for Professionals".] Drugs.com. AHFS. Retrieved 24 December 2018.</ref> See also [https://en.wikipedia.org/wiki/Carvedilol Carvedilol]. | Carvedilol, sold under the brand name Coreg among others, is a medication used to treat high blood pressure, congestive heart failure (CHF), and left ventricular dysfunction in people who are otherwise stable. For high blood pressure, it is generally a second-line treatment.<ref name="a1">[https://www.drugs.com/monograph/carvedilol.html "Carvedilol Monograph for Professionals".] Drugs.com. AHFS. Retrieved 24 December 2018.</ref> See also [https://en.wikipedia.org/wiki/Carvedilol Carvedilol]. | ||
| - | Carvedilol is both a non-selective β-adrenergic receptor antagonist (β1, β2) and an α-adrenergic receptor antagonist (α1). The S(–) enantiomer accounts for the beta-blocking activity whereas the S(–) and R(+) enantiomers have alpha-blocking activity.<ref name="a15">[https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020297s029lbl.pdf "Coreg - Food and Drug Administration"] (PDF).</ref> The affinity (Ki) of carvedilol for the β-adrenergic receptors is 0.32 nM for the human β1-adrenergic receptor and 0.13 to 0.40 nM for the β2-adrenergic receptor.<ref name="a22">[https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=biology&ligandId=551 "Carvedilol | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY"]</ref> | + | Carvedilol is both a non-selective [[Beta-2 Adrenergic Receptor|β-adrenergic receptor]] antagonist (β1, β2) and an α-adrenergic receptor antagonist (α1). The S(–) enantiomer accounts for the beta-blocking activity whereas the S(–) and R(+) enantiomers have alpha-blocking activity.<ref name="a15">[https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020297s029lbl.pdf "Coreg - Food and Drug Administration"] (PDF).</ref> The affinity (Ki) of carvedilol for the β-adrenergic receptors is 0.32 nM for the human β1-adrenergic receptor and 0.13 to 0.40 nM for the β2-adrenergic receptor.<ref name="a22">[https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=biology&ligandId=551 "Carvedilol | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY"]</ref> |
<scene name='10/1009520/Overall/1'>Turkey beta1 adrenergic receptor and bound biased agonist carvedilol</scene> ([[4amj]]). | <scene name='10/1009520/Overall/1'>Turkey beta1 adrenergic receptor and bound biased agonist carvedilol</scene> ([[4amj]]). | ||
Revision as of 14:13, 20 November 2023
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References
- ↑ "Carvedilol Monograph for Professionals". Drugs.com. AHFS. Retrieved 24 December 2018.
- ↑ "Coreg - Food and Drug Administration" (PDF).
- ↑ "Carvedilol | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY"
