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...
49 KB (4,880 words) - 05:38, 11 November 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) - 14:34, 24 July 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 (2,052 words) - 19:07, 10 December 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 (19,663 words) - 09:17, 17 November 2024
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...
68 KB (7,816 words) - 22:20, 21 September 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
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 (3,255 words) - 07:58, 11 September 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 (3,581 words) - 07:36, 21 December 2024
decreased occupancy of the μ-opioid receptor (MOR), thus producing signs and symptoms of morphine withdrawal. Neonatal withdrawal Opioid-induced hyperalgesia...
33 KB (3,485 words) - 03:20, 1 December 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...
71 KB (6,477 words) - 15:37, 13 December 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...
23 KB (1,620 words) - 22:35, 30 October 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) - 04:54, 15 December 2024
Tapentadol (category Mu-opioid receptor agonists)
a synthetic opioid analgesic of the benzenoid class with a dual mode of action as a highly selective full agonist of the μ-opioid receptor and as a norepinephrine...
48 KB (4,584 words) - 22:27, 9 December 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...
108 KB (10,589 words) - 16:30, 14 December 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) - 03:21, 4 September 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 (3,363 words) - 12:06, 2 November 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 (13,432 words) - 06:24, 11 September 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...
125 KB (11,614 words) - 08:10, 12 December 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 (565 words) - 18:15, 21 September 2024
Alazocine (category Delta-opioid receptor agonists)
the μ-opioid receptor (Ki = 1.15 nM for (±)-alazocine against the mouse receptor transfected in HEK293 cells). It is also an agonist of the δ-opioid receptor...
13 KB (1,247 words) - 18:36, 21 October 2024
Endomorphin (category Mu-opioid receptor agonists)
high specificity and affinity for the μ-opioid receptor, binding it exclusively and strongly. Bound μ-opioid receptors typically induce inhibitory effects...
13 KB (1,118 words) - 23:01, 29 May 2024
Dezocine (category Kappa-opioid receptor antagonists)
an opioid receptor modulator, acting as a partial agonist of the μ- and κ-opioid receptors. It is a biased agonist of the μ-opioid receptor. The drug...
25 KB (2,497 words) - 04:33, 24 November 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) - 15:39, 17 September 2024
Buprenorphine (category Delta-opioid receptor antagonists)
Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of opioid receptor, it may be an agonist, partial agonist...
83 KB (7,714 words) - 23:28, 9 December 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
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...
174 KB (16,245 words) - 23:32, 22 December 2024
Alvimopan (category Mu-opioid receptor antagonists)
peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central...
9 KB (782 words) - 15:58, 21 October 2024
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 (2,213 words) - 20:09, 28 September 2024