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Opioid receptor subtypes: fact or artifact?
Citation
Dietis, ND and Rowbotham, DJ and Lambert, DG, Opioid receptor subtypes: fact or artifact?, British Journal of Anaesthesia, 107, (1) pp. 8-18. ISSN 0007-0912 (2011) [Substantial Review]
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Abstract
Summary. There is a vast amount of pharmacological evidence favouring the existence of
multiple subtypes of opioid receptors. In addition to the primary classification of m (mu:
MOP), d (delta: DOP), k (kappa: KOP) receptors, and the nociceptin/orphanin FQ peptide
receptor (NOP), various groups have further classified the pharmacological m into m1–3,
the d into d1–2/dcomplexed/non-complexed, and the k into k1–3. From an anaesthetic
perspective, the suggestions that m1 produced analgesia and m2 produced respiratory
depression are particularly important. However, subsequent to the formal identification
of the primary opioid receptors (MOP/DOP/KOP/NOP) by cloning and the use of this
information to produce knockout animals, evidence for these additional subtypes is
lacking. Indeed, knockout of a single gene (and hence receptor) results in a loss of all
function associated with that receptor. In the case of MOP knockout, analgesia and
respiratory depression is lost. This suggests that further sub-classification of the primary
types is unwise. So how can the wealth of pharmacological data be reconciled with new
molecular information? In addition to some simple misclassification (k3 is probably NOP),
there are several possibilities which include: (i) alternate splicing of a common gene
product, (ii) receptor dimerization, (iii) interaction of a common gene product with other
receptors/signalling molecules, or (iv) a combination of (i)–(iii). Assigning variations in
ligand activity (pharmacological subtypes) to one or more of these molecular
suggestions represents an interesting challenge for future opioid research.
Item Details
| Item Type: | Substantial Review |
|---|---|
| Keywords: | opioid receptor subtypes |
| Research Division: | Biomedical and Clinical Sciences |
| Research Group: | Pharmacology and pharmaceutical sciences |
| Research Field: | Basic pharmacology |
| Objective Division: | Manufacturing |
| Objective Group: | Human pharmaceutical products |
| Objective Field: | Human pharmaceutical products not elsewhere classified |
| UTAS Author: | Dietis, ND (Dr Nikolas Dietis) |
| ID Code: | 80396 |
| Year Published: | 2011 |
| Web of Science® Times Cited: | 93 |
| Deposited By: | Pharmacy |
| Deposited On: | 2012-10-31 |
| Last Modified: | 2015-05-15 |
| Downloads: | 0 |
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