Octopamine is present in relatively high concentrations in neuronal as well as in non-neuronal tissues of most invertebrate species studied, and modulates almost every physiological process. Octopamine acts as neurohormone including desensitization of sensory inputs, influence on learning and memory, or regulation of the mood of the animal in the central nervous system. Octopamine is the only neuroactive non-peptide transmitter whose physiological role is restricted to invertebrates, and all octopamine receptors belong to the family of G-protein coupled receptors.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||38 mg/mL in DMSO|
|Related Dopamine Receptor Products|
A-381393 IS AN EFFECTIVE, SELECTIVE, AND BLOOD-BRAIN BARRIER-PERMEABLE dopamine D4 receptor Antagonist, dopamine D for humans4.4，D4.2 AND D4.7 receptors Ki The values are 1.5, 1.9, and 1.6 nM, respectively, with selectivity being D1，D2，D3，D5 MORE THAN 2700 TIMES THE DOPAMINE RECEPTOR. A-381393 VS. 5-HT2A MODERATE SELECTIVITY, Ki The value is 370 nM.
Pridopidine is a dopamine (DA) stabilizer that acts as a low-affinity dopamine D2 receptor (D2R) antagonist. Pridopidine high affinity acts on sigma 1 receptor (S1R),Ki Values of 70 to 80 nM are approximately 100 times higher than their affinity for D2R.
ML417 is a highly selective and brain penetrant D3 dopamine receptor (D3R) agonist, with EC50 of 38 nM.
Cariprazine is a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor.
PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively.
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