title: The imidazoline receptors and ligands in pain modulation.
abstract: Pain is an unpleasant experience and effects daily routine negatively. Although there are various drugs, many of them are not entirely successful in relieving pain, since pain modulation is a complex process involving numerous mediators and receptors. Therefore, it is a rational approach to identify the factors involved in the complex process and develop new agents that act on these pain producing mechanisms. In this respect, the involvement of the imidazoline receptors in pain modulation has drawn attention in recent years. In this review, it is aimed to focus on the imidazoline receptors and their ligands which contribute to the pain modulation. It is demonstrated that imidazoline-2 (I2) receptors are steady new drug targets for analgesics. Even if the mechanism of I2 receptor is not well known in the modulation of pain, it is known that it plays a role in tonic and chronic pain but not in acute phasic pain. Moreover, the I2 receptor ligands increase the analgesic effects of opioids in both acute and chronic pain and prevent the development of opioid tolerance. So, they are valuable for the chronic pain treatment and also therapeutic coadjuvants in the management of chronic pain with opiate drugs due to the attenuation of opioid tolerance and addiction. Thus, the use of the ligands which bind to the imidazoline receptors is an effective strategy for relieving pain. This educational forum exhibits the role of imidazoline receptors and ligands in pain process by utilizing experimental studies.
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey.
authors.forename: Nurcan
authors.initials: N
authors.lastname: Bektas
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey.
authors.forename: Dilara
authors.initials: D
authors.lastname: Nemutlu
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey.
authors.forename: Rana
authors.initials: R
authors.lastname: Arslan
mesh_terms: D059787:Acute Pain / Q000188:drug therapy* / Q000503:physiopathology; D000700:Analgesics / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D059350:Chronic Pain / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D054755:Imidazoline Receptors / Q000378:metabolism*; D008024:Ligands; D058990:Molecular Targeted Therapy
chemical_list: D000700:Analgesics; D000701:Analgesics, Opioid; D054755:Imidazoline Receptors; D008024:Ligands; C487767:imidazoline receptor 2
keywords: Acute pain; chronic pain; imidazoline receptor ligands; imidazoline receptors