High agonist intrinsic activity

High agonist intrinsic activity (lA), resulting from high receptor occupancy leading to maintenance of the pharmacological effect [11]. 

HU-210 has particularly high affinity for both CB and CB2 receptors. It also exhibits high relative intrinsic activities at these receptors. Indeed, it is remarkably potent as a cannabinoid receptor agonist and exhibits an exceptionally long duration of action in vivo. The marked affinity and efficacy that HU-210 shows at cannabinoid receptors is due largely to the replacement of the pentyl side chain of A -THC with a dimethylheptyl group. 

D-cycloserine and (-l-R)-HA-966 are partial agonists at the glycincB site with different levels of intrinsic activity (Karcz-Kubicha et al. 1997). Although these systemically active partial agonists do not induce receptor desensitization they have favourable therapeutic profiles in some in vivo models (Lanthorn 1994 see Danysz and Parsons 1998). This may, in part, be due to their own intrinsic activity as agonists at the glycines site, which would serve to preserve a certain level of NMDA receptor function even at very high concentrations (Danysz and Parsons 1998). 

Requip Ropinirole HC1 0.25,0.5,1,2,3,4, 5 mg Tablet Parkinson s disease A nonergoline dopamine Croscarmellose Na, lactose agonist with high hydrous, magnesium stearate, relative in vitro MCC specificity and full intrinsic activity at the D2 and D3 dopamine receptor subtypes GSK... 

Buprenorphine is a semi-synthetic, partial mu-agonist, highly lipophilic, opioid drug. Because it is a partial agonist, when buprenorphine competes with morphine or heroin for mu-receptors it can reduce their maximum effect. Buprenorphine binds strongly to mu and kappa opiate receptors it associates with the mu-receptor slowly (30 minutes), but with high affinity, low intrinsic activity and slow and incomplete dissociation. The slow dissociation from the receptor probably limits the intensity of withdrawal by preventing the rapid... 

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