objectives: crocin, a constituent of saffron and yellow gardenia, possesses anti-nociceptive effects. in the present study, we investigated the effects of intra-fourth ventricle injection of crocin in a rat model of orofacial pain. the contribution of opioid system was assessed using intra-fourth ventricle injection of naloxone, an opioid receptor antagonist. materials and methods: a guide cann...

Background and Purpose The μ-opioid receptor (μ receptor) is the primary target for opioid analgesics. 7-transmembrane (TM) 6TM μ isoforms mediate inhibitory excitatory cellular effects. Here, we developed compounds selective 6TM- or 7TM-μ receptors to further our understanding of pharmacodynamic properties receptors. Experimental Approach We performed virtual screening ZINC Drug Now library us...

Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds (I-IV) along with eleven known compounds (V-XV). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (-49.7 and -53.8% displacement, resp.). Compound ...

The -opioid antagonist naltrindole has been shown to inhibit graft rejection in vivo and suppress allogeneic mixed lymphocyte reaction (MLR) in vitro, similarly to cyclosporin A. We investigated whether this action is mediated by -opioid receptors using both genetic and pharmacological tools. Naltrindole and two related compounds, 7-benzylidene-7-dehydronaltrexone and naltriben, inhibited MLR p...

Two 14beta-p-nitrocinnamoyl derivatives of dihydrocodeinone, 14beta-(p-nitrocinnamoylamino)-7,8-dihydrocodeinone (CACO) and N-cyclopropylmethylnor-14beta-(p-nitrocinnamoylamino)- 7, 8-dihydrocodeinone (N-CPM-CACO), and the corresponding chlorocinnamoylamino analogs, 14beta-(p-chlorocinnamoylamino)-7, 8-dihydrocodeinone (CAM) and N-cyclopropylmethylnor-14beta-(p-chlorocinnamoylamino) -7, 8-dihyd...

Opioid receptors have been demonstrated on sensory nerves in both inflamed and normal subcutaneous tissue but locally applied opioid agonists produce analgesia in inflamed tissue only. Inflammation confers a disruption of the perineurial barrier that can also be induced deliberately by hyperosmolar solutions. The present study examines at which stage of Freund's adjuvant-induced inflammation pe...

The development of new drugs to combat neuroinflammation is highly relevant as it opens up possibilities for the treatment a wide range diseases, including Alzheimer’s disease, Parkinson’s epilepsy, schizophrenia, depression, and others. Kappa-opioid agonists represent promising class compounds with а high potential be used in neurological conditions accompanied by neuroinflammation. aim study ...

To obtain benzomorphans with a longer duration of action that may be potential therapeutics for treating cocaine abuse, 8-carboxamidocyclazocine was synthesized. The pharmacological properties of 8-carboxamidocyclazocine were compared with the parent compound cyclazocine. Changing the 8-hydroxyl group on cyclazocine to an 8-carboxamido group resulted in only a 2-fold decrease in the affinity of...

introduction in spite of the increasing trend in opioid abusers worldwide, the prevalence of narcotic bowel syndrome (nbs) is undetermined. we aimed to estimate the prevalence of nbs and other opioid bowel dysfunction (obd) in opioid abusers in kerman, southeast iran. according to the best of our knowledge, this is the first study to assess the prevalence of nbs in opioid abusers. method by ref...

Novel semisynthetic analogs of salvinorin A, a full agonist having extraordinary affinity as well as selectivity for the κ-opioid receptor (KOR), were obtained in good yields. The derivatives are remarkable for their unusual and unique hemiacetal structure in the salvinorin series of compounds. The formation of the hemiacetal occurs with epimerization at C-12, thus preserving the original confi...