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)

Carbolines are a type of chemical compound that contain a carbazole or dibenzopyrrole structure. These compounds have a variety of uses, including as pharmaceuticals and dyes. Some carbolines have been studied for their potential medicinal properties, such as their ability to act as antioxidants or to inhibit the growth of certain types of cells. However, it is important to note that many carbolines are also known to be toxic and can cause harm if ingested or otherwise introduced into the body. As with any chemical compound, it is essential to use caution when handling carbolines and to follow all safety guidelines to minimize the risk of exposure.

β-carboline Alekseyev RS, Kurki AV, Yurovskaya MA (2009). "γ-Carbolines and their hydrogenated derivatives. 1. Aromatic γ- ... γ-Carboline (5H-pyrido[4,3-b]indole), is a nitrogen containing heterocycle. A large number of derivatives are known with ... Part I: Comparison of some methods for the synthesis of α-, γ-, and δ-carbolines (a review)". Pharm Chem J. 44 (12): 654-678. ... Part 2: Comparison of some of the properties of α-, γ-, and δ-carbolines (Review)". Pharm Chem J. 45 (7): 389-400. doi:10.1007/ ...
... 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 ...
... (9-Me-BC) is a heterocyclic amine of the β-carboline family, and a research chemical. 9-Me-BC is a ... Gruss, M; Appenroth, D; Flubacher, A; Enzersperger, C; Bock, J; Fleck, C; Gille, G; Braun, K (2012). "9-Methyl-β-carboline- ... It may be prepared by performing the Eschweiler-Clarke reaction on freebase β-carboline (norharmane)[citation needed] In vitro ... Hamann, J; Wernicke, C; Lehmann, J; Reichmann, H; Rommelspacher, H; Gille, G (2008). "9-Methyl-β-carboline up-regulates the ...
Substituted heterocycle fused gamma-carbolines. Patent US 6552017 Tomesch JC, et al. Preparation of 4-((6BR,10AS)-3-methyl-2,3, ...
Inverse allosteric agonists: beta-carbolines (ex. Harmine, Harmaline, Tetrahydroharmine). Second-order modulators: (−)‐ ...
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 ...
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. ...
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 ... or β-carbolines (like Peganum harmala). Pharmahuasca (pharmaceutical ayahuasca). Indicate the pills produced with freebase DMT ... as demonstrated by a bundle containing the residue of the beta-carboline harmine and various other preserved psychoactive ...
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. ...
"Synthesis of α-Carboline". Org. Synth. 93: 272. doi:10.15227/orgsyn.093.0272. "Buchwald-Hartwig Cross Coupling Reaction". ...
Chapman AG, De Sarro GB, Premachandra M, Meldrum BS (September 1987). "Bidirectional effects of beta-carbolines in reflex ...
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 ...
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 ...
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 ... The coincident occurrence of β-carboline alkaloids and serotonin in Peganum harmala indicates the presence of two very similar ... US 5591738, Lotsof, Howard S., "Method of treating chemical dependency using β-carboline alkaloids, derivatives and salts ...
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- ...
... 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- ...
S. A. Adesanya; M. Chbani; M. Païs; C. Debitus (1992). "Brominated β-Carbolines from the Marine Tunicate Eudistoma album". J. ...
v t e (Articles lacking in-text citations from September 2013, All articles lacking in-text citations, Beta-Carbolines, All ... Oxopropalines are novel cytocidal beta-carbolines isolated from Streptomyces. Abe N, Nakakita Y, Nakamura T, Enoki N, Uchida H ...
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 ( ...
Levels of beta-carbolines and hordenine have also been reported. Lee, Sangtae; Chang, Kae Sun, eds. (2015). English Names for ...
"Exudation of fluorescent b-carbolines from Oxalis tuberosa L. roots". Phytochemistry. 61 (5): 539-543. Bibcode:2002PChem..61.. ...
Duka, T; Edelmann, V; Schütt, B; Dorow, R (1988). "β-Carbolines as Tools in Memory Research: Human Data with the β-Carboline ZK ... ZK-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 ... Dorow, R; Duka, T; Höller, L; Sauerbrey, N (1987). "Clinical perspectives of beta-carbolines from first studies in humans". ...
... 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 ...
"Mechanisms of DNA damage by photoexcited 9-methyl-β-carbolines". Organic & Biomolecular Chemistry. 11 (32): 5300-5309. doi: ...
The beta-carboline hallucinogens of South America. Journal of Psychoactive Drugs 14(3): 205-220. Grisebach, A.H.R. 1849. ...
... , 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 ...
... 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). ...
Gremmen, C.; Willemse, B.; Wanner, M. J.; Koomen, G.-J. (2000). "Enantiopure Tetrahydro-β-carbolines via Pictet-Spengler ...
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 ...
... 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). ...
β-carboline Alekseyev RS, Kurki AV, Yurovskaya MA (2009). "γ-Carbolines and their hydrogenated derivatives. 1. Aromatic γ- ... γ-Carboline (5H-pyrido[4,3-b]indole), is a nitrogen containing heterocycle. A large number of derivatives are known with ... Part I: Comparison of some methods for the synthesis of α-, γ-, and δ-carbolines (a review)". Pharm Chem J. 44 (12): 654-678. ... Part 2: Comparison of some of the properties of α-, γ-, and δ-carbolines (Review)". Pharm Chem J. 45 (7): 389-400. doi:10.1007/ ...
