The blood-brain barrier (BBB) permeability to morphine and morphine-6-glucuronide (M6G) is measured under identical conditions using an intravenous injection method in the rat and HPLC separation of morphine from its metabolites. The brain uptake of M6G expressed as %ID/g was 32-fold lower than that of morphine, and the BBB permeability surface area product (PS) of M6G was 57-fold lower as comp...

  There are several reports on the therapeutic effects of TFG in Iranian traditional medical literature such as antinociceptive, antipyretic, and anti-inflammatory, antidiabetic and antidiuretic effects. The anti-inflammatory and anti-pyretic effects of TFG have been confirmed in experimental models. In the present study, the antinociceptive effect of TFG extract in formalin and tail flick test...

Morphine, Naloxone, Formalin Test,

INTRODUCTION Morphine is a potent analgesic but its continual use results in analgesic tolerance. Mechanisms of this tolerance remain to be clarified. However, changes in the functions of μ-opioid and N-Methyl-D-aspartate (NMDA) receptors have been proposed in morphine tolerance. We examined changes in gene expression of the NMDA receptor subunit 1 (NR1) at mRNA levels in rat striatum and prefr...

Tolerance to the analgesic effect of morphine is a major clinical problem which can be managed by co-administration of another drug. This study investigated the ability of propranolol to potentiate the antinociceptive action of morphine and the possible mechanisms underlying this effect. Antinociception was assessed in three nociceptive tests (thermal, hot plate), (visceral, acetic acid), and (...

introduction: orexin-a and b (hypocretin 1 and 2) are neuropeptides that are mostly expressed in the posterior and lateral hypothalamus (lh). intracisternal (icv) and intratechal (it) injections of orexin-a (hypocretin-1) have been shown to elicit analgesic responses in formalin test. however, the locations of central sites that may mediate these effects have not been clearly elucidated. orexin...

Sustained-release oral morphine sulphate (MST) 20 mg was administered to 11 healthy volunteers. Mean peak plasma morphine concentration was 14.8 ng ml-1, and occurred at a mean time of 142.5 min after ingestion. Analgesia assessed by an ischaemic forearm pain test increased to a maximum approximately 40 min after the calculated peak plasma concentration of morphine had been achieved, and remain...

Spinal intrathecal injections of the nonsteroidal antiinflammatory analgesics (NSAIAs) indomethacin and acetylsalicylic acid, which inhibit prostaglandin synthesis, cause dose-dependent hypoalgesia in the rat. Intrathecal injections of prostaglandin-E2 (PGE2) produce dose-dependent hyperalgesia. To determine whether this action of prostaglandins on the central nervous system is mediated through...

OBJECTIVE(S) There are many reports about the role of rostral ventromedial medulla (RVM) in modulating stress-induced analgesia (SIA). In the previous study we demonstrated that temporal inactivation of RVM by lidocaine potentiated stress-induced analgesia. In this study, we investigated the effect of permanent lesion of the RVM on SIA by using formalin test as a model of acute inflammatory pai...

The cannabinoid 1 receptor and cannabinoid 2 receptor can both be targeted in the treatment of pain; yet, they have some important differences. Cannabinoid 1 receptor is expressed at high levels in the central nervous system, whereas cannabinoid 2 receptor is found predominantly, although not exclusively, outside the central nervous system. The objective of this study was to investigate potenti...