Disease relevance of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• RESULTS: Dapiprazole drops produced a Horner's miosis, but pupils were equally small after induction of anesthesia [1].
• The authors hypothesized that the reflex was primarily a spinal sympathetic reflex that would be blocked by topical application of the alpha1-adrenergic blocking agent dapiprazole and that it would be present in organ donors with intact spinal reflexes and no history of hypoxia [2].
• The results showed a significant reversal of mydriasis by intraocular dapiprazole, especially with the 0.25% and 0.5% concentrations which did not differ significantly in effectiveness and safety [3].
• No difference in the toxicity parameters (inflammatory score, corneal thickness, endothelial cell counting, aqueous humor protein concentration, and intraocular pressure) was found between dapiprazole-treated eyes and saline-solution-treated eyes [4].
• All of our subjects exhibited conjunctival hyperemia after the administration of dapiprazole [5].

High impact information on 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• Ibopamine was administered with and without the alpha-adrenergic antagonist dapiprazole, and its effects were compared with those of tropicamide, with and without dapiprazole in a double-masked, randomized, crossover design [6].
• SETTING: Department of Ophthalmology, Johannes Gutenberg-University, Mainz, Germany. METHODS: In randomized prospective study, 19 healthy volunteers received 2 ophthalmic solutions, dapiprazole and brimonidine, 1 in each eye, for intraindividual comparison [7].
• Ninety patients were enrolled in a double-blind study and divided into three groups of 30 eyes; each group received balanced salt solution (control), 0.25% dapiprazole, or 1% acetylcholine [8].
• Intraocular dapiprazole for the reversal of mydriasis after extracapsular cataract extraction with intraocular lens implantation. Part I: Dose-response correlation [3].
• Although neither the use of dapiprazole nor the degree of iris color/pigmentation was significantly related to visual acuity or glare discomfort, there was a clear trend that these visual measures were affected to a greater degree in subjects with dark brown (primarily Blacks) rather than light brown irides [9].

Chemical compound and disease context of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• In this preliminary experimental animal study, we investigated the intracameral use of 0.2 ml of 0.005%, 0.0075%, 0.01%, and 0.05% dapiprazole to reverse mydriasis by 10% phenylephrine plus 0.5% tropicamide [4].
• Dose-response study of dapiprazole HCl in the reversal of mydriasis induced by 2.5% phenylephrine [10].
• RESULTS: Dapiprazole and pilocarpine together induced miosis significantly faster than each drug alone, showing additive effects [11].
• METHODS: Dapiprazole 0.5% eye drops were administered 3 times daily as adjunctive therapy to 16 pigmentary glaucoma patients in addition to timolol 0.5% eye drops twice daily [12].
• Corneal endothelial toxicity of dapiprazole hydrochloride [13].

Biological context of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• In addition, suppression of diuresis was obtained by combining doses of dapiprazole and morphine or naloxone that were devoid of antidiuretic effects when administered independently [14].
• At doses administered (3-6 mg/kg, IP), dapiprazole had no effect on basal food and water intake or on diuresis [14].
• Ocular pharmacokinetics of dapiprazole [15].

Anatomical context of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• Dapiprazole had relatively high affinity both at rat vas deferens alpha 1A-adrenoceptors (pA2 = 7.93) and at rat aortic alpha 1D-adrenoceptors (pA2 = 8.26), whereas its affinity at guinea-pig splenic alpha 1B-adrenoceptors (pA2 = 7.13) was lower [16].
• The Ca2+-induced contractions of K+-depolarized ileum were also inhibited by dapiprazole [17].
• The results suggest that dapiprazole might inhibit Ca2+ entry through both voltage-and receptor-operated channels of the smooth muscle membrane [17].

Associations of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene with other chemical compounds

• A single drop of dapiprazole has a clinical effect equivalent to the 2 + 2 drop regimen in eyes dilated with 2.5% phenylephrine, which should improve the cost-effectiveness of this mydriolytic agent [10].
• Trazodone, unlike dapiprazole, also inhibits binding to serotonin2 (5-HT2) receptors [18].

Gene context of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• The absence of induced myopia and the lack of dangerous vitreoretinal tractions on retinal periphery make dapiprazole a safe method to reduce exercise-induced pigment dispersion [19].
• PURPOSE: The authors investigated the use of dapiprazole, an alpha-adrenergic blocking agent, in preventing pigment release and IOP increase after exercise in patients affected with PDS [19].

Analytical, diagnostic and therapeutic context of 9-[2-[4-(o-tolyl)pyrazin-1-yl]ethyl]-1,7,8-triazabicyclo[4.3.0]nona-6,8-diene

• In organ donors, the authors measured pupil size after high-intensity tetanic electric stimulation and in dapiprazole-blocked and -unblocked pupils after surgically induced nociception [2].
• Dapiprazole, an alpha-blocking miotic drug, was used intracamerally at the end of extracapsular cataract extraction with posterior chamber intraocular lens (IOL) implantation [3].
• The double-blind study included 120 patients divided into four groups of 30 eyes; the groups received balanced salt solution, 0.125%, 0.25%, or 0.5% intraocular dapiprazole after IOL implantation and before suturing [3].
• CONCLUSION: Co-administration of dapiprazole and pilocarpine at the end of the eye examination will induce fast pupillary constriction, which might be useful in preventing the development of an acute attack of angle-closure glaucoma in patients with anatomically narrow angles [11].
• Contact lenses increase the duration of effects of dapiprazole [20].

References