... Evid Based Complement Alternat Med. 2009; 6(3):315-6 (ISSN ... Maca, a plant native to the Peruvian highlands, contains (1R,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid ( ... MTCA). The family of the tetrahydro-beta-carbolines has been associated with both biologically helpful and harmful compounds. ...
... we report the design and synthesis of novel amide-type hybrid molecules based on anthranilic acid and quinoline or β-carboline ... 3-(1,2,3-Triazol-4-yl)-β-Carbolines and 3-(1H-Tetrazol-5-yl)-β-Carbolines: Synthesis and Evaluation as Anticancer Agents. ... Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity Maja Beus 1 , Leentje ... Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity Maja Beus et al. Mol ...
Carboline Wins 9th Consecutive St. Louis Top Workplaces Award ... For the ninth year in a row, Carboline has been recognized as a ... "Even with the significant changes we made collectively as a team, Carboline saw an impressive 11-point increase in employee ... Louis Top Workplace for the ninth consecutive year," said David Morlen, Vice President of Human Resources at Carboline. "This ...
... α-Carbolines and Nucleosides Containing the α-Carboline Framework. Synthesis , 2009, 14, 2393-2402 ... Fluorinated benzofuro[2,3-b]pyridines, benzothieno[2,3-b]pyridines and 9H-pyrido[2,3-b]indoles (α-carbolines) were synthesized ... α-Carbolines and Nucleosides Containing the α-Carboline Framework ... the preparative approach towards a set of nucleosides and nucleoside mimetics bearing the α-carboline framework was elaborated. ...
9H-beta-carboline-3-carboxylic acid - cas 74214-63-4, synthesis, structure, density, melting point, boiling point ... Tags: melting point of 9H-beta-carboline-3-carboxylic acid - 74214-63-4 , boiling point of 9H-beta-carboline-3-carboxylic acid ... 74214-63-4 , density of 9H-beta-carboline-3-carboxylic acid - 74214-63-4 , refractive index of 9H-beta-carboline-3-carboxylic ...
Here, we present the enantioselective synthesis of small-molecule compounds based on the tetrahydro-beta-carboline core system ... Enantioselective synthesis and biological investigation of tetrahydro‐β‐carboline‐based HDAC6 inhibitors with improved ...
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Ethylbeta-carboline with the InChIKey YTQRHYCHEIXUIU-UHFFFAOYSA-N. ... CH$NAME: Ethylbeta-carboline. CH$COMPOUND_CLASS: Harmala alkaloids. CH$FORMULA: C13H12N2. CH$EXACT_MASS: 196.253. CH$SMILES: ... RECORD_TITLE: Ethylbeta-carboline; LC-ESI-QTOF; MS2. DATE: 2019.03.28. AUTHORS: Tetsuya Mori, Center for Sustainable Resource ...
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Austin to discuss the rich world of beta-Carbolines. ... The beta-Carbolines come from Syrian rue, the Espand. You, and ... Exploring the physiological effects of beta-Carbolines.. *Shauheen and Jonathans personal experiences with beta-Carbolines and ... But back again to this effect and effect of beta-Carbolines.. 0:31:44.6 Shauheen Etminan: This is like the whole thing is all ... What are beta-Carbolines? Theyre an overlooked class of compounds in the world of psychedelics that are often overshadowed by ...
Nullifire SC803 jest ogniochronną farbą pęczniejącą przeznaczoną do zabezpieczenia ogniochronnego konstrukcji stalowych z profili otwartych i zamkniętych. Powłoka ta ma zadanie utrzymanie odporności ogniowej i nośności konstrukcji stalowych do momentu ugaszenia pożaru lub ewakuacji budynku. Farba ogniochronna Nullifire SC803 jest dostarczana w stanie gotowym do użycia. Jako ogniochronna farba wodorozcieńczalna charakteryzuje się niskim czasem schnięcia.
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Products / Firestop / Carboline / Carboline A/D Firefilm III Fireproofing. Carboline A/D Firefilm III Fireproofing. ...
Copyright © 2022 Carboline Polska Sp. z o. o. Słoneczna 29, 83-021 Wiślina, POLAND ...
