1992
DOI: 10.1016/s0960-894x(00)80540-5
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SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndrome

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Cited by 26 publications
(16 citation statements)
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“…29 Among the prepared compounds, BMS-193884 (ET A K i ϭ 1.4 nM; ET B K i ϭ 18,700 nM) showed promising hemodynamic effects in a phase II clinical trial for congestive heart failure. [31][32][33] Similarly, chemical variations of the D 2 /D 3 non-selective benzamide sulpiride ( Figure 6.12 ) led to compound Do 897, a selective and potent D 3 receptor partial agonist. The bioavailability of this compound is 100% in rats and it exhibits oral activity already at a 3 μ M/kg dosing.…”
Section: E New Leads From Old Drugs: the Sosa Approachmentioning
confidence: 99%
“…29 Among the prepared compounds, BMS-193884 (ET A K i ϭ 1.4 nM; ET B K i ϭ 18,700 nM) showed promising hemodynamic effects in a phase II clinical trial for congestive heart failure. [31][32][33] Similarly, chemical variations of the D 2 /D 3 non-selective benzamide sulpiride ( Figure 6.12 ) led to compound Do 897, a selective and potent D 3 receptor partial agonist. The bioavailability of this compound is 100% in rats and it exhibits oral activity already at a 3 μ M/kg dosing.…”
Section: E New Leads From Old Drugs: the Sosa Approachmentioning
confidence: 99%
“…Three simple changes in the structure of minaprine (Fig. 5) like shifting of the methyl group from the 3-to the 4-position (Compound 1), substitution of the morpholine by a tropane (Compound 2), and introduction of an hydroxyl group in the ortho position of the phenyl ring (Compound 3) eliminated the dopaminergic and serotoninergic activities and improved the partial agonistic cholinergic activity of compound 3 [26][27][28]. The noteworthy result was the total abolition of initial activity of minaprine on the dopaminergic and serotoninergic transmission in the final compound 3.…”
Section: Conversion Of Antidepressant Minaprine To a Muscarinic M1 Partial Agonistsmentioning
confidence: 99%
“…In addition to reinforcing serotonergic and dopaminergic transmission, this amino-pyridazine possesses weak affinity for muscarinic M 1 , receptors (K i = 17 lM). Simple chemical variations allowed the dopaminergic and serotonergic activities to be abolished, and the cholinergic activity to be boosted to nanomolar concentrations [36][37][38]. …”
Section: Cholinergic Agonistsmentioning
confidence: 99%