药理术语表

Inhibitor

A molecule that binds to a receptor and decreases its activity. It can be reversible or irreversible, and stops a substrate fromentering the enzyme's active site and/or hinder the enzyme from catalyzing itsreaction.

 

Agonist

A molecule binding to and activating a receptor; It can be full, partial or inverse. A full agonist has higher efficacy than a partial agonist in activating the receptor. An inverse agonist exhibits an opposite effect to that of an agonist, but they bind to the same receptor binding-site.

 

Antagonist

A molecule attenuating an agonist’s activity on a receptor; It can be competitive or non-competitive,each of which can be reversible or irreversible. A competitive antagonist binds to the same site of a receptor as the agonist but does not activate it, thus blocks the agonist's action. A non-competitive antagonist binds to anallosteric (non-agonist) site on the receptor to prevent activation of the receptor. A reversible antagonist binds non-covalently to the receptor, and the inhibition can be reversible. An irreversible antagonist binds covalently to the receptor and cannot be displaced by either competing ligands or washing.

 

Non-Specific Binding

The proportion of radioligand which is not displaced by other competitive ligands specific forthe receptor. It can be binding to other receptors or proteins, partitioninginto lipids or other things.

 

Specific Binding

The proportion of radioligand that can be displaced by competitive ligands specific for thereceptor.

 

IC50

In a functional assay, the molar concentration of an agonist or antagonist which produces 50% of its maximum possible inhibition. In a radioligand binding assay, the molarconcentration of competing ligand which reduces the specific binding of a radioligand by 50%.

 

ID50

A dose of a drug that causes 50% of the maximum possible inhibition.

 

Kd

The dissociation constant for a radiolabeled molecule determined by saturation analysis. It is the molar concentration of radioligand which, at equilibrium, occupies 50% of the receptors.

 

Ki

The inhibition constant for a ligand, which denotes the affinity of the ligand for a receptor. Measured using a radioligand competition binding assay, it is the molar concentration of the competing ligand that occupies 50% of the receptors if no radioligand is present.

 

EC50

The molar concentration of an agonist that exerts 50% of the maximum possible response.

 

ED50

An effective dose of a drug for 50% of its maximum response.

 

Ex vivo

Means that which takes place outside a living organism.

 

Minimum inhibitory concentration (MIC)

The lowest concentration of an agent inhibiting visible growth of a bacterium. This is in difference to the minimum bactericidal concentration (MBC) which is the concentration resulting in microbial death as defined by the inability tore-culture bacteria. The closer the MIC is to the MBC, the more bactericidal the compound.

 

给药途径缩写

p.o.      Oral                               Via mouth

i.p.       Intraperitoneal               Into peritoneal cavity

s.c.      Subcutaneous               Under the skin

i.v.       Intravenous                    Into a vein

i.c.       Intracerebral                  Into the brain

i.c.v.    Intracerebroventricular   Into the ventricles of the brain

i.a.       Intra-arterial                   Into the lumen of an artery
i.d.       Intradermal                    Into the dermal layer of the skin

i.m.      Intramuscular                Into a skeletal muscle

i.t.        Intraperitoneal               Into the spinal canal

 

给药频率缩写

q.d.     Once a day

b.i.d.   Twice a day

t.i.d.    Three times a day