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) 与 4-HNE (HY-113466) 形成稳定加合物，保留时间为 17.5 分钟^[1]。
Carcinine (1 μg-2 mg, 90 mins) 可抑制 4-HNE 诱导的小鼠视网膜蛋白修饰， IC₅₀ 值为 33.2 μg/μL^[1]。
Carcinine (1 mg, 0-72 h) 可逆转预先形成的 4-HNE-视网膜蛋白加合物^[1]。
Carcinine (5 mM, 4-8 h) 可恢复经 4-HNE 处理的小鼠视网膜外植体中视黄醇脱氢酶 12 的蛋白水平^[1]。
Carcinine 对组胺 H₃ 受体表现出高亲和力 (K_i 值为 0.2939 μM)，而对 H₁ 受体 (K_i 值为 3621.2 μM) 和 H₂ 受体 (K_i 值为 365.3. μM) 亲和力较低^[2]。
Carcinine (2-50 μM, 22.5 mins) 会增加小鼠前脑切片中的 K⁺ 诱导的内源性 5-HT 释放，但对多巴胺释放无影响^[2]。
Carcinine (10 mM) 可清除羟基自由基并抑制脱氧核糖损伤^[3]。
Carcinine (10-25 mM, 60 mins) 可减少 PC 脂质体中的亚油酸 13-氢过氧化物 (LOOH) 和磷脂酰胆碱氢过氧化物 (PCOOH) 还原为羟基产物 (LOH)^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Carcinine (2 M，每只眼 1 μL，玻璃体内注射，光照前恢复 48 小时) 对强光暴露的 BALB/c 小鼠的视网膜光感受器有保护作用^[1]。
Carcinine (0.2-20 mg/mouse，灌胃，每日一次，连续 5 天) 对强光暴露的 BALB/c 小鼠的视网膜有保护作用^[1]。
Carcinine (5-50 mg/kg，腹腔注射) 可降低 ICR 小鼠皮质和中脑的组胺含量^[2]。
Carcinine (2-20 mg/kg，腹腔注射，在 PTZ 处理前给药) 可显著降低戊四氮 (PTZ) 诱导的 ICR 小鼠的癫痫发作等级^[2]。
Carcinine (10-20 mg/kg，腹腔注射，在东莨菪碱处理前 30 分钟) 可显著改善东莨菪碱 (HY-N0296) 诱导的 ICR 小鼠学习障碍^[2]。
Carcinine (10-50 mg/kg，腹腔注射) 可增加 ICR 小鼠的总移动距离^[2]。
Carcinine (10-100 μg，通过灌流套管进行心脏灌注) 在豚鼠中显示出正性肌力作用^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

182.22

C₈H₁₄N₄O

56897-53-1

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]