Chemicals and Drugs
Carbolines
Carbolines
A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.

Functional GABAA receptor heterogeneity of acutely dissociated hippocampal CA1 pyramidal cells. (1/508)

CA1 pyramidal cells were voltage clamped, and GABA was applied to individual cells with a modified U-tube, rapid drug application system. With Vh = -50 mV, inward currents elicited by 10 microM GABA were inhibited by GABAA receptor (GABAR) antagonists and were baclofen insensitive, suggesting that GABA actions on isolated CA1 pyramidal cells were GABAR mediated. GABA concentration-response curves averaged from all cells were fitted best with a two-site equation, indicating the presence of at least two GABA binding sites, a higher-affinity site (EC50-1 = 11.0 microM) and a lower-affinity site (EC50-2 = 334.2 microM), on two or more populations of cells. The effects of GABAR allosteric modulators on peak concentration-dependent GABAR currents were complex and included monophasic (loreclezole) or multiphasic (diazepam) enhancement, mixed enhancement/inhibition (DMCM, zolpidem) or multiphasic inhibition (zinc). Monophasic (70% of cells) or biphasic (30% of cells) enhancement of GABAR currents by diazepam suggested three different sites on GABARs (EC50-1 =1.8 nM; EC50-2 = 75.8 nM; EC50-3 = 275.9 nM) revealing GABAR heterogeneity. The imidazopyridine zolpidem enhanced GABAR currents in 70% of cells with an EC50 = 222.5 nM, suggesting a predominance of moderate affinity alpha2 (or alpha3-) subtype-containing BZ Type IIA receptors. A small fraction of cells (10%) had a high affinity for zolpidem, something that is suggestive of alpha1 subtype-containing BZ Type I receptors. The remaining 30% of cells were insensitive to or inhibited by zolpidem, suggesting the presence of alpha5 subtype-containing BZ Type IIB receptors. Whether BZ Type I and Type II receptors coexist could not be determined. The beta-carboline methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) inhibited GABAR currents in all cells at midnanomolar concentrations, but in addition, potentiated GABAR currents in some cells at low nanomolar concentrations, characterizing two groups of cells, the latter likely due to functional assembly of alpha5betaxgamma2GABARs. In all cells, GABAR currents were moderately sensitive (EC50 = 9 microM) to loreclezole, consistent with a relatively greater beta3 subtype, than beta1 subtype, subunit mRNA expression. Two populations of cells were identified based on their sensitivities to zinc(IC50 = 28 and 182 microM), suggesting the presence of at least two GABAR isoforms including alpha5beta3gamma2 GABARs. Consistent with the heterogeneity of expression of GABAR subunit mRNA and protein in the hippocampus and based on their differential responses to GABA and to allosteric modulators, distinct populations of CA1 pyramidal cells likely express multiple, functional GABAR isoforms.  (+info)

Occurrence of stereoisomers of 1-(2'-pyrrolidinethione-3'-yl)- 1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid in fermented radish roots and their different mutagenic properties. (2/508)

Stereoisomers of the tetrahydro-beta-carboline derivative, 1-(2-pyrrolidinethione)-3-yl)-1,2,3,4-tetrahydro-beta-carboline- 3-carboxylic acid (PTCC), were formed from L-tryptophan with 4-methylthio-3-butenyl isothiocyanate, and their mutagenic properties and contents in different types of the radish products were studied. The isomers were identified as (1S*, 3S*, 3R*)- and (1R*, 3S*, 3R*)-PTCCs; the former was found as the major compound but had no mutagenic activity, while the latter was mutagenic toward Salmonella typhimurium TA 98 in the presence of a rat microsomal fraction. Both (1S*, 3S*, 3R*)- and (1R*, 3S*, 3R*)-PTCC were detected in a ratio of about 4:1 in a product fermented for 8 months, but only a trace was apparent in products manufactured within a few weeks.  (+info)

Heterocyclic aromatic amines induce DNA strand breaks and cell transformation. (3/508)

Heterocyclic aromatic amines (HAAs), formed during the cooking of foods, are known to induce tumours in rodent bioassays and may thus contribute to human cancer risk. We tested six HAAs in a morphological transformation assay and in three in vitro genotoxicity assays. The morphological transforming abilities of HAAs were tested, in the presence of rat-liver S9, in the C3H/M2 fibroblast cell line. Concentration levels of 50 microM 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (8-MeIQx), 100 microM 2-amino-3,4,8-trimethylimidazo-[4,5-f]quinoxaline (4,8-DiMeIQx), 50 microM 2-amino-3-methylimidazo[4,5-f]quinoline (IQ), 100 microM 2-amino-9H-pyrido[2,3-b]indole (AalphaC), 100 microM 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeAalphaC) and 15 microM 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) induced maximum transformation potencies of 5.5, 6.6, 6.3, 5.2, 7.3 and 9.2 transformed foci per 10(4) surviving cells, respectively. Bacterial mutagenic activity was determined in the presence of rat-liver S9 using the Salmonella typhimurium reverse-mutation assay employing strain YG1019. Mutagenic potencies of 3800 revertants (revs)/ng with 8-MeIQx, 2900 revs/ng with 4,8-DiMeIQx, 3480 revs/ng with IQ, 1.6 revs/ng with AalphaC, 2.9 revs/ng with MeAalphaC and 5 revs/ng with PhIP were observed. Clastogenic activity in vitro was analysed by the micronucleus assay in metabolically competent MCL-5 cells. Dose-dependent induction of micronuclei was observed for all HAAs tested with 1-5.4% of cells containing micronuclei at 10 ng/ml. Micronucleus induction was in the order 4,8-DiMeIQx > 8-MeIQx > IQ > MeAalphaC > PhIP > AalphaC. DNA strand-breaking activity in MCL-5 cells was measured by the alkaline single cell-gel (comet) assay. The lowest effect doses for significant increases (P < or = 0.0007, Mann-Whitney test) in comet tail length (microm) were 45.5 microg/ml (200 microM) for PhIP, 90.9 microg/ml (410-510 microM) for 4,8-DiMeIQx, IQ, MeAalphaC and AalphaC, and 454.5 microg/ml (2130 microM) for 8-MeIQx. It is not yet clear which of these assays most accurately reflects the genotoxic potential to humans of compounds of this class of environmental carcinogens.  (+info)

