Sumanirole maleate is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. It has greater than 200-fold selectivity for the D2 receptor subtype versus the other dopamine receptor subtypes in radioligand binding assays. In cell-based assays, sumanirole is a fully efficacious agonist, with EC50 values between 17 and 75 nM. In animals, sumanirole elicits many physiological responses attributed to D2-like receptor function. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels (ED50 = 12.1 μmol/kg i.p.). Sumanirole s.c. dose dependently decreased plasma prolactin levels and depressed dopamine neuron firing rates in the substantia nigra pars compacta with an ED50 of 2.3 μmol/kg i.v.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related Dopamine Receptor Products|
SHP099 hydrochloride is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM.
Sulpiride is a dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid.
rac-Rotigotine Hcl is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM.
Promazine (hydrochloride) is a D2 dopamine receptor antagonist, belongs to the phenothiazine class of antipsychotics, used to treat schizophrenia.
|Prochlorperazine dimaleate salt
Prochlorperazine dimaleate is a dopamine (D2) receptor antagonist.
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