Befiradol
Encyclopedia
Befiradol is a very potent
and highly selective
5-HT1A receptor
full agonist. It has powerful analgesic
and antiallodynic effects comparable to those of high doses of opioid
painkillers, but with fewer and less prominent side effect
s, as well as little or no development of tolerance with repeated use. A SAR study revealed that replacement of the dihalophenyl moiety by 3-benzothienyl
increases maximal efficacy from 84% to 124% (Ki=2.7 nM)
Potency (pharmacology)
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug evokes a larger response at low concentrations, while a drug of lower potency evokes a small response at low concentrations...
and highly selective
Binding selectivity
Binding selectivity refers to the differing affinities with which different ligands bind to a substrate forming a complex. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate...
5-HT1A receptor
5-HT1A receptor
The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gi/Go and mediates inhibitory neurotransmission...
full agonist. It has powerful analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
and antiallodynic effects comparable to those of high doses of opioid
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
painkillers, but with fewer and less prominent side effect
Adverse effect
In medicine, an adverse effect is a harmful and undesired effect resulting from a medication or other intervention such as surgery.An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. If it results from an unsuitable or incorrect dosage or...
s, as well as little or no development of tolerance with repeated use. A SAR study revealed that replacement of the dihalophenyl moiety by 3-benzothienyl
Benzothiophene
Benzothiophene is an aromatic organic compound with a molecular formula C8H6S and an odor similar to naphthalene . It occurs naturally as a constituent of petroleum-related deposits such as lignite tar. Benzothiophene has no household use...
increases maximal efficacy from 84% to 124% (Ki=2.7 nM)