16234-95-0Relevant academic research and scientific papers
Study on zwitter-ionization of drugs. II. Synthesis and pharmacological activity of some N-[3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)propyl]-N- methylamino- and N-[3-(6H-dibenz[b,e]oxepin-11-ylidene)propyl]-N-methylamino- alkanoic acid derivatives and related compounds
Muramatsu,Sawanishi,Iwasaki,Kakiuchi,Ohashi,Kato,Ito
, p. 1987 - 1993 (1993)
A series of N-[3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)propyl]-N- methylamino- (6a) and N-[3-(6H-dibenz-[b,e]oxepin-11-ylidene)propyl]-N- methylamino-alkanoic acid derivatives (6b) and related compounds (6c-f) were synthesized and examined for pharmacological activities in vitro, i.e., inhibitory effect on monoamine [noradrenaline (NA) and 5-hydroxytryptamine (5-HT)] uptake, inhibitory effect on 5-HT-, histamine-, acetylcholine- and NA-induced contraction, and binding affinity for α2-adrenoceptor and dopamine D2-receptor. In vitro tests indicated that zwitter-ionization was capable of maintaining H1-antihistaminic activity while greatly reducing other pharmacological activities. Further, 6a-f showed much stronger inhibitory effects on compound 48/80-induced lethality in rats than did the corresponding N,N-dimethylamines (2a-f). 3-[N-[3-(6H-Dibenz[b,e]oxepin-11- ylidene)propyl]-N-methylamino]-propionic acid (6b-2), selected as a candidate antiallergic agent of a new type, equally potent in rats and guinea-pigs, exhibited strong inhibitory effects on 48 h homologous passive cutaneous anaphylaxis (PCA) in rats (ED50=0.019 mg/kg, p.o.) and on histamine- induced bronchoconstriction in anesthetized guinea-pigs (ED50=0.0067 mg/kg, p.o.).
COMPOSITIONS AND METHODS FOR THE TREATMENT OF FIBROMYALGIA PAIN
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Paragraph 0125, (2015/04/28)
The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain.
