产品
编 号：F618911
分子式：C23H26ClFN4O4S
分子量：508.99
分子式：C23H26ClFN4O4S
分子量：508.99
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CAS No: 2250025-91-1
产品详情
生物活性：
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
体内研究：
LEI-101 (2, 6, and 20 mg/kg, po) shows in vivo activity in a spinal nerve ligation model of neuropathic pain in rats.LEI‐101 (p.o. or i.p.) at 3 or 10?mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice.Animal Model:Neuropathy-induced mechanical allodynia in male wistar rats.
Dosage:2, 6, and 20 mg/kg.
Administration:PO, single dose.
Result:Induced a dose-dependent antinociceptive effect after 2 h of dosing.
Animal Model:Fed male Wistar rats.
Dosage:1 mg/kg iv and 5 mg/kg po (Pharmacological Analysis).
Administration:IV and PO.
Result:Exhibited T1/2 of 1.7 h and 0.8 h for po and iv administration.Had a low clearance and 100% oral bioavailability.
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
体内研究：
LEI-101 (2, 6, and 20 mg/kg, po) shows in vivo activity in a spinal nerve ligation model of neuropathic pain in rats.LEI‐101 (p.o. or i.p.) at 3 or 10?mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice.Animal Model:Neuropathy-induced mechanical allodynia in male wistar rats.
Dosage:2, 6, and 20 mg/kg.
Administration:PO, single dose.
Result:Induced a dose-dependent antinociceptive effect after 2 h of dosing.
Animal Model:Fed male Wistar rats.
Dosage:1 mg/kg iv and 5 mg/kg po (Pharmacological Analysis).
Administration:IV and PO.
Result:Exhibited T1/2 of 1.7 h and 0.8 h for po and iv administration.Had a low clearance and 100% oral bioavailability.
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