The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins...
22 KB (2,424 words) - 08:47, 18 May 2024
to be the μ opioid receptor, using 3H-naloxone. That study has been widely credited as the first definitive finding of an opioid receptor, although two...
40 KB (4,427 words) - 12:37, 12 January 2024
suggested however that the pain modulated by the μ-opioid receptor and that modulated by the δ-opioid receptor are distinct types, with the assertion that...
28 KB (3,262 words) - 06:56, 10 July 2024
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone...
11 KB (1,340 words) - 03:04, 25 May 2024
relief. As a class of substances, they act on opioid receptors to produce morphine-like effects. The terms 'opioid' and 'opiate' are sometimes used interchangeably...
222 KB (19,665 words) - 02:48, 7 July 2024
Opioid peptides or opiate peptides are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides. Such...
19 KB (1,419 words) - 18:28, 15 March 2024
Carfentanil (category Mu-opioid receptor agonists)
analogue of the synthetic opioid analgesic fentanyl. It acts as an ultrapotent and highly selective agonist of the μ-opioid receptor. Carfentanil was first...
22 KB (2,039 words) - 06:04, 14 July 2024
Peripherally acting μ-opioid receptor antagonists (PAMORAs) are a class of chemical compounds that are used to reverse adverse effects caused by opioids interacting...
30 KB (3,278 words) - 14:56, 26 October 2023
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that in humans is encoded...
67 KB (7,675 words) - 03:40, 2 May 2024
Antipruritic (section μ-Opioid receptor antagonists)
are therefore associated with fewer side effects in usual doses. μ-opioid receptor antagonists are usually well-tolerated and have no abuse potential...
37 KB (3,582 words) - 18:50, 6 February 2024
(~60%) with the ‘classical’ opioid receptors μ-OP (MOP), κ-OP (KOP), and δ-OP (DOP), it possesses little or no affinity for opioid peptides or morphine-like...
28 KB (3,339 words) - 08:49, 10 June 2024
Tianeptine (category Mu-opioid receptor agonists)
act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. This may explain part of its antidepressant...
70 KB (6,369 words) - 04:33, 15 July 2024
Agonist (redirect from Receptor agonist)
affecting the same signal transduction pathway. Oliceridine is a μ-opioid receptor agonist that has been described to be functionally selective towards...
14 KB (1,622 words) - 00:36, 7 July 2024
Oxycodone (category Mu-opioid receptor agonists)
appears relatively safe. Opioid withdrawal may occur if rapidly stopped. Oxycodone acts by activating the μ-opioid receptor. When taken by mouth, it has...
124 KB (11,461 words) - 00:27, 7 July 2024
Buprenorphine (category Delta-opioid receptor antagonists)
preferential μ-opioid receptor antagonist), appears useful for treatment-resistant depression. In combination with samidorphan or naltrexone (μ-opioid receptor antagonists)...
80 KB (7,311 words) - 17:06, 31 May 2024
Lofentanil (category Mu-opioid receptor agonists)
development of tolerance triggered by receptor over-activation could be rapid. In addition to acting on the μ-opioid receptor, lofentanil has also been found...
8 KB (745 words) - 18:48, 23 May 2024
Cebranopadol (category Kappa-opioid receptor agonists)
of action as an opioid, binding to and activating all four of the opioid receptors; it acts as a full agonist of the μ-opioid receptor (Ki = 0.7 nM; EC50...
7 KB (564 words) - 21:35, 26 April 2024
Depressant (section Opioids/opiates)
exogenous opioids.[citation needed] The μ-opioid receptor is responsible for the analgesic, euphoric, and adverse effects of opioids. The μ-opioid receptor is...
130 KB (13,447 words) - 18:34, 12 July 2024
14-Methoxymetopon (category Mu-opioid receptor agonists)
morphine. It binds strongly to the μ-opioid receptor and activates it to a greater extent than most similar opioid drugs. This produces an unusual pharmacological...
4 KB (302 words) - 13:12, 5 June 2024
Fentanyl (category Mu-opioid receptor agonists)
relatively small quantity can cause overdose. Fentanyl works by activating μ-opioid receptors. Fentanyl is sold under the brand names Actiq, Duragesic and Sublimaze...
173 KB (15,974 words) - 17:12, 19 July 2024
Naltrexone (category Delta-opioid receptor antagonists)
opioid receptors. Naltrexone is specifically an antagonist preferentially of the μ-opioid receptor (MOR), to a lesser extent of the κ-opioid receptor...
107 KB (10,529 words) - 21:40, 17 July 2024
active μ-opioid receptor agonist and a peripherally selective μ-, κ-, and δ-opioid receptor antagonist. Cebranopadol (GRT-6005) – non-selective μ-opioid receptor...
18 KB (1,274 words) - 09:53, 9 January 2024
SR-17018 (category Mu-opioid receptor agonists)
SR-17018 is a drug which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin...
4 KB (301 words) - 14:46, 20 November 2023
Aticaprant (category Kappa-opioid receptor antagonists)
target of the endogenous opioid peptide dynorphin. The medication has decent selectivity for the KOR over the μ-opioid receptor (MOR) and other targets...
24 KB (2,211 words) - 00:08, 10 March 2024
Vitro Functional Profiling of Fentanyl and Nitazene Analogs at the μ-Opioid Receptor Reveals High Efficacy for Gi Protein Signaling". ACS Chemical Neuroscience...
27 KB (1,871 words) - 04:28, 22 July 2024
Mitragyna speciosa (category Opioids)
μ-opioid receptor. While most data indicates agonism at all three opioid receptors, other data suggests the alkaloids are antagonists of the δ-opioid...
83 KB (8,924 words) - 15:07, 12 July 2024
either an opioid agonist or antagonist. An example of an opioid modulator is buprenorphine, which is a partial agonist of the μ-opioid receptor and an antagonist...
1,022 bytes (101 words) - 11:00, 17 April 2023
Research thus far has primarily implicated the μ-opioid receptors (MOR) abnormal activation of NMDA receptors in the central nervous system, and long-term...
28 KB (3,511 words) - 15:34, 10 April 2024
Dezocine (category Kappa-opioid receptor antagonists)
opioid receptor modulator, acting as a partial agonist of the μ- and κ-opioid receptors. It has a similar profile of effects to related opioids acting...
19 KB (1,803 words) - 07:04, 5 January 2024
Herkinorin (category Kappa-opioid receptor agonists)
a selective κ-opioid receptor agonist with no significant μ-opioid receptor affinity, herkinorin is predominantly a μ-opioid receptor agonist. Compared...
7 KB (662 words) - 00:40, 18 February 2024