Amylin, amide, rat is a GABA uptake inhibitor selective for the BGT-1 (mGAT-2) transporter[1-2]. Amylin, amide, rat lowers blood glucose levels by inhibiting glucagon secretion and delaying gastric emptying, while also increasing satiety through central nervous system action to reduce food intake. Amylin, amide, rat and its analogs are utilized in research on diabetes and related metabolic disorders[3-4].
In vitro, HepG2 human liver cancer cells were treated with Amylin, amide, rat (1nM–1µM) for 10-45 minutes. Amylin, amide, rat dose-dependently stimulated adenylate cyclase activity in their cell membrane preparations[5]. Amylin, amide, rat (1nM–1µM) was applied to HEK293S and Cos 7 cells expressing human amylin receptors, and the cAMP response was measured. Amylin, amide, rat significantly activated the AMY1(a) and AMY3(a) receptors while enhancing cAMP production[6].
In vivo, Amylin, amide, rat (0.312-80.0µg) was administered to rats via intracerebroventricular injection. Amylin, amide, rat dose-dependently reduced their spontaneous motor activity, significantly increased body temperature, and decreased food intake in animals fasted for 22 hours[7]. In anesthetized male Sprague-Dawley rats, a single intravenous injection of Amylin, amide, rat (10-1000pmol/kg) elicited a significant pressor response at low doses (10-100pmol/kg), which appeared within 30-60 seconds and lasted for 15 minutes, while also increasing plasma renin activity. Higher doses (>1nmol/kg) induced a depressor response[8].
References:
[1] Bower RL, Hay DL. Amylin structure-function relationships and receptor pharmacology: implications for amylin mimetic drug development. Br J Pharmacol. 2016 Jun;173(12):1883-98.
[2] Gostynska SE, Karim JA, Ford BE, et al. Amylin receptor subunit interactions are modulated by agonists and determine signaling. Sci Signal. 2025 Aug 19;18(900):eadt8127.
[3] Harris PJ, Cooper ME, Hiranyachattada S, et al. Amylin stimulates proximal tubular sodium transport and cell proliferation in the rat kidney. Am J Physiol. 1997 Jan;272(1 Pt 2):F13-21.
[4] Vine W, Smith P, LaChappell R, et al. Effects of rat amylin on renal function in the rat. Horm Metab Res. 1998 Aug;30(8):518-22.
[5] Sheriff S, Fischer JE, Balasubramaniam A. Characterization of amylin binding sites in a human hepatoblastoma cell line. Peptides. 1992 Nov-Dec;13(6):1193-9.
[6] Gingell JJ, Burns ER, Hay DL. Activity of pramlintide, rat and human amylin but not Aβ1-42 at human amylin receptors. Endocrinology. 2014 Jan;155(1):21-6.
[7] Bouali SM, Wimalawansa SJ, Jolicoeur FB. In vivo central actions of rat amylin. Regul Pept. 1995 Apr 14;56(2-3):167-74.
[8] Haynes JM, Hodgson WC, Cooper ME. Rat amylin mediates a pressor response in the anaesthetised rat: implications for the association between hypertension and diabetes mellitus. Diabetologia. 1997 Mar;40(3):256-61.
Amylin, amide, rat是一种大鼠来源的酰胺化肽激素，具有调节血糖的活性[1-2]。Amylin, amide, rat可通过抑制胰高血糖素分泌和延缓胃排空来降低血糖水平，同时通过中枢作用增加饱腹感以减少食物摄入。Amylin, amide, rat及其类似物可用于糖尿病和相关代谢疾病的研究[3-4]。
在体外，Amylin, amide, rat（1nM–1μM）处理人肝癌细胞HepG2 10-45分钟。Amylin, amide, rat可以剂量依赖性地刺激其细胞膜制备物中腺苷酸环化酶的活性[5]。Amylin, amide, rat（1nM–1μM）处理表达人amylin受体的HEK293S和Cos 7细胞，随后测量cAMP响应。Amylin, amide, rat显著激活AMY1(a)和AMY3(a)受体，同时增强cAMP产生[6]。
在体内，Amylin, amide, rat（0.312-80.0μg）通过侧脑室注射给予大鼠，Amylin, amide, rat可剂量依赖性地降低其自发运动活动并显著升高体温，同时减少禁食22小时动物的食物摄入[7]。Amylin, amide, rat（10-1000pmol/kg；单次静脉注射）用于处理麻醉的雄性Sprague-Dawley大鼠。Amylin, amide, rat可在低剂量（10-100pmol/kg）时引发显著的升压反应，该效应在30-60秒内出现并持续15分钟，同时增加血浆肾素活性。高剂量（>1nmol/kg）则引起降压反应[8]。