Agonists moderate

Tramadol Mixed effects weak P-agonist, moderate SERT inhibitor, weak NET inhibitor Analgesia Moderate pain adjunct to opioids in chronic pain syndromes Duration 4-6 h Toxicity Seizures... 

CLASS STRONG AGONIST MODERATE AGONIST PARTIAL AGONIST antagonists... 

P-Adrenergic receptor 2 Amino acid variants moderately associated with receptor function and agonist induced down regulation. Some variants may predispose to some types of asthma and modulate action of p-2-adrenergic drugs. 

All clinically used opiates have the same pharmacology since they all act on the mu receptor with the exception of the kappa agonist, pentazocine. Opiates are used to relieve moderate to severe pain whatever the cause (accidents, post-operative pain, cancer, etc.) and are used pre-, intra- and post-operatively. The mu opiates differ only in potency and pharmacokinetics. Examples are ... 

In addition to the aetions of MDMA and other derivatives at 5-HT2 serotonin reeeptors. some of the effeets on serotonergic systems could be mediated via S-HTja reeeptors, at whieh MDMA has a moderate affinity. Direct agonist effects at this site might eontribute to the mood-altering and calming effects of the drug, sinee similar effects have been reported for novel anxiolyties sueh as ipsaperone and buspirone, which interact with 5-HTia serotonin reeeptors. 

A -THC, the main psychoactive component of cannabis, is a moderately potent partial agonist of the CBi and CB2 receptors, while cannabidiol has little affinity for either receptor (Table 6.7). The term classical cannabinoids is used to describe cannabinoid receptor modulators structurally related to (67), which have a tricyclic dibenzopyran core. While several other structural types of cannabinoid receptor modulators have been discovered in recent years, the classical cannabinoids are still by far the most extensively studied group in terms of SAR and pharmacology. 

The in vivo properties of compounds (464), (466) and (468)-(470) relative to (382) were investigated in two animal models a CBi agonist-induced hypotension rat model and a CBi agonist-induced hypothermia mouse model. Shown to be only moderately active in the in vitro screens, thiazole (464) and triazole (466) analogues failed to demonstrate convincing oral activity. Compound (468) was active in the hypotension model but showed... 

A series of 4,5-diarylimidazole-2-carboxamides has been reported as human CBi inverse agonists [312]. The initial HTS hit, (495), based on an analogous scaffold to (382), was found to have moderate affinity for the CBi receptor (7,000 nM). 

The addition of ipratropium bromide to inhaled p2-agonist therapy in acute severe asthma improves pulmonary function and decreases hospitalization rates in both adult and pediatric patients.31 The benefit of combining ipratropium and albuterol appears to be greatest in moderate to severe exacerbations, and the combination should be considered first-line therapy in severe exacerbations. 

Tegaserod maleate (Zelnorm) is a partial serotonin (5-HT4) receptor agonist that causes an increase in peristaltic activity and intestinal secretion and moderation of visceral sensitivity. It increases the frequency of bowel movements and reduces abdominal discomfort, bloating, and straining. It is indicated for the treatment of patients younger than 65 years of age who experience chronic idiopathic constipation. The most common adverse effects include headache, abdominal pain, diarrhea, and nausea. 

Isoproterenol (104) is an important agent for classification because of its selective p-receptor agonist activity. It is of special interest that its chronotropic (increase in heart rate) and inotropic (increase in force of contraction) effects exceed that of epinephrine it is also used in the management of mild to moderate asthma due to its bronchodilating effect, resulting in increased vital capacity of the lungs. 

LY 156735 is a [1-substituted analog of melatonin that has greater bioavailability than melatonin (Nickelsen et al. 2002). It is in an earlier stage of clinical trials in initial trials, it reduced the sleep onset time in patients with moderate sleep-onset insomnia. Several other specific melatonin receptor agonists and antagonists are in development (Rivara et al. 2005 Zlotos 2005) and presumably will be clinically tested over the next few years. 

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