Mapping quantitative trait loci for seizure response to a GABAA receptor inverse agonist in mice. (4/508)

To define the genetic contributions affecting individual differences in seizure threshold, a beta carboline [methyl-beta-carboline-3-carboxylate (beta-CCM)]-induced model of generalized seizures was genetically dissected in mice. beta-CCM is a GABAA receptor inverse agonist and convulsant. By measuring the latency to generalized seizures after beta-CCM administration to A/J and C57BL6/J mice and their progeny, we estimated a heritability of 0.28 +/- 0.10. A genome wide screen in an F2 population of these parental strains (n = 273) mapped quantitative trait loci (QTLs) on proximal chromosome 7 [logarithm of the likelihood for linkage (LOD) = 3.71] and distal chromosome 10 (LOD = 4.29) for seizure susceptibility, explaining approximately 22 and 25%, respectively, of the genetic variance for this seizure trait. The best fitting logistic regression model suggests that the A/J allele at each locus increases the likelihood of seizures approximately threefold. In a subsequent backcross population (n = 223), we mapped QTLs on distal chromosome 4 (LOD = 2.88) and confirmed the distal chromosome 10 QTLs (LOD = 4.36). In the backcross, the C57BL/6J allele of the chromosome 10 QTL decreases the risk of seizures approximately twofold. These QTLs may ultimately lead to the identification of genes influencing individual differences in seizure threshold in mice and the discovery of novel anticonvulsant agents. The colocalization on distal chromosome 10 of a beta-CCM susceptibility QTL and a QTL for open field ambulation and vertical movement suggests the existence of a single, pleiotropic locus, which we have named Exq1.  (+info)

The fluorescence of scorpions and cataractogenesis. (5/508)

BACKGROUND: Protein cross-linking and fluorescence are widely recognized markers of oxidative aging in human proteins. Oxidative protein aging is a combinatorial process in which diversity arises from the heterogeneity of the targets and is amplified by the nonselective nature of the reactants. The cross-links themselves defy analysis because they are generally embedded in a covalent matrix. Arthropods rely upon oxidative cross-linking in the hardening of the cuticle - a process known as sclerotization. Among arthropods, scorpions are noteworthy in that the process of sclerotization is accompanied by the buildup of strong visible fluorescence. To date, the nature of the fluorescent species has remained a mystery. RESULTS: We have identified one of the soluble fluorescent components of the scorpions Centuroides vittatus and Pandinus imperator as beta-carboline - a tryptophan derivative that has previously been identified by hydrolysis and oxidation of lens protein. We have also shown that beta-carboline-3-carboxylic acid is released from both scorpion exuvia (the shed cuticle) and human cataracts upon hydrolysis, suggesting that the protein-bound beta-carboline and free beta-carboline have common chemical origins. CONCLUSIONS: Cataractogenesis and cuticular sclerotization are disparate oxidative processes - the former is collateral and the latter is constitutive. The common formation of beta-carbolines shows that similar patterns of reactivity are operative. These fundamental mechanisms provide predictive insight into the consequences of human protein aging.  (+info)

Apparent pA2 values of benzodiazepine antagonists and partial agonists in monkeys. (6/508)

Drugs that bind to benzodiazepine recognition sites of gamma-aminobutyric acid type A receptor complexes may function as agonists in some behavioral assays and as antagonists in other behavioral assays. The present studies compared the effects of the benzodiazepines midazolam, flumazenil, bretazenil, Ro 41-7812, and Ro 42-8773 and the beta-carboline, beta-carboline-3-carboxylate-t-butyl ester (beta-CCt) under two different types of schedule-controlled responding in squirrel monkeys. One group of monkeys responded under a fixed-ratio schedule of stimulus-shock termination, and a second group of monkeys responded under a multiple fixed-ratio schedule of food presentation involving suppressed and nonsuppressed behavior. Under the schedule of stimulus-shock termination, midazolam produced dose-related decreases in response rate, and these effects were surmountably antagonized by flumazenil, bretazenil, Ro 41-7812, Ro 42-8773, and beta-CCt. Schild plot analysis of these data revealed the following mean pA(2) values: flumazenil, 7.18; bretazenil, 7.62; Ro 41-7812, 7. 06; Ro 42-8773, 6.95. Apparent pA(2) values were not calculated for beta-CCt because the CL of the slope of the Schild plot included positive values. Under the multiple schedule, midazolam, bretazenil, and Ro 42-8773 dose-dependently increased rates of suppressed responding, whereas flumazenil, Ro 41-7812, and beta-CCt had no significant rate-altering effects. Flumazenil antagonized the antisuppressant effects of midazolam and bretazenil; however, individual variability in these effects prohibited the determination of apparent pA(2) values. These results indicate that in vivo pA(2) values may be determined for benzodiazepine-site ligands. These results further demonstrate that some benzodiazepine-site ligands, e. g., bretazenil and Ro 42-8773, may function as both agonists and as competitive antagonists in vivo.  (+info)

Dual mode of stimulation by the beta-carboline ZK 91085 of recombinant GABA(A) receptor currents: molecular determinants affecting its action. (7/508)

