The effects of putative calmodulin antagonists on the binding of [3H]opioid ligands to rat brain membranes were examined. Chlorpromazine, trifluoperazine, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) and N2-dansyl-L-arginine-4-t-butylpiperidine amide (TI 233, No. 233) inhibited the binding of [3H] [D-Ala2, Met5]enkephalinamide ([3H]DALAMID) in a dose-dependent manner, and this inhib...

BACKGROUND The clinical treatment of various types of pain relies upon the use of opioid analgesics. However most of them produce, in addition to the analgesic effect, several side effects such as the development of dependence and addiction as well as sedation, dysphoria, and constipation. One solution to these problems are chimeric compounds in which the opioid pharmacophore is hybridized with...

Mitragynine (1) is a major alkaloidal component in the Thai traditional medicinal herb, Mitragyna speciosa, and has been proven to exhibit analgesic activity mediated by opioid receptors. By utilizing this natural product as a lead compound, synthesis of some derivatives, evaluations of the structure-activity relationship, and surveys of the intrinsic activities and potencies on opioid receptor...

Much evidence points to the involvement of N-methyl-D-aspartate (NMDA) receptors in the development and maintainance of neuropathic pain. In neuropathic pain, there is generally involved a presumed opioid-insensitive component, which apparently can be blocked by NMDA receptor antagonists. However, in order to obtain complete analgesia, a combination of an NMDA receptor antagonist and an opioid ...

N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines (2a,b) are opioid receptor antagonists where the antagonist properties are not due to the type of N-substituent. In order to gain a better understanding of the contribution that the 3- and 4-methyl groups make to the pure antagonist properties of 2a,b, we synthesized analogues of 2a,b that lacked the 4-methyl (5a,b), 3-methyl (6a,b...

Previous research has shown that compounds with mixed and activity may have utility for the treatment of cocaine abuse and dependence. The present study characterizes the pharmacological profile of a bivalent morphinan that was shown to be a opioid receptor agonist and a opioid receptor agonist/antagonist. MCL-145 [bis(N-cyclobutylmethylmorphinan) fumarate] is related to the morphinan cyclorpha...

In this study, the activity of the d-opioid receptor subtypeselective agonist, SB 227122, was investigated in a guinea pig model of citric acid-induced cough. Parenteral administration of selective agonists of the d-opioid receptor (SB 227122), m-opioid receptor (codeine and hydrocodone), and k-opioid receptor (BRL 52974) produced dose-related inhibition of citric acid-induced cough with ED50 v...

27 * Department of Pharmacology, School of Pharmacy, Marmara University, T›bbiye Cad. No: 49 Haydarpafla, 81010 Istanbul, Turkey ° Corresponding author Opioid Control of Renal Excretion of Water and Sodium Summary : The kidneys act to regulate total body water and sodium via numerous neural and humoral mechanisms, including pathways that involve the renal sympathetic nerves, antidiuretic hormon...