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GREENWOOD / BLACK WALL STREET WILMINGTON 1898 LITTLE ROCK NINE TUSKEGEE STUDY ROSEWOOD 1923 THE TUSKEGEE AIRMEN SENECA VILLAGE BLACK TOWNS GREENWOOD / BLACK WALL STREET WILMINGTON 1898 LITTLE ROCK NINE TUSKEGEE STUDY ROSEWOOD 1923 THE TUSKEGEE AIRMEN SENECA VILLAGE BLACK TOWNS
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MY'STORY

The MOVE Fire

This is a personal recollection on the Move fire on May 13, 1985 Philadelphia police fired thousands of rounds at the MOVE house, city officials approved dropping an explosive device on the roof, the resulting fire was allowed to burn, 11 people—including five children—died, and 61 homes were destroyed. Philadelphia City Council later called it a “brutal attack carried out by the City of Philadelphia on its own citizens” and acknowledged that no individual faced criminal consequences for the bombing. One timeline correction worth preserving for the BHP record: the major previous MOVE-police confrontation was August 8, 1978, about seven years before the bombing, not a year or two earlier. Officer James Ramp was killed, other police and firefighters were wounded, nine MOVE members were later convicted, and television cameras recorded police beating Delbert Africa during his arrest. The 1985 MOVE Commission later specifically criticized city planners for failing to adequately use lessons from that 1978 confrontation. And that actually strengthens the point you’re making: 1985 did not happen without precedent or institutional memory. There had already been a deadly confrontation with MOVE, years of conflict, negotiations and police involvement before Osage Avenue.

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BLACK FACTS
The Truths They Never Taught You...

Wilmington 1898 — An American Coup

Wilmington, North Carolina once had a thriving Black middle class and an elected interracial government. In 1898 white supremacists used violence to overthrow that government, kill Black residents and drive many others from the city.

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Wikipedia

Indazolethylamine

Indazolethylamines, or indazolylethylamines, are a group of indazole derivatives closely related to the tryptamines (indolylethylamines). Examples include the simple indazolethylamines AL-34662 and O-methyl-AL-34662 and the cyclized indazolethylamines AL-38022A, VU6067416, and YM-348. These indazolethylamines are known to act as serotonin 5-HT2 receptor agonists. Some of them, such as O-methyl-AL-34662 and AL-38022A, have been shown to produce psychedelic-like effects in animals similarly to tryptamines.[1][2][3][4][5][6][7][8]

Chemical structures of selected indazolethylamines

See also

[edit]

References

[edit]
  1. ^ Nichols, David E. (2012). "Structure–activity relationships of serotonin 5‐HT 2A agonists" (PDF). Wiley Interdisciplinary Reviews: Membrane Transport and Signaling. 1 (5): 559–579. doi:10.1002/wmts.42. ISSN 2190-460X.
  2. ^ Nichols DE (2018). "Chemistry and Structure-Activity Relationships of Psychedelics". Curr Top Behav Neurosci. 36: 1–43. doi:10.1007/7854_2017_475. PMID 28401524.
  3. ^ Kargbo RB (November 2023). "Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment". ACS Medicinal Chemistry Letters. 14 (11): 1498–1500. doi:10.1021/acsmedchemlett.3c00444. PMC 10641896. PMID 37974947.
  4. ^ May JA, Dantanarayana AP, Zinke PW, McLaughlin MA, Sharif NA (January 2006). "1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity". Journal of Medicinal Chemistry. 49 (1): 318–328. doi:10.1021/jm050663x. PMID 16392816.
  5. ^ Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S (February 2008). "Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists". Bioorganic & Medicinal Chemistry. 16 (4): 1966–1982. doi:10.1016/j.bmc.2007.10.100. PMID 18035544.
  6. ^ May JA, Sharif NA, Chen HH, Liao JC, Kelly CR, Glennon RA, Young R, Li JX, Rice KC, France CP (January 2009). "Pharmacological properties and discriminative stimulus effects of a novel and selective 5-HT2 receptor agonist AL-38022A [(S)-2-(8,9-dihydro-7H-pyrano[2,3-g]indazol-1-yl)-1-methylethylamine]". Pharmacol Biochem Behav. 91 (3): 307–314. doi:10.1016/j.pbb.2008.07.015. PMC 3763814. PMID 18718483.
  7. ^ May JA, Sharif NA, McLaughlin MA, Chen HH, Severns BS, Kelly CR, Holt WF, Young R, Glennon RA, Hellberg MR, Dean TR (November 2015). "Ocular Hypotensive Response in Nonhuman Primates of (8R)-1-[(2S)-2-Aminopropyl]-8,9-dihydro-7H-pyrano[2,3-g]indazol-8-ol a Selective 5-HT2 Receptor Agonist". J Med Chem. 58 (22): 8818–8833. doi:10.1021/acs.jmedchem.5b00857. PMID 26551970.
  8. ^ Kimura Y, Hatanaka K, Naitou Y, Maeno K, Shimada I, Koakutsu A, Wanibuchi F, Yamaguchi T (January 2004). "Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist". Eur J Pharmacol. 483 (1): 37–43. doi:10.1016/j.ejphar.2003.10.004. PMID 14709324.



