agonist effect造句

• The mechanism for this is complex and may be separate from its delta agonist effects.
• The ? 1-agonist effect of both compounds was weak or non-existent.
• However, there is an agonist effect as well, which is a voltage-dependent effect.
• "' Trimebutine "'is a drug with antimuscarinic and weak mu opioid agonist effects.
• Initially, hallucinogens were thought to blockade these serotonin neurotransmitters, but persistent research led to this agonist effect conclusion.
• The toxicity is due to a partial agonist effect at M3 muscarinic receptors, leading to DNA fragmentation and neuronal death by apoptosis.
• Inverse agonists exert the opposite pharmacological effect of a receptor agonist, not merely an absence of the agonist effect as seen with antagonist.
• After psilocybin has been ingested and dephosphorylated, to psilocin, the mechanism it uses in the brain has a direct agonist effect on the 5-HT serotonin receptors.
• The weak partial agonist effect can be useful for some purposes, and has previously been used for purposes such as long-term maintenance of former alcohol or barbiturates.
• Some opioid antagonists are not pure antagonists but in fact do produce some weak opioid partial agonist effects, and can produce analgesic effects when administered in high doses to opioid-naive individuals.
• Naloxone on the other hand has no partial agonist effects, and is in fact a partial inverse agonist at ?-opioid receptors, and so is the preferred antidote drug for treating opioid overdose.
• By combining buprenorphine with samidorphan to block the MOR agonist effects, the combination acts more like a selective KOR antagonist, and produces only antidepressant effects, without typical MOR effects such as euphoria or substance dependence being evident.
• Buprenorphine has shown antidepressant effects in some human studies, thought to be because of its antagonist effects at the KOR, but has not been further developed for this application because of its MOR agonist effects and consequent abuse potential.
• The KOR agonist effects of oxilorphan are associated with dysphoria, which combined with its hallucinogenic effects, serve to limit its clinical usefulness; indeed, many patients who experienced these side effects refused to take additional doses in clinical trials.
• It is described as a mixed agonist / antagonist at the cannabinoid CB 1, meaning that it acts as an antagonist when co-administered alongside a more potent CB 1 agonist, but exhibits weak partial agonist effects when administered by itself.
• This suggests that it is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist effects at androgen receptors prevent the side effects associated with the anti-androgenic drugs traditionally used for treatment of BPH.
• For instance, mesulergine and metergoline are reported to be neutral antagonists at the h5-HT 7 ( a ) and h5-HT 7 ( d ) receptor isoforms but these drugs display marked inverse agonist effects at the h5-HT 7 ( b ) splice variant.
• The effect of RWJ-394674 when administered " in vivo " thus produces potent agonist effects at both ? and ? receptors through the combined actions of the parent drug and its active metabolite, with the ?-agonist effects counteracting the respiratory depression from the ?-opioid effects, and the only prominent side-effect being sedation.
• The effect of RWJ-394674 when administered " in vivo " thus produces potent agonist effects at both ? and ? receptors through the combined actions of the parent drug and its active metabolite, with the ?-agonist effects counteracting the respiratory depression from the ?-opioid effects, and the only prominent side-effect being sedation.
• It is derived from the widely used CB 1 antagonist rimonabant, and has similar potency and selectivity for the CB 1 receptor, but has been modified to remove the hydrogen bonding capability in the C-3 substituent region, which removes the inverse agonist effect that rimonabant produces at high doses, so that VCHSR instead acts as a neutral antagonist, blocking the receptor but producing no physiological effect of its own.