  • Carboline Plasite 4500 is a solvent-free epoxy coating. (cpphenolics.nl)
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  • Carboline is part of RPM International Inc., a $6.1 billion, multinational company with subsidiaries that are world leaders in specialty coatings, sealants, building materials and related services. (seniorsinjobs.com)
  • Tetrahydro-β-carboline (THBC) derivatives are frequently used as drugs or drug candidates. (chemistryviews.org)
  • Zhihui Shao, Henan Agricultural University, Zhengzhou, China, and colleagues have developed an efficient and green method for the synthesis of tetrahydro-β-carbolines via the dehydrogenative coupling of alcohols with tryptamine (general reaction pictured below). (chemistryviews.org)
  • The distribution of radioactivity after intravenous injection of 14C-labelled 1,2,3,4-tetrahydro-beta-carboline (THBC) and 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeO-THBC) was studied on mice by whole-body autoradiography and by liquid scintillation counting (LSC). (erowid.org)
  • These β-carbolines are formed from tryptophan/tryptamines, with tetrahydro-β-carbolines as intermediates. (rsc.org)
  • Fermented plant foods are particularly rich in tetrahydro-β-carbolines, while thermally processed foods are richer in β-carbolines, with coffee attaining the highest amounts. (rsc.org)
  • No report of tetrahydro-β-carbolines in roasted coffee are found, but the norharman and harman amounts are highly variable, depending on the coffee species ( C. arabica L and C. canephora Pierre), roast degree, and beverage type. (rsc.org)
  • Several techniques have been employed to analyze β-carbolines and tetrahydro-β-carbolines, in coffee and other food matrices. (rsc.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)
  • Active substances include the hallucinogen N-N-dimethyltryptamine and beta-carboline alkaloids such as harmine and harmaline. (cdc.gov)
  • This preparation contains the psychedelic 5-HT 2A receptor agonist N,N-dimethyltryptamine (DMT) from P. viridis, plus β-carboline alkaloids with monoamine-oxidase-inhibiting properties from B. caapi. (nih.gov)
  • Acanthostrongylophora ingens is known to be rich with pyrimidine b-carboline and manzamine-type alkaloids. (phcog.com)
  • γ-Carbolines and their hydrogenated derivatives. (wikipedia.org)
  • carboline Derivatives as Anticancer and Cancer-chemopreventive Agents. (umassmed.edu)
  • Penetrating primer/sealer for use on concrete substrates and Carboline Pyrocrete Fireproofing products. (carboline.com)
  • Carboline is proud to announce the release of Hydroplate linings, a new product line specifically designed for the water and wastewater markets. (bicmagazine.com)
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  • ASTM D4541 adhesion pull testing of Carboline Carbomastic 15 over a marginally prepared barge surface achieved impressive results. (carboline.co.uk)
  • Carboline inspectors followed an ocean supply vessel closely for over a decade to analyze the performance of Carbomastic 15 applied to its hull. (carboline.co.uk)
  • Carbolines" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
  • Carboline has a strong commitment to the protective coatings industry and takes an active role in professional organizations that focus on corrosion control, water transmission, and fire protection. (transparencycatalog.com)
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  • Coffee is the major dietary source of harman and norharman, two β-carbolines with biological activities that might be implicated in coffee health effects. (rsc.org)
  • 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)
  • This chapter addresses the current knowledge on β-carboline analysis and content in coffee, compared to other food sources, and explores technological factors that might influence their amounts in coffee and other foods. (rsc.org)
  • This graph shows the total number of publications written about "Carbolines" by people in this website by year, and whether "Carbolines" was a major or minor topic of these publications. (umassmed.edu)
  • Large selection ✓ Top brands ✓ Discover & save Carboline wood protection on farbenloewe.de ➤ Order now! (farbenloewe.com)
  • Affinities Ki values of the beta-carbolines ranged from about 100 nM to greater than 10,000 nM depending upon the degree of saturation of the pyridyl ring, and upon the presence and location of methoxy substituents in the benzenoid ring. (erowid.org)
  • Carboline is an Equal Opportunity Employer that values the strength diversity brings to the workplace. (seniorsinjobs.com)
  • In the present study, we examined the binding of 15 beta-carbolines at rat 5-HT2A and 5-HT2C receptors. (erowid.org)
  • The family of the tetrahydro-beta-carbolines has been associated with both biologically helpful and harmful compounds. (medscape.com)
  • 12. Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP. (nih.gov)
  • Carboline delivers… The Right Products. (carbolineindia.com)
  • however, the suspected decomposition products, the beta-carbolines, exhibit a variety of biologic properties (7). (cdc.gov)
  • 14. Synthesis and biological evaluation of novel 3,9-substituted β-carboline derivatives as anticancer agents. (nih.gov)
  • The Pictet-Spengler reaction is an important class of name reaction employed extensively for the synthesis of tetrahydro-β-carboline [1-9] . (beilstein-journals.org)
  • 1. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. (nih.gov)
  • 4. Computational & experimental evaluation of the structure/activity relationship of β-carbolines as DYRK1A inhibitors. (nih.gov)
  • 8. Discovery of 4-benzylamino-substituted α-carbolines as a novel class of receptor tyrosine kinase inhibitors. (nih.gov)
  • They explain the unique neurobiological and subjective effects of beta-Carbolines, including when combined with tryptamine-containing substances such as in an Ayahuasca brew. (thethirdwave.co)
  • Even with the significant changes we made collectively as a team, Carboline saw an impressive 11-point increase in employee connectedness to the company," he added. (coatingspromag.com)
  • By applying advanced scientific tools in chemistry, neurophysiology and psychopharmacology to the study of the Iranian inebriating elixir of truth, Haoma, his team discovered neurological health properties in beta-carbolines and developed Magi ancestral nootropic supplements. (thethirdwave.co)