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PZM21
PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is claimed to be a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potency and efficacy similar to morphine, but with less β-arrestin 2 recruitment. However, recent reports highlight that this might be due to its low intrinsic efficacy, rather than functional selectivity or 'G protein bias' as initially reported. In tests on mice, PZM21 was slightly less potent than morphine or TRV130 as an analgesic, but also had significantly reduced adverse effects, with less constipation than morphine, and very little respiratory depression, even at high doses. This research was described as a compelling example of how modern high-throughput screening techniques can be used to discover new chemotypes with specific activity profiles, even at targets such as the μ-opioid receptor which have already been thoroughly investiga ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SR-17018
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 2 recruitment. In animal studies it produces analgesic effects but with less respiratory depression and development of tolerance than conventional opioids. See also * Bezitramide * Brorphine * J-113,397 * Oliceridine * PZM21 * SR-16435 * SHR9352 * TRV734 TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine Oliceridine ... References {{pharm-stub Mu-opioid receptor agonists Chloroarenes Ureas Piperidines Benzimidazoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TRV734
TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine and has a similar pharmacological profile, but unlike oliceridine which has to be injected, TRV734 is suitable to be administered orally. See also * PZM21 * SHR9352 * SR-17018 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 2 recruitment. In animal studies it produces analgesic effects but with less respiratory de ... References {{pharm-stub Mu-opioid receptor agonists Pyridines Fluoroarenes Spiro compounds Oxygen heterocycles Amines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SHR9352
SHR9352 is a drug which acts as a potent and selective biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It was structurally derived from oliceridine by replacing the benzylic side chain with a cyclised group, although only some compounds in the series retained the desired biased agonist profile, with some derivatives such as compound 12 being potent, unbiased μ-opioid full agonists. ] See also * PZM21 * SR-17018 * TRV734 TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine Oliceridine ... References External links * Mu-opioid receptor agonists Dithiolanes 2-Pyridyl compounds Spiro compounds {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AT-121
AT-121 is an experimental analgesic. It was designed to be bifunctional, acting as an agonist at both the μ-opioid receptor and the nociceptin receptor. The interaction with the nociceptin receptor is expected to block the abuse and dependence-related side effects that are typical of opioids. A study in nonhuman primates found that AT-121 has morphine-like analgesic effects, but suppressed the addictive effects. See also * AT-076 * Cebranopadol * Oliceridine * PZM21 PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is claimed to be a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potenc ... References Mu-opioid receptor agonists Nociceptin receptor agonists Sulfamides 4-Phenylpiperidines Experimental drugs Tetrahydroisoquinolines {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Constipation
Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the bowel movement. Complications from constipation may include hemorrhoids, anal fissure or fecal impaction. The normal frequency of bowel movements in adults is between three per day and three per week. Babies often have three to four bowel movements per day while young children typically have two to three per day. Constipation has many causes. Common causes include slow movement of stool within the colon, irritable bowel syndrome, and pelvic floor disorders. Underlying associated diseases include hypothyroidism, diabetes, Parkinson's disease, celiac disease, non-celiac gluten sensitivity, colon cancer, diverticulitis, and inflammatory bowel disease. Medications associated with constipation include opioids, certain antacids, calcium channel blockers, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biased Ligands
Bias is an inclination toward something, or a predisposition, partiality, prejudice, preference, or predilection. Bias may also refer to: Scientific method and statistics * The bias introduced into an experiment through a confounder * Algorithmic bias, machine learning algorithms that exhibit politically unacceptable behavior * Cultural bias, interpreting and judging phenomena in terms particular to one's own culture * Funding bias, bias relative to the commercial interests of a study's financial sponsor * Infrastructure bias, the influence of existing social or scientific infrastructure on scientific observations * Publication bias, bias toward publication of certain experimental results * Bias (statistics), the systematic distortion of a statistic ** Biased sample, a sample falsely taken to be typical of a population ** Estimator bias, a bias from an estimator whose expectation differs from the true value of the parameter * Personal equation, a concept in 19th- and early ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AT-076
AT-076 is a so-called opioid "pan" antagonist and is the first reasonably balanced antagonist known of all four opioid receptor types. It acts as a silent antagonist of all four of the opioid receptors, behaving as a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM) and as a noncompetitive 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 JDTic via removal of the 3,4-dimethyl group of the ''trans''-(3''R'',4''R'')-dimethyl-4-(3-hydroxyphenyl)piperidine antagonist scaffold, which increased affinity for the nociceptin receptor by 10-fold and for the μ- and δ-opioid receptors by 3-6-fold. See also * AT-121 * Cebranopadol * Buprenorphine * BU09059 BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR). It was derived from the irreversible (long-acting) KOR ant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DPI-3290
DPI-3290 was discovered by scientists at Burroughs Wellcome and licensed to Delta Pharmaceutical and is a drug that is used in scientific research. It is a potent analgesic drug, which produces little respiratory depression. DPI-3290 acts as an agonist at both μ- and δ-opioid receptor, with an IC50 of 6.2nM at μ and 1.0nM at δ. See also * BW373U86 * DPI-221 * DPI-287 DPI-287 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant Antidepressants are a class ... References {{Piperazines Synthetic opioids Delta-opioid receptor agonists Piperazines Benzanilides Phenols Fluoroarenes Allyl compounds Mu-opioid receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cebranopadol
Cebranopadol (developmental code GRT-6005) is an opioid analgesic of the benzenoid class which is currently under development internationally by Grünenthal, a Germany, German pharmaceutical company, and its partner Depomed, a pharmaceutical company in the United States, for the treatment of a variety of different acute and chronic pain, chronic pain, pain states. As of November 2014, it is in Phase III clinical trials, phase III clinical trials. Cebranopadol is unique in its mechanism 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 = 1.2 nM; IA = 104%), and δ-opioid receptor (Ki = 18 nM; EC50 = 110 nM; IA = 105%), and as a partial agonist of the nociceptin receptor (Ki = 0.9 nM; EC50, EC50 = 13.0 nM; = 89%) and κ-opioid receptor (Ki = 2.6 nM; EC50 = 17 nM; IA = 67%). The Effective dose (pharmacology), EC50 values of 0.5–5.6  ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