In electrophysiological measurements the beta-carboline ethyl 6-benzyloxy-beta-carboline-3-carboxylate (ZK 91085) acts as a positive allosteric modulator on rat recombinant alpha1beta2gamma2 GABA(A) receptors and binds with high affinity (IC50-1.5 nM) to the [3H]-flunitrazepam site. Flumazenil was able to partially counteract the current modulation. These observations indicate an action of ZK 91085 at the benzodiazepine binding site. At the dual subunit combination alpha1beta2, which lacks the gamma subunit required for benzodiazepine modulation, we still observed a potentiation of GABA currents. Thus ZK 91085 acts via an additional site on the channel. At the subunit combination alpha1beta1, ZK 91085 potentiation is strongly reduced as compared to alpha1beta2. In binding studies, ZK 91085 was able to decrease [35S]-TBPS binding in alpha1beta2gamma2 and alpha1beta2 but not in alpha1beta1. This selectivity of ZK 91085 for receptors containing the beta2 isoform over those containing the beta1 isoform is reminiscent of the action of loreclezole. To identify amino acid residues important for the second type of modulation, we functionally compared wild type alpha1beta2 and mutant receptors for stimulation by ZK 91085. The mutation beta2N265S, that abolishes loreclezole effects, also abolishes ZK 91085 stimulation. The mutation beta2Y62L increased stimulation by ZK 91085 3-4 fold, locating an influencing entity of the second type of action of ZK 91085 at an alpha/beta subunit interface. Structural intermediates of ZK 91085 and the beta-carboline abecarnil, the latter of which only slightly potentiated GABA currents in alpha1/beta2, were analysed to determine structural requirements for modulation. ZK 91085 thus allosterically stimulates the GABA(A) receptor through two sites of action: the benzodiazepine site and the loreclezole site in contrast to classical beta-carbolines, that confer negative allosteric modulation through the benzodiazepine site.  (+info)

Improvement in pain and bowel function in female irritable bowel patients with alosetron, a 5-HT3 receptor antagonist. (8/508)

BACKGROUND: No currently available treatment provides consistent relief of irritable bowel syndrome. Colonic sensory and motor function are modulated partly through 5HT3-receptors. AIM: To evaluate effects of the 5HT3-receptor antagonist, alosetron, in irritable bowel syndrome. METHODS: Randomized, double-blind, placebo-controlled, dose-ranging (1, 2, 4, 8 mg b.d. alosetron), 12-week trial in 370 patients with diarrhoea-predominant or alternating constipation and diarrhoea irritable bowel syndrome. Weekly measurement of adequate relief was the key end-point; other irritable bowel syndrome symptoms were collected daily using an electronic phone system. RESULTS: Alosetron (1 mg or 2 mg b.d.) significantly (P < 0.05 vs. placebo) increased the proportion of females, but not males, reporting adequate relief. Stool consistency, frequency and percentage days with urgency improved over placebo (P < 0.05) within the first month with all doses of alosetron, and persisted throughout the trial with all doses in female patients. With 1 mg b.d. alosetron, females had improved stool consistency and urgency within the first week, and adequate relief and improved stool frequency within the first 2 weeks. There was no consistent improvement in bowel function among male patients. CONCLUSION: In female irritable bowel syndrome patients with predominant diarrhoea or alternating constipation and diarrhoea, alosetron is effective in treatment of abdominal pain and discomfort and bowel-related symptoms.  (+info)

