Carcinine
Carcinine (β-Alanylhistamine) is a selective and orally active histamine H3 receptor antagonist with a Ki of 0.2939 μM. Carcinine can reduce histamine content. Carcinine exhibits anti-oxidant activity and neuroprotective effects. Carcinine shows positive inotropic effect and can reduce blood sugar and blood lipid levels. Carcinine can be used for the researches of inflammation, neurological, cardiovascular and metabolic disease, such as retinal damage, seizure and diabetes.
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- CAS No.: 56897-53-1
- Formule: C8H14N4O
- Masse moléculaire:182.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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H3 receptor 0.2939 μM (Ki) |
H2 Receptor 365.3 μM (Ki) |
H1 Receptor 3621.2 μM (Ki) |
Carcinine (0.5 mM, 16 h) forms a stable adduct with 4-HNE (HY-113466) a retention time of 17.5 mins[1].
Carcinine (1 μg-2 mg, 90 mins) inhibits 4-HNE-induced modification of mouse retinal proteins with an IC50 of 33.2 μg/μL[1].
Carcinine (1 mg, 0-72 h) reverses pre-formed 4-HNE-retinal protein adducts[1].
Carcinine (5 mM, 4-8 h) rescues the protein level of retinol dehydrogenase 12 in mouse retinal explants treated with 4-HNE[1].
Carcinine shows high affinity for histamine H3 receptor (Ki = 0.2939 μM) and extremely low affinity for H1 (Ki = 3621.2 μM) and H2 (Ki = 365.3 μM) receptors[2].
Carcinine (2-50 μM, 22.5 mins) increases K+-induced endogenous 5-HT release but shows no effect on dopamine release in mouse forebrain slices[2].
Carcinine (10 mM) scavenges hydroxyl radicals and inhibits deoxyribose damage[3].
Carcinine (10-25 mM, 60 mins) reduces linoleic acid 13-monohydroperoxide (LOOH) and phosphatidylcholine hydroperoxide (PCOOH) in PC liposomes to hydroxy products (LOH)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Carcinine (0.2-20 mg/mouse, i.g., daily for 5 days) protects the retina in BALB/c mice with bright light exposure[1].
Carcinine (5-50 mg/kg, i.p.) decreases cortical and midbrain histamine content in ICR mice[2].
Carcinine (2-20 mg/kg, i.p., before PTZ) significantly reduces the seizure stage induced by pentylenetetrazole (PTZ) in ICR mice[2].
Carcinine (10-20 mg/kg, i.p., 30 mins before scopolamine) significantly ameliorates Scopolamine (HY-N0296)-induced learning deficit in ICR mice[2].
Carcinine (10-50 mg/kg, i.p.) increases the total ambulation distance in ICR mice[2].
Carcinine (10-100 μg, heart injection via perfusate cannula) shows positive inotropic effect in guinea pigs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice with bright light exposure[1]
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Dosage:0.2, 2 and 20 mg/mouse
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Administration:Orally gavage, daily for 5 days
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Result:Showed that the rod a-wave amplitude increases from 84 μV to 257 μV, and the b-wave increaseed from 183 μV to 606 μV.
Decreased the loss rate of photoreceptor nuclei.
Prevented light-induced reduction of RDH12 protein level.
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Animal Model:Pentylenetetrazole (PTZ)-induced kindling mice models[2]
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Dosage:2, 10 and 20 mg/kg
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Administration:Intraperitoneally injection, before PTZ
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Result:Reduced the seizure stage.
Prolonged the latency to myoclonic jerks and latency to generalized clonic seizures.
Chemical Information
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CAS No. 56897-53-1
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Masse moléculaire 182.22
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Formule C8H14N4O
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SMILES
NCCC(NCCC1=CN=CN1)=O
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Synonyms
β-Alanylhistamine
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Marchette LD, et al. Carcinine has 4-hydroxynonenal scavenging property and neuroprotective effect in mouse retina. Invest Ophthalmol Vis Sci. 2012 Jun 20;53(7):3572-83. [Content Brief]
[2]. Chen Z, et al. Pharmacological effects of carcinine on histaminergic neurons in the brain. Br J Pharmacol. 2004 Nov;143(5):573-80. [Content Brief]
[3]. Babizhayev MA, et al. L-carnosine (beta-alanyl-L-histidine) and carcinine (beta-alanylhistamine) act as natural antioxidants with hydroxyl-radical-scavenging and lipid-peroxidase activities. Biochem J. 1994 Dec 1;304 ( Pt 2)(Pt 2):509-16. [Content Brief]
[4]. Brotman DN, et al. Positive inotropic effect of carcinine in the isolated perfused guinea pig heart. Crit Care Med. 1990 Mar;18(3):317-21. [Content Brief]
[5]. Palmieri B, et al. The role of Carcinine treatment on glico-lipidic imbalance of patients with altered blood glucose pattern. Clin Ter. 2023 Mar-Apr;174(2):195-202. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Carcinine Related Classifications
HY-107567 Related Classifications
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