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
agonist action at the κ-opioid receptor. As they induce opioid withdrawal effects in people who are taking, or have recently used, opioid full agonists, these...
11 KB (1,340 words) - 14:34, 24 July 2024
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins...
40 KB (4,427 words) - 12:37, 12 January 2024
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 (4,885 words) - 11:31, 6 October 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
Agonist-antagonist (redirect from Agonist–antagonist opioid)
at κ-opioid receptor and antagonist activity at the delta opioid receptor (δ) nalbuphine, κ-agonist/μ-antagonist analgesic Agonist–antagonist opioids usually...
7 KB (715 words) - 18:05, 18 February 2024
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein...
28 KB (3,262 words) - 06:56, 10 July 2024
Aticaprant (category Kappa-opioid receptor antagonists)
developmental codes JNJ-67953964, CERC-501, and LY-2456302, is a κ-opioid receptor (KOR) antagonist which is under development for the treatment of major...
24 KB (2,213 words) - 20:09, 28 September 2024
ISSN 0040-4020. Santino, Federica; Gentilucci, Luca (January 2023). "Design of κ-Opioid Receptor Agonists for the Development of Potential Treatments of Pain with...
13 KB (1,218 words) - 05:12, 3 April 2024
Salvinorin B methoxymethyl ether (category Kappa-opioid receptor agonists)
Structures bound to the κ-opioid receptor have also been reported. Salvinorin B methoxymethyl ether has a Ki of 0.60 nM at the κ opioid receptor, and is around...
6 KB (535 words) - 20:27, 22 January 2024
Carfentanil (category Mu-opioid receptor agonists)
values (Ki) of 0.051 nM for the μ-opioid receptor, 4.7 nM for the δ-opioid receptor, and 13 nM for the κ-opioid receptor in rat brain. Thus, carfentanil...
22 KB (2,039 words) - 06:04, 14 July 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 (19,664 words) - 01:55, 11 October 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 (3,378 words) - 13:44, 13 August 2024
JDTic (category Delta-opioid receptor antagonists)
JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related...
14 KB (1,468 words) - 21:09, 22 January 2024
Oxycodone (category Mu-opioid receptor agonists)
β-endorphin. Oxycodone has low affinity for the δ-opioid receptor (DOR) and the κ-opioid receptor (KOR), where it is an agonist similarly. After oxycodone...
124 KB (11,480 words) - 12:18, 24 September 2024
Buprenorphine/samidorphan (category Delta-opioid receptor antagonists)
μ-opioid receptor (MOR), antagonist/very weak partial agonist of the κ-opioid receptor (KOR), and, to a lesser extent, antagonist of the δ-opioid receptor...
20 KB (1,992 words) - 02:21, 5 November 2023
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
Nalorphine (category Kappa-opioid receptor agonists)
Nalorphine acts at two opioid receptors — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM;...
8 KB (506 words) - 22:26, 2 December 2023
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) - 01:37, 2 October 2024
14-Methoxymetopon (category Mu-opioid receptor agonists)
respiratory depression which is believed to involve interaction with the κ-opioid receptor 14-Methoxydihydromorphinone US 5886001, "Agonist compounds" . King...
4 KB (302 words) - 13:12, 5 June 2024
Noribogaine (category Delta-opioid receptor antagonists)
Noribogaine has been determined to act as a biased agonist of the κ-opioid receptor (KOR). It activates the G protein (GDP-GTP exchange) signaling pathway...
9 KB (796 words) - 03:37, 8 September 2024
Chronic pain Disease Some drugs can produce dysphoria, including κ-opioid receptor agonists like salvinorin A (the active constituent of the hallucinogenic...
8 KB (759 words) - 14:07, 10 August 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 (7,718 words) - 04:06, 30 September 2024
RB-64 (category Kappa-opioid receptor agonists)
agonist, with a reactive thiocyanate group that forms a bond to the κ-opioid receptor (KOR), resulting in very high potency. It is functionally selective...
4 KB (252 words) - 11:34, 23 September 2024
Cebranopadol (category Kappa-opioid receptor agonists)
= 0.9 nM; EC50 = 13.0 nM; IATooltip intrinsic activity = 89%) and κ-opioid receptor (Ki = 2.6 nM; EC50 = 17 nM; IA = 67%). The EC50 values of 0.5–5.6 μg/kg...
7 KB (565 words) - 18:15, 21 September 2024
Norbuprenorphine (category Kappa-opioid receptor agonists)
metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist...
4 KB (212 words) - 16:52, 28 April 2024
Tifluadom (category Kappa-opioid receptor agonists)
tifluadom has no activity at the GABAA receptor, but instead is a selective agonist for the κ-opioid receptor. It has potent analgesic and diuretic effects...
5 KB (383 words) - 14:11, 5 September 2024
Levomethorphan (category Delta-opioid receptor agonists)
potent agonist of all three of the opioid receptors, μ, κ (κ1 and κ3 but notably not κ2), and δ, as an NMDA receptor antagonist, and as a serotonin-norepinephrine...
8 KB (486 words) - 10:26, 24 April 2024
AT-076 (category Delta-opioid receptor antagonists)
antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM). AT-076 was derived from the selective κ-opioid receptor antagonist...
3 KB (182 words) - 08:47, 2 May 2023
Alazocine (category Delta-opioid receptor agonists)
partial agonist of the κ-opioid receptor (Ki = 0.4 nM, EC50 = 24 nM, and Emax = 66% for (±)-alazocine against the mouse receptor transfected in HEK293...
13 KB (1,247 words) - 14:53, 19 June 2024