Name: TMB 8 (hydrochloride)
Rating: 5 (10 reviews)

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HIT ID:HIT212030632
Cas No:53464-72-5
常用名:TMB 8 (hydrochloride)
IUPAC:8-(diethylamino)octyl 3,4,5-trimethoxybenzoate hydrochloride
IUPAC:8-(diethylamino)octyl 3,4,5-trimethoxybenzoate hydrochloride
InChI key:KFJZVXKPPQIYCG-UHFFFAOYSA-N

分子式:C22H38ClNO5
分子量:432
氢键供体数 (HBD):0
氢键受体数 (HBA):5
LogP:3.84
SMILES:Cl.CCN(CC)CCCCCCCCOC(=O)c1cc(OC)c(OC)c(OC)c1
SMILES:Cl.CCN(CC)CCCCCCCCOC(=O)c1cc(OC)c(OC)c(OC)c1

TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration of 50 μM and inhibiting calcium influx and efflux in isolated guinea pig ileum when used at a concentration of 65 μM. It has been used in the study of intracellular calcium dynamics, particularly in smooth muscle. TMB 8 also inhibits protein kinase C (PKC) activity in a dose-dependent manner.

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