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Modulation of gamma-aminobutyric acidA receptor-operated chloride channels by benzodiazepine inverse agonists is related to...Modulation of gamma-aminobutyric acidA receptor-operated chloride channels by benzodiazepine inverse agonists is related to...
Modulation of gamma-aminobutyric acidA receptor-operated chloride channels by benzodiazepine inverse agonists is related to genetic differences in ethanol withdrawal seizure severity. Article date: 1991/12/1 PubMed ID: 1658234 Journal name: Journal of neurochemistry (ISSN: 0022-3042)
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IHCH-7113IHCH-7113
Substituted heterocycle fused gamma-carbolines. Patent US 6552017 Tomesch JC, et al. Preparation of 4-((6BR,10AS)-3-methyl-2,3, ...
https://en.wikipedia.org/wiki/IHCH-7113
GABAA receptorGABAA receptor
Inverse allosteric agonists: beta-carbolines (ex. Harmine, Harmaline, Tetrahydroharmine). Second-order modulators: (−)‐ ...
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6-MeO-THH6-MeO-THH
October 2001). "beta-carboline binding to imidazoline receptors". Drug and Alcohol Dependence. 64 (2): 203-8. doi:10.1016/S0376 ... 6-MeO-THH, or 6-methoxy-1,2,3,4-tetrahydroharman, is a β-carboline (or more specifically a pinoline) derivative and a ... Beta-carboline Harmala alkaloid Tryptamine Shulgin A, Shulgin A (September 1997). TiHKAL: The Continuation. Berkeley, ... August 2000). "Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A)), dopamine (D(2)) and ...
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Essential tremorEssential tremor
Louis ED, Zheng W, Jiang W, Bogen KT, Keating GA (June 2007). "Quantification of the neurotoxic beta-carboline harmane in ... Pfau W, Skog K (March 2004). "Exposure to beta-carbolines norharman and harman". Journal of Chromatography B. 802 (1): 115-26. ...
https://en.wikipedia.org/wiki/Essential_tremor
AyahuascaAyahuasca
Harmala alkaloids are MAO-inhibiting beta-carbolines. The three most studied harmala alkaloids in the B. caapi vine are harmine ... root bark is mixed with a native source of beta-Carbolines (e.g., passion flower in North America) to produce a hallucinogenic ...
https://en.wikipedia.org/wiki/Ayahuasca
Pineal glandPineal gland
The compound pinoline is also claimed to be produced in the pineal gland; it is one of the beta-carbolines. This claim is ... Formation of tetrahydro-β-carbolines at physiologicalpH". Journal of Heterocyclic Chemistry. 31 (2): 431-435. doi:10.1002/jhet. ...
https://en.wikipedia.org/wiki/Pineal_gland
Palladium(II) acetatePalladium(II) acetate
"Synthesis of α-Carboline". Org. Synth. 93: 272. doi:10.15227/orgsyn.093.0272.{{cite journal}}: CS1 maint: uses authors ...
https://en.wikipedia.org/wiki/Palladium(II)_acetate
QuazepamQuazepam
Chapman AG, De Sarro GB, Premachandra M, Meldrum BS (September 1987). "Bidirectional effects of beta-carbolines in reflex ...
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GrewiaGrewia
G. mollis is reputed to contain β-carboline alkaloids, though whether such compounds occur in other species too and whether ... Brown, Dan (2001): Angiosperm Families Containing Beta-Carbolines. Version of 2001-OCT-04. Retrieved 2008-JUN-25. Heywood, V.H ...
https://en.wikipedia.org/wiki/Grewia
List of psychoactive plantsList of psychoactive plants
Beta-carbolines Psychotria viridis, Beta-carbolines Simira klugei, Beta-carbolines Simira rubra, Beta-carbolines Uncaria ... Beta-carbolines Picrasma crenata, Beta-carbolines Picrasma excelsa, Beta-carbolines Picrasma javanica, Beta-carbolines Vestia ... Beta-carbolines Meconopsis paniculata, Beta-carbolines Meconopsis robusta, Beta-carbolines Meconopsis rudis, Beta-carbolines ... Phalaris aquatica, Beta-carbolines Phalaris arundinacea, Beta-carbolines Nectandra megapotamica, Beta-carbolines Acacia ...
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HarmineHarmine
The β-carboline carboxylic acid subsequently undergoes decarboxylation to produce 1-methyl β-carboline III. Hydroxylation ... Harmine is a beta-carboline and a harmala alkaloid. It occurs in a number of different plants, most notably the Syrian rue and ... This could explain the cytotoxic effect of Peganum harmala on these cells." Beta-carboline MAO inhibitors, such as harmine, ... The coincident occurrence of β-carboline alkaloids and serotonin in Peganum harmala indicates the presence of two very similar ...
https://en.wikipedia.org/wiki/Harmine
Ochrosia oppositifoliaOchrosia oppositifolia
Oppositines are vasorelaxant beta-carbolines isolated from Ochrosia oppositifolia. "Ochrosia oppositifolia". World Checklist of ... new vasorelaxant beta-carboline alkaloids from Neisosperma oppositifolia". Chemical & Pharmaceutical Bulletin. 58 (8): 1085- ...
https://en.wikipedia.org/wiki/Ochrosia_oppositifolia
ZK-93423ZK-93423
... beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3- ... ZK-93423 has also been used as a base to develop new and improved beta-carboline derivatives and help map the binding site of ... ZK-93423 is an anxiolytic drug from the β-Carboline family, closely related to abecarnil. It is a nonbenzodiazepine GABAA ... Dodd RH, Ouannès C, Potier MC, Prado de Carvalho L, Rossier J, Potier P (July 1987). "Synthesis of beta-carboline- ...
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EudistomaEudistoma
S. A. Adesanya; M. Chbani; M. Païs; C. Debitus (1992). "Brominated β-Carbolines from the Marine Tunicate Eudistoma album". J. ...
https://en.wikipedia.org/wiki/Eudistoma
OxopropalineOxopropaline
... s are novel cytocidal beta-carbolines isolated from Streptomyces. Abe N, Nakakita Y, Nakamura T, Enoki N, Uchida H ... Beta-Carbolines, All stub articles, Biochemistry stubs). ...
https://en.wikipedia.org/wiki/Oxopropaline
TetrahydroisoquinolineTetrahydroisoquinoline
PMID 7202207., Myers, R. D. (1989). "Isoquinolines, beta-carbolines and alcohol drinking: involvement of opioid and ... "Formaldehyde-derived tetrahydroisoquinolines and tetrahydro-beta-carbolines in human urine". Journal of Chromatography B. 683 ( ...
https://en.wikipedia.org/wiki/Tetrahydroisoquinoline
Phalaris arundinaceaPhalaris arundinacea
