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Monographs of fragrance chemicals and extracts that have caused contact allergy / allergic contact dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Acetyl hexamethyl tetralin is a white crystalline solid; its odor type is musk and its odor at 100% is described as ‘strong sweet amber fruity musk powdery’ (www.thegoodscentscompany.com). It is used as a fragrance in cosmetics, detergents, fabric softeners, household cleaning products and air fresheners (U.S. National Library of Medicine). Acetyl hexamethyl tetralin is a synthetic chemical, not found in nature (and consequently not in essential oils).
Serotonin Modulation of Gastrointestinal Motility
Published in T.S. Gaginella, J.J. Galligan, SEROTONIN and GASTROINTESTINAL FUNCTION, 2020
Marcello Tonini, Fabrizio De Ponti
As mentioned above, in the guinea pig GI tract, 5-HT causes presynaptic and prejunctional inhibition of cholinergic and noncholinergic excitatory transmitter release, and membrane hyperpolarization in a subset of enteric neurons. Since these inhibitory effects are mimicked by 5-CT and 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and reduced with high affinity by antagonists such as spiperone, buspirone and NAN-190, the receptor involved is probably the 5-HT1A subtype.16,18,59–63 The inhibition of excitatory neural transmission mediated by 5-HT1A receptor activation might reasonably explain the reduction of peristaltic activity (which followed an initial stimulation) caused by 5-HT administration to the serosal side in the guinea pig ileum.64 In contrast with this hypothesis, 5-CT (like 5-HT) was found to cause a substantial stimulation of peristaltic activity in the same preparation.43 However, it is noteworthy to point out that 5-CT may also behave as a 5-HT4 receptor agonist in the guinea pig ileum42 and may stimulate ileal peristaltic activity by this mechanism.43Table 1 summarizes the effects mediated by 5-HT1 receptors in the GI tract in vitro.
Dopamine Receptors, Signaling Pathways, and Drugs
Published in Nira Ben-Jonathan, Dopamine, 2020
The development, structure, pharmacology, and therapeutic efficacy of selective drugs for DAR subtypes have been covered in several extensive reviews [61,72]. In spite of a certain overlap in the binding affinities of various drugs to the three D2R-like, some antagonists, mostly derived from a piperazine structure, show higher selectivity for D3R or D4R over D2R. Nonetheless, the development of potent and highly selective D3R or D4R agonists has been less successful. Few promising D3R agonists include tetralin analogs, while effective D4R agonists include modified acetamides and benzamides.
A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019)
Published in Expert Opinion on Therapeutic Patents, 2020
Unlike most researchers that focused on phenyl/heteroaryl-based hydroxamates, Forma Therapeutics (Forma) extended their interest into the discovery of spiro-fused tetraline/indane based hydroxamates containing aromatic caps (Figure 4(c)) (e.g. compounds 28–30) [102–104]. Biochemical assays indicated that IC50 values against HDAC6 were lower than 100 nM, but no further biological information was reported in these patent applications. As 2-aminotetralin has been demonstrated as a useful linker to develop potent and selective HDAC6/8 dual inhibitors [105], compounds 28–30 might be expected to exhibit moderate HDAC8 activity. Subsequently, Forma also developed hydroxamate analogs bearing tetrahydrobenzo-1,4-oxazepine or tetrahydrobenz-1,5-oxazocine groups (e.g. 31–33) as linkers [106–108]. The exploration of the 1,4-oxazepine class was based on an investigation of different substituents on the nitrogen atom followed by another patent focusing on derivatives bearing various amide substituents. Most compounds contain an S-configured stereocenter bearing an aromatic ring at the C3 position and exhibited reasonably good HDAC6 inhibitory activity (IC50 < 100 nM). However, their selectivity over other HDAC isoforms is unknown. The 1,5-oxazocine class was developed in a similar manner, and some of the compounds displayed nanomolar potency against HDAC6 (IC50 < 100 nM).
Mineral oil in food, cosmetic products, and in products regulated by other legislations
Published in Critical Reviews in Toxicology, 2019
Ralph Pirow, Annegret Blume, Nicole Hellwig, Matthias Herzler, Bettina Huhse, Christoph Hutzler, Karla Pfaff, Hermann-Josef Thierse, Tewes Tralau, Bärbel Vieth, Andreas Luch
Concerning the carcinogenicity of MOAH, information was derived from animal studies with PAHs (including methylated derivatives), C10–C15 (predominantly C12) branched-chain alkyl benzene (i.e. dodecylbenzene), a partially hydrogenated aromatic hydrocarbon (tetralin), mineral oils, and other petroleum-derived substances. Several food-grade mineral oils and waxes, which very likely contained (but had not been tested for) MOAH, were not carcinogenic in chronic dietary studies (see Section “Carcinogenicity of PAHs and MOAH”). No data are available for the dietary exposure to non-food grade mineral oils. Dermal and inhalation studies were therefore used instead. The carcinogenicity of petroleum-derived materials appeared to be in general due to the presence of PAC containing three or more aromatic rings. The CONTAM Panel concluded that many MOAH with three or more aromatic rings and little or no alkylation can be bioactivated to genotoxic carcinogens. C10–C15 branched-chain alkyl benzene, which was taken as a representative of highly alkylated MOAH, has a skin irritation-related promotion effect (see Section “Carcinogenicity of PAHs and MOAH”). Some simple MOAH such as naphthalene (C10) are carcinogenic by a non-genotoxic mode of action, involving cytotoxicity and a proliferative response.
5-HT1A receptor ligands and their therapeutic applications: review of new patents
Published in Expert Opinion on Therapeutic Patents, 2018
Jakub Staroń, Ryszard Bugno, Adam S. Hogendorf, Andrzej J. Bojarski
In turn, researchers at Northeastern University developed a group of compounds [70,71] (Figure 4) that modulate serotonin receptors in the periphery, which might be useful in therapies for gastrointestinal and cardiopulmonary disorders. The design was based on a tetralin core substituted at C2 with a trialkyl amino moiety and with an aryl or cycloalkyl moiety at C5. Additional substituents at C7 and C8 might also be included. The compounds possessed a positive charge by design, which made them unable to cross the blood-brain barrier. Unfortunately, detailed biological activity data were only provided for 5-HT7R (the most active compound for 5-HT7R Ki = 6 nM, R1 = 2-fluorophenyl, *(S)-trimethylamino), and authors only briefly stated in the description of the invention that some compounds bound to 5-HT1AR with a “…100-fold higher affinity than a corresponding enantiomer.”