Osemozotan ( MKC-242 ) is a selective 5-HT 1A receptor agonist with some functional selectivity: it acts as an agonist for presynaptic receptors and as a partial agonist for postsynaptic ones. [1] Stimulation of 5-HT 1A receptors affects the release of several other neurotransmitters, including serotonin , dopamine , norepinephrine , acetylcholine . [2] Receptors of the 5-HT 1A subtype are inhibitory G-protein-coupled receptors that inhibit adenylate cyclase and reduce neuronal activity. [3] Osemozotan has antidepressant , anxiolytic , anti-obsessive, anti-aggressive, analgesic properties in animal studies. [4] [5] [6] , [2] It is used to study the role of 5-HT 1A receptors in modulating the release of dopamine and serotonin in the brain [7] [8] and the role of these receptors and neurotransmitters in developing addiction to psychostimulants, such as cocaine and amphetamine , methamphetamine . [9] [10] [11] [12] [13]
| Osemozotan | |
|---|---|
| Chemical compound | |
| IUPAC | 5- (3 - [((2S) -1,4-benzodioxan-2-ylmethyl) amino] propoxy) -1,3-benzodioxole |
| Gross formula | C 19 H 22 ClNO 5 |
| Molar mass | 341.400 g / mol |
| Cas | |
| PubChem | |
Content
- 1 Pharmacodynamics
- 2 Pharmacokinetics
- 3 Use
- 3.1 pain
- 3.2 Aggressive behavior
- 3.3 Anxiety and depression
- 3.4 Obsessive-compulsive disorder (OCD)
- 3.5 Drug dependence
- 4 Prevalence of mental diseases targeted by Osemozotan
- 5 See also
- 6 notes
Pharmacodynamics
Pharmacokinetics
Usage
Pain
Aggressive Behavior
Anxiety and Depression
Obsessive Compulsive Disorder (OCD)
Addiction
Prevalence of Osemozotan Mental Illnesses Target
See also
- Piclozotan
- Robalsotan
- Sarisotan
- Naluzotan
Notes
- ↑ Matsuda T. , Yoshikawa T. , Suzuki M. , Asano S. , Somboonthum P. , Takuma K. , Nakano Y. , Morita T. , Nakasu Y. , Kim HS Novel benzodioxan derivative, 5- (3 - [( (2S) -1,4-benzodioxan-2-ylmethyl) amino propoxy) -1,3-benzodioxole HCl (MKC-242), with a highly potent and selective agonist activity at rat central serotonin1A receptors.] / / Japanese journal of pharmacology. - 1995. - Vol. 69, no. 4 . - P. 357-366. - PMID 8786639 .
- ↑ 1 2 Matsuda, Toshio. "Neuropharmacologic Studies on the Brain Serotonin1A Receptor Using the Selective Agonist Osemozotan." Biol.Pharm.Bull . 36 .12 (2013): 1871-882.
- ↑ Saudou F, Hen R. 5-Hydroxytryptamine receptor subtypes in vertebrates and invertebrates. Neurochem. Int. 25 , 503-532 (1994)
- ↑
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- ↑ Abe, Michikazu, Hiroshi Nakai, Reiko Tabata, Ken-Ichi Saito, and Mitsuo Egawa. “Effect of 5- {3 - [((2S) -1,4-Benzodioxan-2-ylmethyl) amino] propoxy} -1,3-benzodioxole HCL (MKC-242), a Novel 5-HT1A-Receptor Agonist, on Aggressive Behavior and Marble Burying Behavior in Mice. ” Jpn. J. Pharmacol. 76 (1998): 297-304.
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