5-HT1A receptor agonists

Hasrat JA, De Bruyne T, De Backer JP, Vauquelin G, Vlietinck AJ. Isoquinoline derivatives isolated from the fruit of Annona muricata as 5-HTergic 5-HT1A receptor agonists in rats unexploited antidepressive (lead) products. J Pharm Pharmacol 1997 49 1145-1149. 

Monti, J. M. Jantos, H. (1992). Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat. J. Sleep Res. 1,... 

Lopez-Rodriguez, M.L., Rosado, M.L., Benhamu, B., Morcillo, M.J., Sanz, A.M., Orensanz, L., Beneitez, M.E., Fuentes, J. A. and Manzanares, J. (1996) Synthesis and structure-activity relationships of a new model of arylpiperazines. 1.2-[4-(o-Methoxy-phenyl) piperazin-l-ylmethyl]-l,3-dioxoperhydroimidazo[l,5-a]-pyridine a selective 5-HT1A receptor agonist. Journal of Medicinal Chemistry, 39, 4439-4450. 

Yamada J, Sugimoto Y, Yoshikawa T. Effects of adrenalectomy on hyperphagia induced by the 5-HT1A receptor agonist 8-OH-DPAT and 2-deoxy-D-glucose in rats. Neuroreport 1998 9 1831-1833. 

Miczek KA, Hussain S, Faccidomo S. Alcohol-heightened aggression in mice attenuation by 5-HT1A receptor agonists. Psychopharmacology (Berl) 1998 139 160-168. 

Blier P, de Montigny C. Electrophysiological investigation of the adaptive response of the 5-HT system to the administration of 5-HT1A receptor agonists. J Cardiovac Pharmacol 1990 15 S42-S48. 

Therefore, the activation of 5-HT1A receptors in the 5-HT cells by the endogenous transmitter or 5-HT1A receptor agonists increases K+ conductance, which hyperpolarizes the neuronal membrane (see below), thus inhibiting 5-HT cell firing (19-22) (see below) and reducing 5-HT release in the cell body area (23-27) and projection structures (24,25,28-30) (Fig. 1). 

Casanovas JM, Berton O, Celada P, Artigas F. In vivo actions of the selective 5-HT1A receptor agonist BAY x 3702 on serotonergic cell firing and release. Naunyn-Schmiedebergs Arch Pharmacol 2000 362 248-254. 

To characterize 5-HTlA-agonist-induced hypothermia, Zuideveld et al. [554] developed a mathematical model that describes the hypothermic effect on the basis of the concept of a set point and a general physiological response model [431,555]. The model was applied to characterize hypothermic response vs. time profiles after administration of different doses of the reference 5-HT1A receptor agonists R- and S-8-OH-DPAT. 

The classical three-compartment model describes pharmacokinetics of 5-HT1A receptor agonists. By means of a sigmoidal function E (c), the 5-HT1A agonist concentration c (t) influences the set-point signal that dynamically interacts with the body temperature. By using x (t) and y (t) as dimensionless state variables for the set-point and temperature, respectively, the model is expressed by the set of two nonlinear differential equations ... 

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