Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
37 Results for "
peripherally acting
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "peripherally acting" in MCE Product Catalog:
8
8 Publications Verification
Target:
Forschungsgebiete:
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
4
4 Cited Publications
Art. -Nr.: HY-19721
CAS. Nr.: 1235560-28-7
Target:
Forschungsgebiete:
ABT-639 is a novel, peripherally acting, selective T-type Ca 2+ channel blocker.
2
2 Cited Publications
Art. -Nr.: HY-A0118A
CAS. Nr.: 1354744-91-4
Synonyms: NKTR-118 oxalate; AZ-13337019 oxalate
Target:
Forschungsgebiete:
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol oxalate inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol oxalate is applicable to research related to opioid-induced constipation .
1
Target:
Forschungsgebiete:
1
1 Cited Publications
Art. -Nr.: HY-17436
CAS. Nr.: 167221-71-8
Target:
Forschungsgebiete:
Clevidipine is a selective, short-acting L-type calcium channel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury .
1
1 Cited Publications
Synonyms: (-)-Scopolamine methyl bromide; Hyoscine methyl bromide
Target:
Forschungsgebiete:
Methscopolamine bromide ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice .
Art. -Nr.: HY-P10746
CAS. Nr.: 2770688-48-5
Target:
Forschungsgebiete:
Target:
Forschungsgebiete:
Doxapram is a respiratory stimulant. Doxapram increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity .
Target:
Forschungsgebiete:
Doxapram hydrochloride hydrate is a respiratory stimulant. Doxapram hydrochloride hydrate increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram hydrochloride hydrate inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram hydrochloride hydrate significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram hydrochloride hydrate can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity .
Target:
Synonyms: BIA 3-202
Target:
Forschungsgebiete:
Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease .
Target:
Forschungsgebiete:
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
Art. -Nr.: HY-14280R
CAS. Nr.: 130929-57-6
Target:
Forschungsgebiete:
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
Synonyms: EMD 45609 hydrochloride
Target:
Forschungsgebiete:
Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo .
Art. -Nr.: HY-P10965
CAS. Nr.: 3013543-64-8
Synonyms: ZT002
Target:
Forschungsgebiete:
Art. -Nr.: HY-17609S1
Synonyms: CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride
Category:
Art. -Nr.: HY-A0118
CAS. Nr.: 854601-70-0
Synonyms: NKTR-118; AZ-13337019
Target:
Forschungsgebiete:
Naloxegol (NKTR-118; AZ-13337019) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol is applicable to research related to opioid-induced constipation .
Art. -Nr.: HY-14280A
CAS. Nr.: 1047659-02-8
Target:
Forschungsgebiete:
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
