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This paper present ultraviolet-visible absorption spectra of imazamethabenz-methyl (IMBM) (mixture of the isomers methyl 6-[(RS)-4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl]-m-toluate, m-imazamethabenz, and methyl 2-[(RS)-4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl]-p-toluate, p-imazamethabenz) and the corresponding carboxylic acid, imazamethabenz-acid (IMBA). The spectral characteristics are determined as functions of the pH. The appreciable absorbance in the visible (or near-ultraviolet) region of the spectra indicates ...
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Four 2-amino-3-methylimidazo[4,5-b][1,x]naphthyridines, x = 5-8 (6-9) have been obtained from aromatic aldehydes (11-14) and 2-amino-1-methyl-2-imidazolin-5-one (15) in one step. The N-1 - and N-3 -methyl isomers of 2-aminoimidazo-[4,5-b]quinoline (5 and 10) were prepared from 2-nitrobenzaldehyde via the isolated E-isomers of imidazolin-5-one (17) and imidazolin-4-one (20).. ...
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As described in the accompanying paper, the novel ligand S18327 (1-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperid-1-yl]ethyl}3-phenyl imidazolin-2-one) displays pronounced antagonist properties at α1-adrenergic receptors (ARs), serotonin [5-hydroxytryptamine (5-HT)2A], and D4 receptors, as well as less potent antagonist actions at α2-AR and D1and D2 receptors. Interestingly, the α2-AR antagonist properties of S18327 underlie a generalized enhancement of cerebral adrenergic transmission and a preferential facilitation of the activity of frontocortical compared with subcortical dopaminergic pathways. On the other hand, the inhibitory influence of S18327 on the activity of serotonergic neurons originating in the dorsal raphe nucleus may be attributed to its antagonist actions at α1-ARs. Notably, S18327 only weakly accelerates striatal turnover of dopamine (DA). In light of these observations, in the present study we examined the activity of S18327 in paradigms predictive of the control of ...
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Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific literature by Sumitomo Chemical as "β-adrenergic blocking, antiarrhythmic compound S-596". It is used in the treatment of high blood pressure and essential tremor. Recommended dosage is 10-30 mg per day. Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol. 79 (7): 585-593. doi:10.1139/cjpp-79-7-585. PMID 11478592. Takahashi, H; Yoshida, T; Nishimura, M; Nakanishi, T; Kondo, M; Yoshimura, M (September 1992). "Beta-3 Adrenergic Agonist, BRL-26830A, and Alpha/Beta Blocker, Arotinolol, Markedly Increase Regional Blood Flow in the Brown Adipose Tissue in Anesthetized Rats". Japanese Circulation Journal. 56 (9): 936-42. ...
Product Description Hot Sale Synephrine steroid for Losing Weight CAS 94-07-5 chemical Synephrine Details: CAS: 94-07-5 MF: C9H13NO2 MW: 167.21 EINECS: 202-300-9 Appearance: Light yellow to off-white fine powder Usage: used for rising blood pressure Product Categories: Plant Extract Synonyms: oxedrine;Synephrine;(+/-)-SYNEPHRINE;SYNEPHRINE;4-hydroxy-alpha-(methylaminomethyl)benzyl alcohol;AKOS NCG1-0008;1-[4-HYDROXYPHENYL]-2-METHYLAMINOETHANOL;AURORA KA-6561 Description: Synephrine is a kind of biological active substance, mainly extracted from the…
Product Description Hot Sale Synephrine steroid for Losing Weight CAS 94-07-5 chemical Synephrine Details: CAS: 94-07-5 MF: C9H13NO2 MW: 167.21 EINECS: 202-300-9 Appearance: Light yellow to off-white fine powder Usage: used for rising blood pressure Product Categories: Plant Extract Synonyms: oxedrine;Synephrine;(+/-)-SYNEPHRINE;SYNEPHRINE;4-hydroxy-alpha-(methylaminomethyl)benzyl alcohol;AKOS NCG1-0008;1-[4-HYDROXYPHENYL]-2-METHYLAMINOETHANOL;AURORA KA-6561 Description: Synephrine is a kind of biological active substance, mainly extracted from the…
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Pharmacological studies on synephrine date back to the late 1920s, when it was observed that injected synephrine raised blood pressure, constricted peripheral blood vessels, dilated pupils, stimulated the uterus, and relaxed the intestines in experimental animals.[37][37][61][62] Representative of this early work is the paper by Tainter and Seidenfeld, who were the first researchers to systematically compare the different effects of the two synephrine enantiomers, d- and l- synephrine, as well as of the racemate, d,l-synephrine, in various animal assays.[41] In experiments on anesthetized cats, Tainter and Seidenfeld confirmed earlier reports of the increase in blood pressure produced by intravenous doses of synephrine, showing that the median pressor doses for the isomers were: l-synephrine: 0.5 mg/kg; d,l-synephrine: 1.0 mg/kg; and d-synephrine: 2-20 mg/kg. These effects lasted 2-3 minutes, peaking at ~30 seconds after administration. l-Synephrine was thus the more potent enantiomer, with ...
If given by the intra-arterial route, the immediate effect of the hydrogenated alkaloids of ergot is unpredictable. Vasodilation is obtained in some patients only. However, it was found that in those cases who do not react, the vessels respond more easily to the release of sympathetic tone, proving that, nevertheless, the drug has had an (potential) effect, probably on the neurovascular apparatus. This effect could be demonstrated for many hours and is, therefore, of considerable therapeutic interest. Even with the higher local concentrations possible by the intra-arterial route, the hydrogenated alkaloids of ergot still did not exhibit any adrenolytic action on the peripheral blood vessels in man.. ...
Substitution reactions of (E)-11-(3-bromopropylidene)-6,11-dihydrodibenzo[b,e]thiepin (VIIIa) and its 2-chloro derivative VIIIb with 1-(2-hydroxyethyl)piperazine gave the title compounds IIIa and IIIb which afforded by treatment with acetic anhydride, decanoyl chloride and 3,4,5-trimethoxybenzoyl chloride the esters IVab-VIab. Reduction of the olefinic compounds IIIa and IIIb with hydrolytic acid resulted in the saturated amines IXa and IXb. The piperazine derivativeX was obtained by a substitution reaction of 2,11-dichloro-6,11-dihydrobenzo[b,e]thiepin with 1-(2-hydroxyethyl)piperazine. The amino alcohols IIIa and IIIb, as well as their acetates and 3,4,5-trimethoxybenzoates, are almost devoid of the CNS effects. The decanates Va and Vb have not the properties of the depot antipsychotics (neither antidepressants, nor neuroleptics). The saturated amino alcohol IXa showed some antihistamine, spasmolytic and adrenolytic effects.. ...
Atipamezole HCl is a selective ??2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for ??2A, ??2B, ??2C, ??1A and ??1B receptors respectively). Has been shown to be a brain penetrant.
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