Download - Potent A1 adenosine receptor agonist
![Page 1: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/1.jpg)
Potent A1 adenosine receptor agonistAdenosine amine congener ADAC CAS 96760-69-9, C28H32N8O6 MW 576.60 Purity: 98 %Biological Activity:
![Page 2: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/2.jpg)
Receptores Serotoninérgicos
Ph.D. Randolph Alonso
![Page 3: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/3.jpg)
Serotonina
La serotonina juega un papel muy importante en el funcionamiento normal del cerebro, esto puede incluir la modulación de los estados de humor, apetito, sex, sueño, memoria, emociones, ansiedad, efectos endocrinos, y muchos otros, este receptor esta ampliamente distribuido e el cerebro.
![Page 4: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/4.jpg)
Biosíntesis
![Page 5: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/5.jpg)
![Page 6: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/6.jpg)
Receptores Serotoninérgicos
(5-HT) constituyen al menos 15 subtipos, clasificados en 5-HT1 (con cuatro subtipos), 5-HT2 y 5-HT3. Los receptores 5-HT1A, localizados presinápticamente en el núcleo del rafe (inhibiendo la recaptación presináptica de 5-HT) y postsinápticamente en el hipocampo, modulan la adenilato-ciclasa. Los receptores 5-HT2, localizados en la cuarta capa de la corteza cerebral, intervienen en la hidrólisis del fosfoinosítol. Los receptores 5-HT3 se localizan presinápticamente en el núcleo del tracto solitario.
![Page 7: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/7.jpg)
Receptor
![Page 8: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/8.jpg)
5HT Receptor
![Page 9: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/9.jpg)
Receptor (5HT1- 5HT7) →PG →AC (-); TM1-TM75HT2 → PGq5HT 4,6,7 → PGs5HT1 todos, 5HT 5A y B → PGi/o5HT3 canles de Na+
![Page 10: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/10.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Agonista Receptor 5HT1A Buspirona agonista parcial arilpiperazina anxiolitico, antidepresivo
![Page 11: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/11.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Antagonista Receptor 5HT1APropanolol ( β-adrenergico) → bloquea 5HT1A ↑ [ ] postsinaptica
![Page 12: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/12.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Receptor 5HT1D →PG →AC (-)Propanolol ↓ afinidad se una a las TM1-TM2- TM3-
TM7
![Page 13: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/13.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Pindolol ↓ afinidad 5HT1D
![Page 14: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/14.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Agonista Receptor 5HT1DSumatriptan indolalquilamina ansiedad y depresión
![Page 15: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/15.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Antagonista Receptor 5HT1DGR 127935
![Page 16: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/16.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Receptor 5HT1F LY-334370 Anti-migraña
![Page 17: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/17.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Receptor 5HT2A Agonista Receptor 5HT2ADOI (Fenilalquilamina) no selectivo
![Page 18: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/18.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Antagonista 5HT2AKetanserin (piperazinaarindalone) Apetito, sueño,
antisicótico, antidepresivo y termorregulación Psicosis depresiva /D2
![Page 19: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/19.jpg)
Drogas que afecta la Neurotransmisión Serotoninérgica
Receptor 5HT3 acoplado a canal iónico de Na o KAntagonistas 5HT3Bemestron derivado de la cocaína
migraña, antisicótico
![Page 20: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/20.jpg)
Antagonista 5HT4 →PG →AC (+)DAU6285 Memoria aprendizaje, reflujo
gastroesofágico, motilidad gastroinstestinal.
Drogas que afecta la Neurotransmisión Serotoninérgica
![Page 21: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/21.jpg)
Agonista selectivo 5HT6 SNC→PG →AC (+)
Ro046790 etil-5-metoxi-N-N-dimetiltriptamina Antisicótico
Drogas que afecta la Neurotransmisión Serotoninérgica
![Page 22: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/22.jpg)
Antagonista 5HT7 →PG →AC (+)Derivado de la ErgolinaLy215840 Enfermedades coronarias.
Drogas que afecta la Neurotransmisión Serotoninérgica
![Page 23: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/23.jpg)
Síntesis de drogas que afecta la Neurotransmisión Serotoninérgica
![Page 24: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/24.jpg)
Recaptura Serotonina
![Page 25: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/25.jpg)
![Page 26: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/26.jpg)
![Page 27: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/27.jpg)
Fluoxetina
OH OH
O
OH
OH
OMs
OH
NH
OH
CH3
NH
O
CH3
FF
F
a b
c
de
Reactivos: (a) L-(+)-diisopropyl tartrate, ; (b) D-(-)-diisopropyl tartrate; (c) DME, Red-Al, PhMe, 0-20° over 3 h; (d) EtN, MsCI, Et2O, -10°, 3 h; (e) MeNH2, H2O, THF, 65°, 3 h; (f) DMA, NaH, 90°, 1.5 h then 4-chlorobenzotrifIuoride, 100°, 2.5 h. (5)
![Page 28: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/28.jpg)
Sertralina
O
Cl
Cl
O CH3
O
CH3
O
O
Cl
Cl
O
CH3
O CH3
Cl
Cl
OH O
Cl
Cl
O
Cl
Cl
NH
CH3
ab
c
d
![Page 29: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/29.jpg)
Paroxetina
N
O
OCH3
CH3
N
O
OCH3
CH3
F
N
CH3
F
O
Cl
N
CH3
F
O
O
CH3 CH3
CH3
N
CH3
F
OH
N
CH3
F
O
OO
NH
F
O
O
O
a b
c
de
Scheme 6.8. Reagents: (a) 4-F-C6H4MgBr; (b) NaOMe, PhH, 2 h, reflux; (c) aq. HCI; (d) SOCI2, 3 h, rt; (e) (-)-menthol, pyridine, 0°, then 16 h rt; (f) fractional distillation to give the single diastereomer; (g) LAH; (h) SOCI2, CHCI3, 10° then reflux 6 h; (i) Na, MeOH, 3,4-methylenedioxyphenol, reflux 16 h; (j) DCM, PhOCOCI, 0° then 16 h at rt; (k) KOH, methylcellusolve, reflux, 4 h.
![Page 30: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/30.jpg)
Subtipos de Receptores de Serotonina
![Page 31: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/31.jpg)
Horas de estudio independiente para este tema
10 horas
![Page 32: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/32.jpg)
![Page 33: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/33.jpg)
![Page 34: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/34.jpg)
![Page 35: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/35.jpg)
![Page 36: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/36.jpg)
![Page 37: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/37.jpg)
![Page 38: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/38.jpg)
![Page 39: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/39.jpg)
![Page 40: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/40.jpg)
![Page 41: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/41.jpg)
![Page 42: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/42.jpg)
![Page 43: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/43.jpg)
![Page 44: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/44.jpg)
![Page 45: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/45.jpg)
![Page 46: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/46.jpg)
![Page 47: Potent A1 adenosine receptor agonist](https://reader036.vdocuments.us/reader036/viewer/2022062310/56815d8e550346895dcba269/html5/thumbnails/47.jpg)