Levels of beta-carbolines and hordenine have also been reported. Waterside hot water hay pellet furnace Lee, Sangtae; Chang, ...
https://en.wikipedia.org/wiki/Phalaris_arundinacea
Oxalis tuberosaOxalis tuberosa
"Exudation of fluorescent b-carbolines from Oxalis tuberosa L. roots". Phytochemistry. 61 (5): 539-543. doi:10.1016/S0031-9422( ...
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ZK-93426ZK-93426
... (ethyl-5-isopropoxy-4-methyl-beta-carboline-3-carboxylate) is a drug from the beta-carboline family. It acts as a weak ... File, SE; Pellow, S; Jensen, LH (1986). "Actions of the beta-carboline ZK 93426 in an animal test of anxiety and the holeboard ... Duka, T; Edelmann, V; Schütt, B; Dorow, R (1988). Beta-carbolines as tools in memory research: human data with the beta- ... Duka, T; Ott, H; Rohloff, A; Voet, B (1996). "The effects of a benzodiazepine receptor antagonist beta-carboline ZK-93426 on ...
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EudistominEudistomin
... U is a β-carboline derivative. The structure of this molecule is made up of a β-carboline with an aromatic indole at ... Eudistomins are β-carboline derivatives, isolated from ascidians (marine tunicates of the family Ascidiacea), like Ritterella ... Davis RA, Carroll AR, Quinn RJ (June 1998). "Eudistomin V, a New β-Carboline from the Australian Ascidian Pseudodistoma aureum ... Edrada-Ebel, RuAngelie; Schupp, Paul R (2003). "Eudistomins W and X, Two New β-Carbolines from the Micronesian Tunicate ...
https://en.wikipedia.org/wiki/Eudistomin
PhotosensitizerPhotosensitizer
"Mechanisms of DNA damage by photoexcited 9-methyl-β-carbolines". Organic & Biomolecular Chemistry. 11 (32): 5300-5309. doi: ...
https://en.wikipedia.org/wiki/Photosensitizer
Callaeum antifebrileCallaeum antifebrile
The beta-carboline hallucinogens of South America. Journal of Psychoactive Drugs 14(3): 205-220. Grisebach, A.H.R. 1849. ...
https://en.wikipedia.org/wiki/Callaeum_antifebrile
PharmahuascaPharmahuasca
As a rule, the fewer the β-carbolines, the less nausea; the more DMT, the more spectacular the visions. The constituents are ...
https://en.wikipedia.org/wiki/Pharmahuasca
TryptolineTryptoline
... , also known as tetrahydro-β-carboline and tetrahydronorharmane, is a natural organic derivative of beta-carboline. ... Norharmane harmane beta-Carboline Harmala alkaloid H. Rommelspacher; H. Kauffmann; C. Heyck Cohnitz; H. Coper (1977). " ... Comparison of the inhibition kinetics of tetrahydro-β-carbolines for serotonin and epinephrine reuptake to that of the platelet ...
https://en.wikipedia.org/wiki/Tryptoline
TetrahydroharmolTetrahydroharmol
... is a bioactive beta-carboline harmala alkaloid. It acts as a reversible inhibitor of monoamine oxidase A. ... Buckholtz NS, Boggan WO (November 1977). "Monoamine oxidase inhibition in brain and liver produced by beta-carbolines: ... Beta-Carbolines, All stub articles, Alkaloid stubs). ...
https://en.wikipedia.org/wiki/Tetrahydroharmol
IndoleIndole
Gremmen, C.; Willemse, B.; Wanner, M. J.; Koomen, G.-J. (2000). "Enantiopure Tetrahydro-β-carbolines via Pictet-Spengler ...
https://en.wikipedia.org/wiki/Indole
Pictet-Spengler reactionPictet-Spengler reaction
Gremmen, C.; Willemse, B.; Wanner, M. J.; Koomen, G.-J. (2000). "Enantiopure Tetrahydro-β-carbolines via Pictet-Spengler ... 4-tetrahydro-β-carbolines in which a new chiral center at C-1 adopts either a cis or trans configuration towards the C-3 ... 4-tetrahydro-β-carbolines by carbon-13 spectroscopy". J. Am. Chem. Soc. 102 (23): 6976-6984. doi:10.1021/ja00543a012. (All ... where it has been employed in the development of many beta-carbolines. Natural Pictet-Spengler reaction typically employ an ...
https://en.wikipedia.org/wiki/Pictet–Spengler_reaction
NostocarbolineNostocarboline
... is a beta-carboline isolated from freshwater cyanobacterium. Becher, P. G.; Beuchat, J.; Gademann, K.; Jüttner, ... Beta-Carbolines, Halogen-containing alkaloids, Chloroarenes, Quaternary ammonium compounds). ...
https://en.wikipedia.org/wiki/Nostocarboline
KopsanoneKopsanone
Layne, Tanya H.; Roach, Joy S.; Tinto, Winston F. (January 2015). "Review of β-carboline Alkaloids from the Genus Aspidosperma ...
https://en.wikipedia.org/wiki/Kopsanone
Curtin-Hammett principleCurtin-Hammett principle
... carboline ring system from the marine sponge Cribrochalina olemda". Journal of the American Chemical Society. 117 (31): 8271- ...
https://en.wikipedia.org/wiki/Curtin–Hammett_principle
Browsing Journal Articles by Subject CarbolinesBrowsing Journal Articles by Subject "Carbolines"
JavaScript is disabled for your browser. Some features of this site may not work without it ...
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Beta-Carboline - WikipediaBeta-Carboline - Wikipedia
β-Carboline alkaloids are widespread in prokaryotes, plants and animals. Some β-carbolines, notably tetrahydro-β-carbolines, ... secretes a β-carboline (1-acetyl-β-carboline) preventing the pathogenic fungus Candida albicans to change to a more virulent ... Smoking is another source of fully aromatic β-carbolines with levels up to thousands of µg per smoker each day. β-Carbolines ... The pharmacological effects of specific β-carbolines are dependent on their substituents. For example, the natural β-carboline ...
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Re: beta carbolines to reverse benzo cognitive pro linkadge | Psycho-Babble
beta carbolines to reverse benzo cognitive probs linkadge 8/6/07. .... *Re: Getting Doctors to prescribe opiates Deus_Abscondis ... The beta carbolines have a short half life. Probably shorter than the shortest acting benzo (I would need to double check that ... Re: beta carbolines to reverse benzo cognitive pro linkadge. Posted by psychobot5000 on October 22, 2007, at 13:32:18 ... I think its the beta-carbolines in the coffee, being helpful.. It could be a placebo effect, of course, but thats what Ive ...
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Erowid.org: Erowid Reference 8140 : Investigation of hallucinogenic and related beta-carbolines : Grella B, Dukat M, Young R,...Erowid.org: Erowid Reference 8140 : Investigation of hallucinogenic and related beta-carbolines : Grella B, Dukat M, Young R,...
