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Katherine Johnson’s mathematical calculations helped guide some of America’s most important early space missions while she confronted the racial and gender barriers faced by Black women in twentieth-century America.
MORE →Reflects the personal views, recollections, and perspective of the author, Mike Davis.
This is a personal recollection on the Move fire on May 13, 1985
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| Trade names | Contralac, Liserdol |
| Other names | Methergoline; FI-6337; [(8β)-1,6-Dimethylergolin-8-yl)methyl]carbamic acid phenylmethyl ester |
| Routes of administration | Oral |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.037.881 |
| Chemical and physical data | |
| Formula | C25H29N3O2 |
| Molar mass | 403.526 g·mol−1 |
| 3D model (JSmol) | |
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  (what is this?) (verify) | |
Metergoline (INN, BAN), also known as methergoline and sold under the brand names Contralac (veterinary) and Liserdol (clinical), is a monoaminergic medication of the ergoline group which is used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) and to suppress lactation.[1][2][3]
Metergoline is a ligand of various serotonin and dopamine receptors.[4][5][6][7][8][9]
| Site | Affinity (Ki [nM]) | Efficacy (Emax [%]) | Action |
|---|---|---|---|
| 5-HT1A | 4.3 | ? | Antagonist |
| 5-HT1B | 5.2–36 | ? | Partial agonist |
| 5-HT1D | 0.60–11.7 | ? | Partial agonist |
| 5-HT1E | 776–1,122 | ? | ? |
| 5-HT1F | 339–341 | ? | ? |
| 5-HT2A | 0.12–2.3 | ? | Antagonist |
| 5-HT2B | 0.71–1.8 | ? | Antagonist |
| 5-HT2C | 0.18–1.8 | ? | Antagonist |
| 5-HT3 | >5,000–7,400 | ? | ? |
| 5-HT4 | 354 | ? | ? |
| 5-HT5A | 630 | ? | ? |
| 5-HT5B | 1,000 | ? | ? |
| 5-HT6 | 61–400 | ? | ? |
| 5-HT7 | 6.4–6.5 | ? | Antagonist |
| D2 | ? | ? | Agonist |
| Notes: All sites are human except 5-HT3 (rat/pig), 5-HT4 (pig), and 5-HT5B (rat—no human counterpart).[4] | |||
Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites
Source: Wikipedia. Article content is retrieved live through the MediaWiki API.
Metergoline (INNTooltip INN, BANTooltip British Approved Name), also known as methergoline and sold under the brand names Contralac (veterinary) and Liserdol (clinical), is a monoaminergic medication of the ergoline group which is used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) and to suppress lactation.
A serotonin 5-HT2A receptor antagonist, or simply 5-HT2A antagonist, is a drug which acts as an antagonist of the serotonin 5-HT2A receptor. Aside from simple competitive antagonists, these drugs may also be inverse agonists of the serotonin 5-HT2A receptor. They include non-selective agents like atypical antipsychotics, tricyclic antidepressants (TCAs), tetracyclic antidepressants (TeCAs), and serotonin antagonists and reuptake inhibitors (SARIs) as well as selective agents. Examples of non-selective serotonin 5-HT2A receptor antagonists include antipsychotics like chlorpromazine, clozapine, olanzapine, quetiapine, risperidone, spiperone (spiroperidol), and ziprasidone; antihistamines like cyproheptadine, hydroxyzine, and LY-2624803; TCAs like amitriptyline, clomipramine, doxepin, imipramine, iprindole, and trimipramine; TeCAs like mianserin, mirtazapine, and esmirtazapine; SARIs and related like trazodone, nefazodone, mepiprazole, niaprazine, and lubazodone; and others like adatanserin, cyclobenzaprine, deramciclane, DSP-6745, flibanserin, landipirdine, metergoline, metitepine (methiothepin), MT-1207, opiranserin, pizotifen, roluperidone, and XOB (ASR-6001). More selective serotonin 5-HT2A receptor antagonists include 4-PhPr-PEA, 4F-4PP, AMDA, altanserin, butanserin, cinanserin, eplivanserin, fananserin, glemanserin, iferanserin, ketanserin, lidanserin, LY03017, metrenperone, NH130, pelanserin, pimavanserin, pirenperone, pruvanserin, R-96544, R-102444, remlifanserin, ritanserin, seganserin, setoperone, SpAMDA, and volinanserin. Peripherally selective or acting serotonin 5-HT2A receptor antagonists are known as well and include BW-501C67, irindalone, naftidrofuryl, sarpogrelate, temanogrel, trelanserin, and xylamidine. Selective serotonin 5-HT2A receptor antagonists have been studied in the treatment of sleeping disorders such as insomnia, psychiatric disorders such as depression, anxiety, and schizophrenia, and for other indications. Several selective serotonin 5-HT2A receptor antagonists reached and/or completed phase 3 clinical trials, including and eplivanserin, pimavanserin, pruvanserin, and volinanserin. However, all of them except pimavanserin were discontinued, with pimavanserin having been approved only for the treatment of Parkinson's disease psychosis. Though not approved for insomnia, selective serotonin 5-HT2A receptor antagonists have been found to improve sleep and sleep quality, including increasing deep slow wave sleep (SWS) without affecting REM sleep. Serotonin 5-HT2A receptor antagonists are useful as so-called "trip killers" or hallucinogen antidotes in aborting or shortening the effects of serotonergic psychedelics like psilocybin, LSD, and mescaline. Ketanserin, risperidone, chlorpromazine, and cyproheptadine have all been formally studied and found to be effective for such purposes. Ketanserin, pimavanserin, and eplivanserin/volinanserin are under formal development and/or study for this use as well. In addition, recreational psychedelic users often use trip killers to abort psychedelic experiences, with frequent use of trazodone, quetiapine, olanzapine, and mirtazapine for these purposes having been documented.
