Bioactivity | (S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems[1]. |
Invitro | PNU-282987 (free base) (Compound C7) 可取代大鼠脑匀浆中的 R7 选择性拮抗剂甲基乌头碱 (MLA),Ki 为 27 nM[1]。PNU-282987 具有 α7 nAChR 激动剂活性,EC50 为 154 nM[1]。PNU-282987 还对 5-HT3 受体具有抑制作用,IC50 值为 4541 nM[1]。 0 --> (S)-PNU-282987 hydrochloride 相关抗体: |
In Vivo | PNU-282987 (free base) (Compound C7) (静脉注射;1, 3 mg/kg) 可逆转门控缺陷[1]。PNU-282987 (30 μM) 以浓度依赖性和 MLA 可阻断的方式在大鼠海马神经元中激发电流[1]。 |
Name | (S)-PNU-282987 hydrochloride |
CAS | 128311-08-0 |
Formula | C14H18Cl2N2O |
Molar Mass | 301.21 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Bodnar AL, Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8. |