partial agonism造句

• Varenicline's partial agonism on the ? 4 ? 2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's.
• It was found that partial agonism results from deficiency in the first step, and that the opening and shutting steps are essentially the same for both full and partial agonists.
• Unlike most current antipsychotics, such as haloperidol, risperidone, and olanzapine, lumateperone does not disrupt signaling, a property which is likely due to partial agonism of presynaptic D 2 receptors.
• Moreover, due to partial agonism of the KOR, where it appears to possess significantly greater intrinsic activity relative to the MOR, diprenorphine can produce sedation as well as, in humans, hallucinations.
• 4-" O "-Methylhonokiol is a potent partial agonism via different pathways ( cAMP and Ca 2 + ) and potently inhibits osteoclastogenesis . 4-O-Methylhonokiol further attenuates memory impairment in presenilin 2 mutant mice through reduction of oxidative damage and inactivation of astrocytes and the ERK pathway.
• These super-potent opioids, with the single exception of buprenorphine ( which has an improved safety-profile due to its partial agonism character ), are not used in humans because the dose for a human is so small that it would be difficult to measure properly, so there is an excessive risk of overdose leading to fatal respiratory depression.
• The fact that receptor conformation ( state ) would affect binding affinity of a ligand was used to explain a mechanism of partial agonism of receptors by del Castillo & Katz in 1957 was based on their work on the action of acetylcholine at the motor endplate The del Castillo-Katz mechanism divorces the binding step ( that can be made by agonists as well as antagonists ) from the receptor activation step ( that can be only exerted by agonists ), describing them as two independent events.