- Three-dimensional pharmacophore hypotheses of octopamine/tyramine agonists which inhibit [1-14C]acetate incorporation in Plodia interpunctella
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Three-dimensional pharmacophore hypotheses were built from a set of 36 octopamine (OA)/tyramine (TA) agonists responsible for the inhibition of sex-pheromone production in Plodia interpunctella. Among the ten chemical-featured models generated by a program Catalyst/Hypo, hypotheses including hydrogen-bond acceptor (HBA), hydrogen-bond acceptor aliphatic (HBAl), hydrophobic (Hp), hydrophobic aromatic (HpAr) and hydrophobic aliphatic (HpAl) features were considered to be important and predictive in evaluating OA/TA agonists. Active agonists mapped well onto all the features of the hypothesis such as HBA, HBAl, Hp, HpAr and HpAl features. On the other hand, inactive compounds were shown to be poorly capable of achieving an energetically favorable conformation shared by the active molecules in order to fit the 3-D chemical-feature pharmacophore models. Those hypotheses are considered to be used in designing new leads for hopefully more active compounds. Further research on the comparison of models from the agonists may help elucidate the mechanisms of OA/TA receptor-ligand interactions.
- Hirashima, Akinori,Eiraku, Tomohiko,Shigeta, Yoko,Kuwano, Eiichi
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- Three-dimensional common-feature hypotheses for octopamine agonist 2-(arylimino)imidazolidines
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Three-dimensional pharmacophore hypotheses were built from a set of 10 octopamine (OA) agonist 2-(Arylimino)imidazolidines (AIIs), 2-(Arylimino)thiazolidines (AITs) and 2-(Arylimino)oxazolidines (AIOs). Among the 10 common-featured models generated by program Catalyst/HipHop, a hypothesis including a ring aromatic (RA), a positive ionizable (PI) and three hydrophobic aliphatic (HpA1) features was considered to be important in evaluating the OA-agonist activity. Active OA agonist 2,6-Et2 AII mapped well onto all the RA, PI and HpAl features of the hypothesis. On the other hand, less active compounds were shown to be difficult to achieve the energetically favorable conformation which is found in the active molecules in order to fit the 3-D common-feature pharmacophore models. Taken together, 2,6-Et2-Ph and foramidine structures are important as OA agonists. The present studies on OA agonists demonstrate that a RA, a PI and three HpAl sites located on the molecule seem to be essential for OA-agonist activity. Copyright
- Hirashima, Akinori,Morimoto, Masako,Kuwano, Eiichi,Taniguchi, Eiji,Eto, Morifusa
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p. 117 - 123
(2007/10/03)
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- TREATMENT OF URINARY INCONTINENCE BY ADMINISTRATION OF ALPHA 1L-ADRENOCEPTOR AGONISTS
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The present invention relates to the use of α lL-agonists for treating urinary incontinence.
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- A probe for octopamine receptors: Synthesis of 2-[(4-azido-2,6-diethylphenyl)imino]imidazolidine and its tritiated derivative, a potent reversible-irreversible activator of octopamine-sensitive adenylate cyclase
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In order to develop an irreversible ligand for octopamine receptors, a highly potent azido-substituted 2-(phenylimino)imidazolidine (NC-5Z, 8) and its tritiated derivative (3H-NC-5Z, 11) have been designed and synthesized. Under reversible-binding conditions, NC-5Z is 50-100-fold more potent than octopamine in activating octopamine-sensitive adenylate cyclase in a variety of tissues. After photolysis, 3H-NC-5Z binds irreversibly to cell membranes, and this binding is reduced by preincubation with octopamine agonists and antagonists but not by norepinephrine, dopamine, serotonin, or histamine. NC-5Z should be useful both as a potent reversible octopamine agonist and as an affinity probe for characterizing and isolating octopamine-receptor proteins.
- Nathanson,Kaugars
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p. 1795 - 1799
(2007/10/02)
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- Method of lowering intraocular pressure using phenylimino-imidazoles
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A method is provided of treating glaucoma in a patient which comprises administering, preferably as eye drops, an effective amount of the compound STR1 which is preferably in the form of its hydrochloride. The compound is administered preferably in the form of a sterile pharmacologically acceptable solution which contains from 0.1 to 5, and more preferably 0.1 to 2.0, percent by weight of said compound. The patient preferably obtains the anti-glaucoma agent in the form of a kit which comprises the sterile pharmacologically acceptable solution and an eyedropper for dispensing said sterile pharmacologically acceptable solution to the affected eyes of a patient suffering from glaucoma.
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- Method for lowering intraocular pressure using phenylimino-imidazoles
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2-(Trisubstituted phenylimino)-imidazole compounds also known as 2-(trisubstituted anilino)-1,3 diazacyclopentene-(2) compounds are used to lower intraocular pressure.
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- 2-(Trisubstituted phenylimino)-imidazolines
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2-Trisubstituted Phenylimino-imidazolines also known as 2-(trisubstituted anilino)-1,3 diazacyclopentene-(2) compounds and their use for lowering intraocular pressure are disclosed.
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