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CAS No. : 642407-63-4
MCE 国际站:Iptakalim hydrochloride
产品活性:Iptakalim hydrochloride 是亲脂性的对氨基化合物,是 ATP 敏感的钾通道 (KATP) 的开放剂,也是包含α4β2 的烟碱乙酰胆碱受体 (nAChR)拮抗剂。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:Potassium Channel | nAChR
In Vitro: Iptakalim (Ipt) hydrochloride has been shown to reverse pulmonary resistance vascular remodeling, inhibit proliferation of pulmonary arterial smooth muscle cells (PASMCs) and airway smooth muscle cells (ASMCs), as well as protect PAECs from pathological stimulation.
Iptakalim has an inhibitory effect on [Ca2+]cyt increase and the proliferation of pulmonary arterial SMCs induced by endothelin-1 through activation of KATP channels. Iptakalim (10 μM, 10 min) pretreatment of pulmonary arterial SMCs significantly prevents ransient ncrease of [Ca2+]cyt elicited by endothelin-1.
Iptakalim at he concentrations of 0.1, 1, and 10 AM lowered[3H]thymidine incorporation by 19.75±4.60% (n=10), 41.20±9.49% (n=10), and 54.74±10.11% (n=10), respectively, compared with that of cells treated only with endothelin-1.
In Vivo: Iptakalim (10-60 mg/kg) attenuates nicotine-evoked conditioned responding. Iptakalim also attenuates chamber activity in these nicotine test sessions.
.Iptakalim (60 mg/kg) pretreatment significantly reduced activity (LSD comparisons).
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