Taminadenant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Taminadenant 是一种腺苷受体 A2a 拮抗剂。

Taminadenant is an adenosine receptor A2a antagonist.

Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A2ARSNAP, but completely antagonizes the agonist-mediated cAMP accumulation in A2ARSNAP expressing HEK cells with an IC50 of 72.8 ± 17.4 nM.

Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) attenuates the cataleptic effects of Haloperidol, attenuates pilocarpine-induced tremulous jaw movement, enhances the effects of L-DOPA, shows a robust antiparkinsonian activity and displays antidyskinetic efficacy. Animal Model:Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))Dosage:3, 10, or 30 mg/kgAdministration:p.o.; single dosage Result:Dose-dependently attenuated the cataleptic effects of Haloperidol when administered 1 h after Haloperidol injection.Animal Model:Sprague-Dawley rats (240-250 g; induced tremulous jaw movement by s.c. with 1 mg/kg Pilocarpine (HY-B0726A))Dosage:0.3, 3, or 7.5 mg/kg Administration:p.o.; single dosage Result:Dose-dependently attenuated pilocarpine-induced tremulous jaw movement, being effective at the lowest dose tested.Animal Model:Sprague-Dawley rats (240-250 g; induced hemiparkinsonian by unilateral injection of 6-OHDA (HY-B1081) in the medial forebrain bundle)Dosage:0.3 and 3 mg/kg Administration:p.o.; single dosage Result:Enhanced the effects of L-DOPA with a minimum efficacious dose (MED) of 3 mg/kg p.o..Animal Model:Sprague-Dawley rats (240-250 g; induced dyskinesias by i.p. 4 mg/kg L-DOPA (HY-N0304) for 14 days and i.p. 15 mg/kg Benserazide hydrochloride (HY-B0404A))Dosage:0.3 or 3 mg/kg Administration:p.o.; single dosage Result:Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.

Taminadenant

Apoptosis

Adenosine Receptor

Adenosine Receptor

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1337962-47-6

306.127

C10H8BrN7

>98% (HPLC)

DMSO : 125 mg/mL 408.34 mM

NC1=NC(N2N=CC=C2)=NC(N3N=CC=C3)=C1Br

5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine

(-20℃)

With Ice Pack

≥ 2 years