iodocyanopindolol
Sign in to saveAlso known as 3-iodocyanopindolol, 4-[3-(tert-Butylamino)-2-hydroxypropoxy]-3-iodo-1H-indole-2-carbonitrile
Iodocyanopindolol (), also known as ICYP, is a synthetic compound derived from pindolol, primarily used as a radioligand in pharmacological research. It functions as a non-selective β-adrenoceptor antagonist and a serotonin 5-HT1A and 5-HT1B receptor antagonist. Its 125I-radiolabelled derivative, [125I]-iodocyanopindolol ([125I]-ICYP), is widely employed to map the distribution and density of β-adrenoceptors and serotonin receptors in tissues, particularly in the brain, heart, and other organs. Iodocyanopindolol is not used clinically but remains a critical tool in studying receptor pharmacolo
Research
1,058 papers- The iodocyanopindolol and SM-11044 binding protein belongs to the TM9SF multispanning membrane protein superfamily.Gene · 2001
- Application of [125I]iodocyanopindolol to measure 5-hydroxytryptamine1B receptors in the brain of the rat.The Journal of pharmacology and experimental therapeutics · 1988
- Beta-adrenoceptors in the tree shrew brain. I. Distribution and characterization of [125I]iodocyanopindolol binding sites.Cellular and molecular neurobiology · 1997
- Molecular pharmacology of beta-adrenoceptors.Journal of cardiovascular pharmacology · 1986
- Drug-induced regulation of [125I]iodocyanopindolol-labeled 5-hydroxytryptamine1B receptor binding sites in the central nervous system.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 1994
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Wikidata facts
- Subclass of
- alcohols
- Mass
- 413.06002488
- Has use
- medication
Show 4 more facts
- Commons category
- 3-Iodocyanopindolol
- subject has role
- beta blocker
- canonical SMILES
- CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12
- chemical formula
- C₁₆H₂₀IN₃O₂
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Encyclopedic overview
7 sectionsContents
- Pharmacological properties
- Research applications
- Mechanism and binding characteristics
- History
- See also
- References
- External links
Iodocyanopindolol (), also known as ICYP, is a synthetic compound derived from pindolol, primarily used as a radioligand in pharmacological research. It functions as a non-selective β-adrenoceptor antagonist and a serotonin 5-HT1A and 5-HT1B receptor antagonist. Its 125I-radiolabelled derivative, [125I]-iodocyanopindolol ([125I]-ICYP), is widely employed to map the distribution and density of β-adrenoceptors and serotonin receptors in tissues, particularly in the brain, heart, and other organs. Iodocyanopindolol is not used clinically but remains a critical tool in studying receptor pharmacology and signal transduction. Its application extends to the central nervous system, where it labels 5-HT1B receptors in regions like the brainstem, hippocampus, and cortex, aiding research on serotonin autoreceptor regulation.
== Pharmacological properties == Iodocyanopindolol acts as a high-affinity antagonist at β1 and β2 adrenoceptors, with a lesser affinity for β3 adrenoceptors. It also antagonizes 5-HT1A and 5-HT1B serotonin receptors, making it a versatile radioligand for studying both adrenergic and serotonergic systems. The [125I]-ICYP form binds with high specificity, allowing quantitative analysis of receptor density (Bmax) and affinity (Kd) through techniques like autoradiography and radioligand binding assays.
Excerpted from Wikipedia’s “iodocyanopindolol” article, available under the CC BY-SA 4.0 licence.