Opioids receptor agonists

Receptor desensitization, internalization, and/or down-regulation may play a role in the development of tolerance to opioid receptor agonists (Clark et al. 

Anzini M, Canullo L, Braile C, et ah Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. J Med Chem 46 3833-3864, 2003... 

Heroin, a synthetic derivative of the p opioid receptor agonist morphine, is a well-documented narcotic that alters mood and rewarding behaviors. To date, heroin is the most abused opioid with an estimated 750,000-1,000,000 hardcore users in the... 

Glaum SR, Miller RJ, Hammond DL (1994) Inhibitory actions of delta 1-, delta 2-, and mu-opioid receptor agonists on excitatory transmission in lamina II neurons of adult rat spinal cord. 

Choi Y, Chuang LF, Lam KM, Kung HF, Wang JM, Osburn BI, Chuang RY (1999) Inhibition of chemokine-induced chemotaxis of monkey leukocytes by mu-opioid receptor agonists. In Vivo 13 389-396... 

Iwamoto, E.T. Locomotor activity and antinociception after putative mu, kappa and sigma opioid receptor agonists in the rat Influence of dopaminergic agonists and antagonists. J Pharmacol Exp Ther 217 451-460, 1981. 

Zimmerman DM, Leander JD. Selective opioid receptor agonists and antagonists research tools and potential therapeutic agents. J Med Chem 1990 33 895-902. 

Chang KJ, Rigdon GC, Howard JL, McNutt RW. A novel, potent and selective nonpeptidic delta opioid receptor agonist. J Pharmacol Exp Ther 1993 267 852-857. 

Calderon SN, Rothman RB, Porreca F, Flippen-Anderson JL, McNutt RW, Xu H, Smith LE, Bilsky EJ, Davis P, Rice KC. Probes for narcotic receptor mediated phenomena. 19. Synthesis of ( + )-4-[(aR)-a-((25,5R)-4-allyl-2,5-dimethyl-l -piperazinyl)-3-methoxybenzyl]-/V,/V-diethylbenzamide (SNC80) a highly selective, nonpeptide delta opioid receptor agonist. J Med Chem 1994 37 2125-2128. 

Kamei J, Saitoh A, Ohsawa M, Suzuki T, Misawa M, Nagase H, Kasuya Y. Antinociceptive effects of the selective non-peptidic delta-opioid receptor agonist TAN-67 in diabetic mice. Eur J Pharmacol 1995 276 131-135. 

Substance P First order sensory neuron Sensitization Opioid receptor agonists (e.g., morphine)... 

Shippenberg T., Heidbreder C. Kappa opioid receptor agonists prevent sensitization to the rewarding effects of cocaine. NIDA Res. Monogr. 153 456, 1994. 

Heidbreder C., Goldberg S., Shippenberg T. The kappa-opioid receptor agonist U-69,593 attenuates cocaine-induced behavioral sensitization in the rat. Brain Res. 616 335, 1993. 

Portoghese P, Moe S, Takemori A. A selective deltal opioid receptor agonist derived from oxymorphone evidence for separate recognition sites for deltal opioid receptor agonists and antagonists. 

Aminoacid Aminoacid DCC Opioid receptor agonist 96 2006JME1773... 

Delta opioid receptor Agonist analog Diarylmethyl piperazine 23... 

Waddell AB, Holtzman SG. (1999). Modulation of cocaine-induced antinociception by opioid-receptor agonists. Pharmacol Biochem Behav. 62(2) 247-53. 

Cao YJ, Bhargava HN. (1997). Effects of ibogaine on the development of tolerance to antinociceptive action of mu-, delta-, and kappa-opioid receptor agonists in mice. Brain Res. 752(1-2) 250-4. Cappendijk SL, Dzoijic MR. (1993). Inhibitory effects of ibogaine on cocaine self-administration in rats. EurJ Pharmacol. 241(2-3) 261-65. 

The 1,2-aminoamides are now established as a chemical series with several highly selective kappa opioid receptor agonists. However, the biological activity of 1,2-aminoamides is not restricted to kappa analgesics. Several related structures exhibit biological activity in other systems of importance and interest. In order to appraise the significance of this chemical class and to put the SAR for kappa receptor activity into context, a selection of these compounds is discussed here. This is not a comprehensive literature review but rather a selection of a few compounds to illustrate the broad range of medieinal activity exhibited by these somewhat similar chemical structures. 

Eguchi M. Recent advances in selective opioid receptor agonists and antagonists. Med Res Rev 2004 24 182-212. 

The discovery of a potent and selective K-opioid receptor agonist compound, salvinorin A (54), a hallucinogenic neoclerodane diterpenoid from Salvia divinorum Epling and Jativa, has created particular interest in recent years, since it is the first nonnitrogenous compound found to demonstrate this type of activity. 

Acute abdominai conditions As with other p-opioid receptor agonists, the administration of buprenorphine or buprenorphine/naloxone may obscure the diagnosis or clinical course of patients with acute abdominal conditions. 

However, k opioid receptor agonists offer an indirect possibility to modulate some of the abuse-related effects of narcotics. Presently, more research is needed on this subject. 

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