Ibodutant (MEN15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1. Ibodutant selectively blocks the tachykinin receptor NK2, with blockade practically complete in nanomolar concentrations.
|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.
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|[Leu31,Pro34]-NPY TFA (human,rat)
[Leu31,Pro34]-NPY TFA (human,rat) is a specific neuropeptide Y1 receptor agonist.
Vapreotide acetate (BMY-41606 acetate; RC160 acetate) is a neurokinin-1 (NK1) receptor antagonist with IC50 value of 330 nM.
Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
SCH-619734 is an orally bioavailable, centrally-acting, selective neurokinin 1 receptor (NK1-receptor) antagonist with a Ki of 0.66 nM.
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