Repinotan ( BAYx3702 ), a chemical compound, an aminomethylchroman derivative, is a highly potent selective selective 5-HT1A receptor agonist with high efficiency. [1] [2] It has neuroprotective effects in animal experiments [3] [4] [5] and has been studied in humans to reduce brain damage during skull injuries. [6] It was then investigated up to phase II with the goal of treating ischemic stroke, but although the side effects were small and consisted mainly of nausea, repinotan showed insufficient clinical efficacy to justify the cost of further studies. [7] [8] [9] However, repinotan continues to be investigated for other purposes. In particular, it was found that it can be effective in reducing the respiratory depression caused by morphine, although it slightly reduces its analgesic effect. [ten]
| Repinotan | |
|---|---|
 | |
| Chemical compound | |
| IUPAC | (R) - (-) - 2- [4 - [(chroman-2-ylmethyl) -amino] -butyl] -1,1-dioxo-benzo [d] isothiazolone |
| Gross formula | C 21 H 24 N 2 O 4 S |
| Molar mass | 400.491 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Route of administration | |
| Oral | |
Content
History
Chemical and physical properties
2-D Structure of Repinotan Hydrochloride
Synthesis
The first reaction scheme
Second Reaction Scheme
Third Reaction Scheme
Mechanism of Action
Pharmacology
Pharmacodynamics
Pharmacokinetics
Potential effects of gender, age, and weight
Treatment
Ischemic Stroke
Removing Opioid-Depressed Breathing Depression
Repinotan Dose Relationship to Nociception
Other medicines for similar purposes
Side Effects
Initial Expectations and Real Situation
See also
- Robalsotan
- Piclozotan
- Naluzotan
Notes
- β De Vry J. , Schohe-Loop R. , Heine HG , Greuel JM , Mauler F. , Schmidt B. , Sommermeyer H. , Glaser T. Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist . (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 284, no. 3 . - P. 1082-1094. - PMID 9495870 .
- β Dong J. , de Montigny C. , Blier P. Full agonistic properties of BAY x 3702 on presynaptic and postsynaptic 5-HT1A receptors electrophysiological studies in the rat hippocampus and dorsal raphe. (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 286, no. 3 . - P. 1239-1247. - PMID 9732384 .
- β Alessandri B. , Tsuchida E. , Bullock RM The neuroprotective effect of a new serotonin receptor agonist, BAY X3702, upon focal ischemic brain damage caused by acute subdural hematoma in the rat. (English) // Brain research. - 1999. - Vol. 845, no. 2 . - P. 232β235. - PMID 10536203 .
- β Kline AE , Yu J. , HorvΓ‘th E. , Marion DW , Dixon CE The selective 5-HT (1A) receptor agonist repinotan HCl attenuates histopathology and spatial learning deficits following traumatic brain injury in rats. (English) // Neuroscience. - 2001. - Vol. 106, no. 3 . - P. 547β555. - PMID 11591455 .
- β Mauler F. , HorvΓ‘th E. Neuroprotective efficacy of repinotan HCl, a 5-HT1A receptor agonist, in animal models of stroke and traumatic brain injury. (English) // Journal of cerebral blood flow and metabolism: official journal of the International Society of Cerebral Blood Flow and Metabolism. - 2005. - Vol. 25, no. 4 . - P. 451-459. - DOI : 10.1038 / sj.jcbfm.9600038 . - PMID 15674237 .
- β Ohman J. , Braakman R. , Legout V. Repinotan (BAY x 3702): a 5HT1A agonist in traumatically brain injured patients. (English) // Journal of neurotrauma. - 2001. - Vol. 18, no. 12 . - P. 1313-1321. - DOI : 10.1089 / 08977150152725614 . - PMID 11780862 .
- β Lutsep HL Repinotan, A 5-HT1A agonist, in the treatment of acute ischemic stroke. (English) // Current drug targets. CNS and neurological disorders. - 2005. - Vol. 4, no. 2 . - P. 119-120. - PMID 15857296 .
- β Berends AC , Luiten PG , Nyakas C. A review of the neuroprotective properties of the 5-HT1A receptor agonist repinotan HCl (BAYx3702) in ischemic stroke. (English) // CNS drug reviews. - 2005. - Vol. 11, no. 4 . - P. 379-402. - PMID 16614737 .
- β Teal P. , Davis S. , Hacke W. , Kaste M. , Lyden PD , Fierus M. A randomized, double-blind, placebo-controlled trial to evaluate the efficacy, safety, tolerability, and pharmacokinetic / pharmacodynamic effects of a targeted exposure of intravenous repinotan in patients with acute ischemic stroke: modified Randomized Exposure Controlled Trial (mRECT). (English) // Stroke; a journal of cerebral circulation. - 2009. - Vol. 40, no. 11 . - P. 3518β3525. - DOI : 10.1161 / STROKEAHA.109.551382 . - PMID 19745176 .
- β Guenther U., Wrigge H., Theuerkauf N., Boettcher MF, Wensing G., Zinserling J., Putensen C., Hoeft A. Repinotan, a selective 5-HT1A-R-agonist, antagonizes morphine-induced ventilatory depression in anesthetized rats (English) // Anesthesia and Analgesia : journal. - 2010 .-- October ( vol. 111 , no. 4 ). - P. 901-907 . - DOI : 10.1213 / ANE.0b013e3181eac011 . - PMID 20802053 .