cognitive disorder

GR 125743 是选择性的5-HT1B 1D 受体拮抗剂，与野生型的人 h5-HT1B 和 5-HT1D 结合的pKi 分别为 8.85 和 8.31，可用于帕金森病和心血管疾病的研究。

MK-0249 FA 是一种具有口服活性、选择性和高效性的组胺 H3 反向激动剂，可用于研究成人注意力缺陷、多动症神经分裂和认知障碍。

Guanfacine hydrochloride (Intuniv) 是一种 α2A 肾上腺素受体激动剂，Kd=31 nM，具有抗高血压作用。

Samelisant dihydrochloride (SUVN-G3031) is a antagonist of histamine H3 receptor with potential for the treatment of cognitive impairment, dementia, attention deficit hyperactivity disorder, epilepsy, sleep disorders, obesity, schizophrenia, eating disorders, and pain.

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

Sofinicline benzenesulfonate (ABT 894 benzenesulfonate) 为一种针对nAChR的α4β2亚型具有高选择性的烟碱型乙酰胆碱受体激动剂（IC50=0.1 nM）。该化合物展现了调节认知功能的能力，尤其是在改进注意力、记忆以及工作记忆方面。此外，Sofinicline benzenesulfonate 在对抗注意力缺陷及多动障碍（ADHD）的研究领域中具有重要应用价值。