Ketamine is a cyclohexanone-derived dissociative general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia, depression, and pain management. Ketamine exists as its two enantiomers, S- (esketamine) and R- (arketamine), and has antidepressant action likely involving NMDA antagonism as well as other mechanisms. At anesthetic doses, ketamine induces a state of dissociative anesthesia, a trance-like state providing pain relief, sedation, and amnesia. Its distinguishing features as an anesthetic are preserved breathing and airway reflexes, stimulated heart function with increased blood pressure, and moderate bronchodilation. As an anesthetic, it is used especially in trauma, emergency, and pediatric cases. At lower, sub-anesthetic doses, it is used as a treatment for pain and treatment-resistant depression. Ketamine is legally used in medicine but is also tightly controlled, as it is used as a recreational drug for its hallucinogenic and dissociative effects. When used recreationally, it is found both in crystalline, powder and liquid form, and is often referred to by users as "Ket", "Special K" or simply "K". The long-term effects of repeated use are largely unknown and are an area of active investigation. Liver and urinary toxicity have been reported among regular users of high doses of ketamine for recreational purposes. Ketamine can cause dissociation and nausea, and other adverse effects, and is contraindicated in severe heart or liver disease, and uncontrolled psychosis. Ketamine's clinical and antidepressant effects can be influenced by co-administration of other drugs, though these interactions are variable and not yet fully understood. Ketamine was first synthesized in 1962; it was derived from phencyclidine in pursuit of a safer anesthetic with fewer hallucinogenic effects. It was approved for use in the United States in 1970. It has been regularly used in veterinary medicine and was extensively used for surgical anesthesia in the Vietnam War. It later gained prominence for its rapid antidepressant effects discovered in 2000, marking a major breakthrough in depression treatment. Racemic ketamine, especially at higher doses, may be more effective and longer-lasting than esketamine in reducing depression severity. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication.
Quetiapine ( kwi-TY-ə-peen), sold under the brand name Seroquel among others, is a medication of the atypical antipsychotic class. It is used in the treatment of schizophrenia, bipolar disorder, and major depressive disorder. Quetiapine is also widely prescribed off-label as a sleep aid for its tranquillizing effects. Some have raised concerns that the undesirable side effects from off-label use may outweigh its benefits, though this remains an active area of research. It is taken orally. Common side effects include sedation, fatigue, weight gain, constipation, and dry mouth. Other side effects include low blood pressure with standing, seizures, high blood sugar, tardive dyskinesia, and neuroleptic malignant syndrome. In older people with dementia, its use increases the risk of death. Use in the third trimester of pregnancy may result in a movement disorder in the baby for some time after birth. Quetiapine is believed to work by blocking a number of receptors, including those for serotonin and dopamine. Quetiapine was developed in 1985 and was approved for medical use in the United States in 1997. It is available as a generic medication. In 2023, it was the most prescribed antipsychotic and 60th most commonly prescribed medication in the United States, with more than 10 million prescriptions. It is on the World Health Organization's List of Essential Medicines. The drug is typically among two antipsychotics (the other being olanzapine) to have superior efficacy for the treatment of bipolar disorder. Quetiapine is one of only two antipsychotics (the other is cariprazine) that produce equal efficacy as standalone therapies for mixed manic-depressive mood swings as they do in combination with an SSRI antidepressant. However, it is less potent than clozapine, amisulpride, olanzapine, risperidone, and paliperidone in alleviating psychotic symptoms or treating schizophrenia.
Before the 1921 destruction of Tulsa’s Greenwood District, Black residents had created a remarkable center of business and community life. The district included stores, professional offices, entertainment venues and homes owned by Black citizens. Understanding Greenwood means learning what was built—not only what was burned.
MORE →Madam C.J. Walker
