P-opioid receptor agonists

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... 

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. 

Glaum, S. R., Miller, R. J., Hammond, D. L. Inhibitory actions of 81, 82, and p-opioid receptor agonists on excitatory transmission in lamina II neurons of adult rat spinal cord, J. Neurosci. 1994, 14, 4965-4971. 

Ocana, M., Del Pozo, E., Barrios, M., Baeyens, J. M. Subgroups among p-opioid receptor agonists distinguished by ATP-sensitive K+ channel-acting drugs, British Journal of Pharmacology 1995, 114, 1296-1302. 

The development of acute tolerance and dependence evoked in mice by morphine can be suppressed by pretreatment with NTI. Multiple administration of either NTI or 5 NTII before and during chronic implantation with morphine pellets also substantially inhibits the development of morphine tolerance and dependence. These results suggest the use of 8 antagonists to be useful for the prevention of opioid tolerance and physical dependence without compromising the antinociceptive potency of p opioid receptor agonists (Abdelhamid et al., 1991). 

Anidox diphenylpyraline phenylpropanolamine, anileridine [ban, inn.usan] (anileridine hydrochloride [usAN] MK 89) is one of the phenylpiperidine series, a (p) OPIOID RECEPTOR AGONIST and OPIOID ANALGESIC. 

BAM-18P (bovine adrenal medulla octadecapeptide) is a 18 amino acid residue peptide isolated from the bovine adrenal medulla, a derivative of proenkephalin A. It is a (p) opioid receptor agonist. 

P-endorphin is an endogenous 31 amino acid residue peptide present in human, porcine, ovine and bovine pituitaries, with amino acid sequences identical to the 61-91 portion of their respective P-lipotropins, It is a potent (5 and p) OPIOID RECEPTOR AGONIST and OPIOID ANALGESIC. See also endorphins. 

Syncurine decamethonium iodide, syndyphalin (Syndyphalin 33) is a synthetic pseudopeptide enkephalin analogue, and is an OPIOID RECEPTOR AGONIST with OPIOID ANALGESIC activity, syndyphalin 25 (SD 25) is a synthetic pseudopeptide enkephalin analogue, and is a (p) opioid RECEPTOR AGONIST with OPIOID ANALGESIC activity. 

Tramake Tramal Zydol ) is a phenylcyclohexanol derivative, a (p) OPIOID RECEPTOR agonist with partial OPIOID ANALGESIC activity. It is also a monoamine (serotonin and noradrenaline) re-UPTAKE inhibitor, and this mechanism is thought independently to contribute a component to analgesic activity. 

Delta Receptors. There has been considerable interest in 6 opioid agonists because they exhibit antinociceptive effects without the side effects associated with p, opioid receptor agonists. Antinociceptive activity was first demonstrated with 6-selective opioid peptides (see Ref 218 for a review), and more recently with nonpeptidic 6-selective agonists (see Refs. 219-222 for reviews). Of particular interest is the activity of 6 agonists in inflammatory and neuropathic pain (220). Delta opioid receptors also modulate fx opioid receptors and, as discussed earlier, one classification of 6 opioid receptor subtypes was based on their association with p, opioid receptors. There is now considerable evidence that interaction between the two receptor types can alter the activity of p. opioid agonists. Delta agonists... 

It was recently recognized that opioid receptor agonists have antitussive effects [31]. Morphine (Fig. 7) is a potent p opioid receptor agonist that exhibits marked antitussive effect, and it has been used for the treatment of severe coughs. Codeine (Fig. 7) is one of the most reliable centrally acting antitussive agents its antitussive... 

Cami-Kobeci G, Neal AP, Bradbury FA, Purington LC, Aceto MD, Harris LS, Lewis JW, Traynor JR, Husbands SM (2009) Mixed k/p opioid receptor agonists the 6P-naltrexamines. J Med Chem 52 1546-1552... 

Spetea M, Toth F, Schiitz J, Otvos F, Toth G, Benyhe S, Borsodi A, Schmidhammer H (2003) Binding characteristics of [3H] 14-methoxymetopon, a high affinity p-opioid receptor agonist. Eur J Neurosci 18 290-295... 

Bileviciute-Ljungar I, Spetea M, Guo Y, Schiitz J, Windisch P, Schmidhammer H (2006) Peripherally mediated antinociception of the p-opioid receptor agonist 2-[(4, 5a-epoxy-3-hydroxy- l4 S-methoxy-17-methylmorphinan-6[l-yl)amino]acetic acid (HS-731) after subcutaneous and oral administration in rats with carrageenan-induced hindpaw inflammation. 

Although morphine is a classical p opioid receptor agonist, its intrinsic activity is known to be lower than that of a representative full p opioid receptor agonist, DAMGO. Moreover, recent reports showed that morphine was a partial agonist for the opioid p receptor in some pharmacological assays. See [34-38]. 

---