Glennon RA Investigation of hallucinogenic and related beta-carbolines Drug Alcohol Depend 1998 50(2):99-107 ... Certain beta-carbolines are known to be hallucinogenic in humans, and several produce stimulus effects in animals similar to ... In the present study, we examined the binding of 15 beta-carbolines at rat 5-HT2A and 5-HT2C receptors. Affinities Ki values of ... In a further study, six rats were trained to discriminate the hallucinogenic beta-carboline harmaline 3.0 mg/kg, i.p. from ...
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Global Cellulosic Fire Protection Intumescent Coating Market to 2030 - Featuring AkzoNobel, Jotun and Carboline Among Others -...Global Cellulosic Fire Protection Intumescent Coating Market to 2030 - Featuring AkzoNobel, Jotun and Carboline Among Others -...
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Carboline
... Share this post:. Share on TwitterShare on FacebookShare on LinkedInShare on Email ...
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Ethyl beta-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats. - Department of...
Recently, ethyl beta-carboline-3-carboxylate (beta-CCE) has been identified in both human urine and rat brain. beta-CCE may be ... Recently, ethyl beta-carboline-3-carboxylate (beta-CCE) has been identified in both human urine and rat brain. beta-CCE may be ... Ethyl beta-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats. ... Ethyl beta-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats. ...
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Carbolines | Profiles RNS
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Analysis of L-Tryptophan for the Etiology of Eosinophilia-Myalgia SyndromeAnalysis of L-Tryptophan for the Etiology of Eosinophilia-Myalgia Syndrome
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Browsing Journal Articles by SubjectBrowsing Journal Articles by Subject
Carbolines [‎2]‎. Cardiovascular Diseases [‎63]‎. Cardiovascular Infections [‎1]‎. Cardiovascular System [‎1]‎. Career Choice ...
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This website uses cookies and other tracking technologies (also known as pixels or beacons) to aid your experience (such as viewing videos), as well as "performance cookies" to analyze your use of this website and to assist with marketing efforts. If you click the "Accept All Cookies" button or continue navigating the website, you agree to having those first and third-party cookies set on your device. If you do not wish to accept cookies from this website, you can choose to not allow cookies from this website by updating your browser preferences. For more information on how we use Cookies, please read our Privacy Policy.. ...
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Carboline IndonesiaCarboline Indonesia
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Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors - ePrints - Newcastle UniversityStructure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors - ePrints - Newcastle University
Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Lookup NU author(s): Professor ...
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Inhibition study of monoamine oxidases by ß-carboline derivatives.<...
Inhibition study of monoamine oxidases by ß-carboline derivatives. Dans: Drugs of the future. 2010 ; Vol 35, Numéro suppl A. p ... title = "Inhibition study of monoamine oxidases by {\ss}-carboline derivatives.",. author = "J{\e}r{\e}my Reniers and S{\e} ... Inhibition study of monoamine oxidases by ß-carboline derivatives. Drugs of the future. 2010;35(suppl A):189. ... Inhibition study of monoamine oxidases by ß-carboline derivatives.. Jérémy Reniers, Séverine Robert, Raphaël Frédérick, Bernard ...
https://researchportal.unamur.be/fr/publications/inhibition-study-of-monoamine-oxidases-by-%C3%9F-carboline-derivatives
Rodzaje zabezpieczeń ogniochronnych betonu | Carboline PolskaRodzaje zabezpieczeń ogniochronnych betonu | Carboline Polska
Zaprawa ogniochronna. Natrysk ogniochronny do betonu Perlifoc przeznaczony jest do biernej ochrony przed ogniem między innymi elementów betonowych nośnych, płyt betonowych kompozytowych płaskich elementów nośnych z betonu i stali profilowanej. Aplikacja odbywa się z zastosowaniem agregatów tynkarskich z komorą przepływową, gdzie dochodzi do mieszania zaprawy z wodą. Natrysk ogniochronny Perlifoc stanowi mieszaninę surowców, perlitu oraz wermikulitu z hydraulicznym środkiem wiążącym.
https://www.carbolinepolska.pl/post/rodzaje-zabezpieczen-ogniochronnych-betonu
Long-term safety and tolerability of tadalafil in the treatment of erectile dysfunctionLong-term safety and tolerability of tadalafil in the treatment of erectile dysfunction
Carbolines / adverse effects * Carbolines / therapeutic use* * Comorbidity * Erectile Dysfunction / drug therapy* * Humans ...
https://pubmed.ncbi.nlm.nih.gov/15036680/
Beta-CarbolineHarmineAlkaloidDerivativesCoatingsALKALOIDSHarmalineCompanySherwin-WilliamsInhibitorsLiningsDerivativeMonoamine-oxidaseIndolesProductsReceptorsChemicalsCarbonylCandidaMeSHReducesTryptaminesPharmacologicalSubstancesDigestAntioxidantBuspironeGroupHumansMainComplexStudyPrimary
Beta-Carboline12
  • Moreover, 3-hydroxymethyl-beta-carboline blocks the sleep-promoting effect of flurazepam in rodents and - by itself - can decrease sleep in a dose-dependent manner. (wikipedia.org)
  • In a further study, six rats were trained to discriminate the hallucinogenic beta-carboline harmaline 3.0 mg/kg, i.p. from vehicle using a VI-15s schedule of reinforcement. (erowid.org)
  • This represents the first time a hallucinogenic beta-carboline has been used as a training drug in a drug discrimination study. (erowid.org)
  • Ethyl beta-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats. (ox.ac.uk)
  • Recently, ethyl beta-carboline-3-carboxylate (beta-CCE) has been identified in both human urine and rat brain. (ox.ac.uk)
