Biological studies were conducted on (3R)-7-Hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinoline-carboxamide (JDTic), the first potent kappa-selective opioid receptor antagonist not derived from an opiate class of compounds. In the mouse tail-flick test, JDTic, administered subcutaneously (s.c.), blocked anticocicep...

Research of the cannabinoid system has many similarities with that of the opioid system. In both instances, studies into drug-producing plants led to the discovery of an endogenous control system with a central role in neurobiology. Few compounds have had as much positive press from patients as those of the cannabinoid system. While these claims are investigated in disorders such as multiple sc...

while for a long time it has been perceived that neonates and young children do not perceive pain as the adult, this notion had to be corrected on the basis of neurophysiological data and the ontogenisis of the nociceptive system. also, it has been demonstrated conclusively that neonates and the young infant perceive pain at a much lower nociceptive input which is largely due to a still immatur...

C describe the concept of multimodal analgesia and give examples Abstract Opium is the natural substance to which modern narcotics owe their existence. First discovered in the 1500s, opium was the most potent analgesic compound in use, held in high regard, hence its Latin name laudanum (to praise). Subsequent studies into the effects of opium led to the discovery of the opioid receptors, and th...

Temporal lobe epilepsy is considered to be one of the most common and severe forms of focal epilepsies. Patients often develop cognitive deficits and emotional blunting along the progression of the disease. The high incidence of resistance to antiepileptic drugs and a frequent lack of admissibility to surgery poses an unmet medical challenge. In the urgent quest of novel treatment strategies, n...

A novel series of 1-(pyrrolidin-1-ylmethyl)-2-[(3-oxo-indan)-formyl]-1,2,3,4-tetrahydroisoquinoline derivatives maj-3a-maj-3u were synthesized and evaluated in vitro for their binding affinity at κ-opioid receptors. Maj-3c displayed the highest affinity for κ-opioid receptors (Ki = 0.033 nM) among all the compounds evaluated. Furthermore, all four stereoisomers of compound 3c were prepared, and...

BACKGROUND AND PURPOSE Opiates remain the most effective compounds for alleviating severe pain across a wide range of conditions. However, their use is associated with significant side effects. Neuropeptide FF (NPFF) receptors have been implicated in several opiate-induced neuroadaptive changes including the development of tolerance. In this study, we investigated the consequences of NPFF recep...

OBJECTIVE The iboga alkaloids are a class of small molecules defined structurally on the basis of a common ibogamine skeleton, some of which modify opioid withdrawal and drug self-administration in humans and preclinical models. These compounds may represent an innovative approach to neurobiological investigation and development of addiction pharmacotherapy. In particular, the use of the protot...

Although non-steroidal anti-inflammatory drugs (NSAIDs) and opioid compounds are widely used in the releif of pain, they are not always useful due to their side effects. It seems necessary to search for newer analgesic compounds. Therefore, we decided to study the analgesic effects of this plant. For extraction, percolation method was used and different weights of dried extract were dissolved i...

centuries, both in amedicinal and ‘recreational’ manner. Indeed, findings of fossilized opium poppy seeds dating as far back as 30 000 yr ago suggest the use of opium by Neanderthal man. In 1799, Friedrich Serturner discovered the major active ingredient of opium, which he named morphine and opioid pharmacology was born. Morphine and its derivates are used today for the treatment of acute and c...