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Wikipedia

Indazolethylamine

Indazolethylamines, or indazolylethylamines, are a group of indazole derivatives closely related to the tryptamines (indolylethylamines). Examples include the simple indazolethylamines AL-34662 and O-methyl-AL-34662 and the cyclized indazolethylamines AL-38022A, VU6067416, and YM-348. These indazolethylamines are known to act as serotonin 5-HT2 receptor agonists. Some of them, such as O-methyl-AL-34662 and AL-38022A, have been shown to produce psychedelic-like effects in animals similarly to tryptamines.

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Wikipedia

AL-34662

AL-34662 is an indazolethylamine derivative drug that is being developed for the treatment of glaucoma. It acts as a selective serotonin 5-HT2 receptor agonist, including of the 5-HT2A, 5-HT2B, and 5-HT2C receptors (affinity (IC50Tooltip half-maximal inhibitory concentration) = 14.5, 8.1, and 3.0 nM, respectively). The serotonin 5-HT2A receptor is the same target as that of psychedelic drugs like psilocin. Unlike these drugs however, AL-34662 was designed specifically as a peripherally selective drug, which does not cross the blood–brain barrier. This means that AL-34662 can exploit a useful side effect of the hallucinogenic 5-HT2A receptor agonists, namely reduction in intra-ocular pressure and hence relief from the symptoms of glaucoma, but without causing the psychedelic effects that make centrally active serotonin 5-HT2A receptor agonists unsuitable for clinical use. In animal studies, AL-34662 has been shown to be potent and effective in the treatment of symptoms of glaucoma, with minimal side effects. Peripherally acting 5-HT2A agonists have been a rich field of research in recent years, with potential glaucoma treatments being the main proposed application for serotonin 5-HT2A receptor agonists at present, as centrally acting agonists for this receptor tend to be hallucinogenic and thus their medical usefulness is currently limited to the treatment of psychiatric disorders. While many novel, potent, and selective serotonin 5-HT2A receptor agonists have been developed for this application, retaining peripheral selectivity can be a problem, and several of the more lipophilic compounds closely related to AL-34662 such as those shown below, did cross the blood–brain barrier and produced hallucinogen-appropriate responding in animals.

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Wikipedia

VU6067416

VU6067416 is an indazolethylamine and tetrahydropyridinylindazole derivative which acts as an agonist for the 5-HT2 family of serotonin receptors. It is a potent full agonist at 5-HT2B, and has slightly lower affinity and partial agonist effects at 5-HT2A and 5-HT2C, though some related compounds have improved selectivity for 5-HT2A.

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Wikipedia

O-Methyl-AL-34662

O-Methyl-AL-34662, also known as indazole-5-MeO-AMT, is a serotonin receptor agonist and putative serotonergic psychedelic of the indazolethylamine family related to the psychedelic tryptamine 5-MeO-AMT. It is an analogue of 5-MeO-AMT in which the indole ring has been replaced with an indazole ring and the active enantiomer has been purified. The drug is a potent agonist of the serotonin 5-HT2 receptors, including of the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. It is a partial to full agonist of the serotonin 5-HT2A receptor and a full agonist of the serotonin 5-HT2C receptor. Both O-methyl-AL-34662 and 5-MeO-AMT showed around 10-fold lower potency as agonists of the serotonin 5-HT2A receptor compared to the serotonin 5-HT2B and 5-HT2C receptors. The drug has roughly the same activational potencies and efficacies at the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors as 5-MeO-AMT. It potently induces the head-twitch response, a behavioral proxy of psychedelic effects, in mice, and hence may have hallucinogenic effects in humans. Its effective dose for induction of the head-twitch response was 0.16 mg/kg, which was about the same as that of (R)-DOI (0.13 mg/kg) and was about 6-fold more potent than 5-MeO-AMT (1.0 mg/kg). O-Methyl-AL-34662 was first described in the scientific literature by Jesse May and colleagues by 2006. In contrast to the case of O-methyl-AL-34662, the corresponding "flipped" indazole analogue of 5-MeO-DMT has profoundly reduced potency as a serotonin 5-HT2A receptor agonist relative to 5-MeO-DMT (~1,250-fold lower activational potency).

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TOPIC OF THE DAY

Greenwood / Black Wall Street

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.

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TRIVIA QUESTION OF THE DAY

Who was the first African-American woman millionaire in the United States?

Madam C.J. Walker