  • In addition to peaks 97, 100, and 200, ongoing investigation is directed at 1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid (MTCA) (Figure 1B) and bacitracin, detected in LT lots from the implicated manufacturer (6). (cdc.gov)
  • Behavioral evidence for the role of noradrenaline in the putative anxiogenic actions of the inverse benzodiazepine receptor agonist methyl-4-ethyl-6,7-dimethoxy-beta-carboline-3-carboxylate. (aspetjournals.org)
  • The role of noradrenaline in the anxiogenic action of the inverse benzodiazepine receptor agonist methyl-4-ethyl-6,7-dimethoxy-beta-carboline-3-carboxylate (DMCM) was assessed in a drug discrimination procedure using yohimbine as the stimulus cue and a conflict procedure using a conditioned behavioral suppression paradigm in rats. (aspetjournals.org)
  • Other antioxidants in AGE include non organosulfur compounds, such as fructosyl arginine, tetrahydro-beta-carboline derivatives, allixin and saponins. (totalhealthmagazine.com)
  • The findings of a 2017 study Trusted Source in mice suggest that harmine, the primary beta-carboline in ayahuasca, may have neuroprotective and cognitive-enhancing effects because it reduces inflammation and oxidative stress. (onlinepsychedelicshome.com)
  • It contains beta-carboline harmala alkaloids which elevates happiness-promoting chemicals. (homeremediespost.com)
  • The company's patented Beta-carboline derivative (ACB1801) is an actin dynamic modulator which induces cellular F-actin network remodeling (tumor reversal). (biopole.ch)
Harmine5
  • For example, the natural β-carboline harmine has substituents on position 7 and 1. (wikipedia.org)
  • Both of Peganum harmala's major carbolines, harmaline and harmine, are rather intensely fluorescent compounds. (erowid.org)
  • The ß-carboline alkaloid harmine inhibits telomerase activity of MCF-7 cells by down-regulating hTERT mRNA expression accompanied by an accelerated senescent phenotype. (uni-heidelberg.de)
  • Harmine is the β -carboline alkaloid with the highest concentration in the psychotropic plant decoction Ayahuasca. (peerj.com)
  • The seeds contain the carboline alkaloids harmane and harmine. (himalayawellness.in)
Alkaloid1
  • These substances include the neuroprotector carbacetam, an modulator of the GABA-benzodiazepine receptor complex, a derivative of the alkaloid β-carboline. (msu-journal.com)
Derivatives3
  • Synthetically designed β-carboline derivatives have recently been shown to have neuroprotective, cognitive enhancing and anti-cancer properties. (wikipedia.org)
  • β-carboline derivatives also enhance the production of the antibiotic reveromycin A in soil dwelling "Streptomyces" species. (wikipedia.org)
  • Inhibition study of monoamine oxidases by ß-carboline derivatives. (unamur.be)
Coatings9
  • Carboline Company, a manufacturer of industrial coatings, has announced that it will expand its Canadian presence in the coatings, linings, and fireproofing industries and increase its focus on the renewable energy sector through a five-year strategic growth plan. (worldpipelines.com)
  • In 1985, RPM made its largest deal to date with the acquisition of industrial corrosion control coatings manufacturer Carboline Company. (rpminc.com)
  • Coatings manufacturer Carboline Company recently hosted a grand opening for its Carboline Fire-Science Research Center in St. Louis. (paintsquare.com)
  • Coatings manufacturer Carboline Company announced Wednesday that the first steps have been taken toward a new passive fire protection testing facility. (paintsquare.com)
  • Coatings manufacturer Carboline announced Wednesday that it has broken ground on a new passive fire protection testing facility. (paintsquare.com)
  • APC uses only industry leading coating manufacturers to provide industrial coatings to our customers including but not limited to Carboline, CIM Industries, and Chesterton ARC Coatings. (thebluebook.com)
  • Carboline is een van de grootste verffabrikanten ter wereld, gespecialiseerd in beschermende coatings, bekledingen en passieve brandwerende coatings. (paintdeals.com)
  • Carboline has a wide range of coatings, linings, and fireproofing solutions. (proco-fwi.com)
  • It will operate as a free-standing business within the RPM Performance Coatings Group and report through the Carboline Company. (borderless.net)
ALKALOIDS5
  • β-Carboline (9H-pyrido[3,4-b]indole) represents the basic chemical structure for more than one hundred alkaloids and synthetic compounds. (wikipedia.org)
  • β-Carbolines belong to the group of indole alkaloids and consist of a pyridine ring that is fused to an indole skeleton. (wikipedia.org)
  • Targeting cell cycle by β-carboline alkaloids in vitro: Novel therapeutic prospects for the treatment of cancer. (semanticscholar.org)
  • Beta-carbolines, a large group of indole alkaloids are widely distributed in plants. (peerj.com)
  • Our Magic Molecules pattern depicts a selection of various psychoactive molecular compounds that are derived from plant alkaloids, including an assortment of cannabinoids, tryptamines, phenylethylamines, and beta-carbolines. (aimeewilder.com)
Harmaline2
  • Taken together, the results of the present investigation demonstrate that: a certain beta-carbolines bind at 5-HT2 receptors b that harmaline serves as a training drug at 3.0 mg/kg in drug discrimination studies with rats as subjects and that c there is some similarity between the stimulus effects produced by harmaline and DOM. (erowid.org)
  • β-Carbolines such as HARMALINE (HA) has been shown to exert multiple pharmacologic actions, including monoamine oxidase inhibition, convulsive or anticonvulsive action, and anxiolytic effects. (sid.ir)
Company1
  • Through our strategic growth plan, we will expand our geographic reach, add new markets, expand our expertise and enhance our supply chain and distribution processes, all while strengthening our commitment to the renewable energy market," said Russ Nakoneshny, Director - Canada, Carboline Company. (worldpipelines.com)
Sherwin-Williams2
  • The owner-approved Group I manufacturers are Carboline, International Paint, ICI Devoe and Sherwin-Williams. (paintsquare.com)
  • These include International paints, Sherwin Williams, Jotun and Carboline. (stork.com)
