Carcinine  (Synonyms: β-Alanylhistamine)

Carcinine (β-Alanylhistamine) is a selective and orally active histamine H3 receptor antagonist with a K_i 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^{[1][2][3][4][5]}.

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 (K_i = 0.2939 μM) and extremely low affinity for H₁ (K_i = 3621.2 μM) and H₂ (K_i = 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 (2 M, 1 μL per eye, intravitreally injection, 48 h recovery before light exposure) protects retinal photoreceptors in BALB/c mice with bright light exposure^[1].
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.

182.22

C₈H₁₄N₄O

56897-53-1

NCCC(NCCC1=CN=CN1)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]