Loperamide D6 hydrochloride, a deuterium-labeled variant of Loperamide hydrochloride, acts as an opioid receptor agonist utilized for diarrhea treatment.
ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverses loperamide-induced delayed gastric emptying in a rat model of castor oil-induced diarrhea.
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) 是一种对 hNK2R 具有高选择性的NK2R激动剂,EC50为 3.7 nM。该化合物在饮食诱导肥胖 (DIO) 小鼠模型中有效控制体重,并改善野生型小鼠中由Loperamide引起的尿路功能问题。[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) 可用于与神经激肽受体相关的疾病研究,如肥胖、胰岛素抵抗和2型糖尿病。