Inhibitors3
  • Beta-carbolines are both monoamine-oxidase (MAO) inhibitors and serotonin reuptake inhibitors, which means that they prevent the breakdown of serotonin by inhibiting its uptake into the brain's synapses, akin to the action of selective serotonin reuptake inhibitors (SSRIs) like Prozac. (lynnemctaggart.com)
  • 7,8-Dichloro-1-oxo-beta-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes. (weizmann.ac.il)
  • The B. caapi vine contains MAO inhibitors (MAOIs) called beta-carbolines. (onlinepsychedelicshome.com)
Linings2
  • Our NORSOK approved systems for atmospheric applications, decks, splash zone and subsea coupled with a complete line of tank linings and fireproofing makes Carboline a dominant and reliable supplier for offshore protection. (otcnet.org)
  • Carboline offers a comprehensive line of zinc primers, epoxy anticorrosives, high performance topcoats, IMO-approved ballast tank linings, and antifoulings that will provide service for up to 60 months. (epindustrydirectory.com)
Derivative2
  • A synthetic derivative, 9-methyl-β-carboline, has shown neuroprotective effects including increased expression of neurotrophic factors and enhanced respiratory chain activity. (wikipedia.org)
  • Another derivative, methyl-β-carboline-3-carboxylate, stimulates learning and memory at low doses but can promote anxiety and convulsions at high doses. (wikipedia.org)
Monoamine-oxidase2
  • B. caapi is rich in beta-carbolines, which have monoamine oxidase-inhibiting properties, the main pharmacological mechanism of some antidepressants currently used in clinical practice (Meister et al. (springer.com)
  • The beta-carbolines present in Banisteriopsis caapi, inhibit the enzyme Monoamine Oxidase and reduces the metabolism of serotonin. (shamballaretreats.com)
Indoles1
  • A novel cascade reaction of indole-2,3-epoxide equivalents with γ-carbolines by utilizing a double "open and shut" transformation to access multiheterocyclic compounds containing both isotryptamines and pyrimido[1,6-a]indoles has been developed. (elsevier.com)
Products5
  • however, the suspected decomposition products, the beta-carbolines, exhibit a variety of biologic properties (7). (cdc.gov)
  • Penetrating primer/sealer for use on concrete substrates and Carboline Pyrocrete Fireproofing products. (carboline.com)
  • Carboline will also embark on enhancing its supply chain and distribution processes, creating a more effective and streamlined experience for its Canadian market while ensuring customers have access to the best products available so their projects can stay on track. (worldpipelines.com)
  • Carboline delivers… The Right Products. (carboline.com)
  • Background: β-Carbolines are found in cigarette smoke and cooked protein-rich foods such as meat and fish products, reflecting its formation from tryptophan by pyrolysis. (sid.ir)
Receptors3
  • However, β-carbolines with substituents in position 3 reduce the effect of benzodiazepine on GABA-A receptors and can therefore have convulsive, anxiogenic and memory enhancing effects. (wikipedia.org)
  • In the present study, we examined the binding of 15 beta-carbolines at rat 5-HT2A and 5-HT2C receptors. (erowid.org)
  • beta-Carbolines and benzodiazepine receptors: structure-activity relationships and pharmacologic activity. (wustl.edu)
Chemicals1
  • According to recent neurochemical research, the pineal gland also produces the 'neuromodulator' chemicals--called beta-carbolines. (lynnemctaggart.com)
Carbonyl1
  • The Lewis acid assisted imide carbonyl activation methodology was successfully extended to synthesize fused tetrahydro-𝛽-carboline units from the corresponding 𝑁-indolylethylimides. (ias.ac.in)
Candida1
  • secretes a β-carboline (1-acetyl-β-carboline) preventing the pathogenic fungus Candida albicans to change to a more virulent growth form (yeast-to-filament transition). (wikipedia.org)
MeSH1
  • Carbolines" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (rush.edu)
Reduces1
  • Thanks to its complete formula and powerful dosages, Carboline Digest reduces digestive discomfort such as bloating. (euro-pharmas.com)
Tryptamines1
  • The biosynthesis of β-carbolines is believed to follow this route from analogous tryptamines. (wikipedia.org)
Pharmacological1
  • The pharmacological effects of specific β-carbolines are dependent on their substituents. (wikipedia.org)
Substances1
  • In the new investigation, they took a closer look at beta-carbolines and isoquinolines, toxins that resemble MPTP which the body produces from substances found in tobacco smoke, alcohol, and some foods. (upenn.edu)
Digest1
  • Carboline Digest from les 3 Chenes laboratory is indicated in case of digestive discomfort and bloating. (euro-pharmas.com)
Antioxidant1
  • Natural β-carbolines primarily influence brain functions but can also exhibit antioxidant effects. (wikipedia.org)
Buspirone1
  • Buspirone (0.03-0.3 mg/kg), like the beta-carbolines, increased frequency and VE and, like the BZ agonists, decreased VT. (aspetjournals.org)
Group1
  • A member of the class of beta-carbolines that is 9H-beta-carbolin-2-ium substituted by a chloro group at position 6 and a methyl group at position 2. (zfin.org)
Humans1
  • Certain beta-carbolines are known to be hallucinogenic in humans, and several produce stimulus effects in animals similar to those of the classical hallucinogen 1-2,5-dimethoxy-4-methylphenyl-2-aminopropane DOM. (erowid.org)
Main1
  • Both DMT and beta-carbolines, the main psychoactive ingredients in ayahuasca, may protect and restore parts of the brain. (onlinepsychedelicshome.com)
Complex1
  • Carboline levert Pyrolite en Perlifoc HP brandwerende mortels aan het Crescent Tower Complex, naast het Formule 1-circuit, in het Azerbeidzjaanse Bakoe. (paintdeals.com)
Study1
  • Study of the cis to trans isomerization of 1-phenyl-2,3-disubstituted tetrahydro-beta-carbolines at C(1). (academictree.org)
Primary1
  • The primary active ingredient in this part of the plant is N, N-DMT and there is also a small amount of β-carbolines. (thepsychedelicsshop.com)
(carboline.com)
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