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A direct comparison was made of the effects of serotonin 5-HT1A and 5-HT1B selective compounds on the spontaneous firing rate of dorsal raphe serotoninergic neurons in chloral-hydrate-anesthetized rats. Following intravenous administration, the 5-HT1A selective compounds ipsapirone (TVX Q 7821) and LY 165163 potently inhibited single-unit activity in a(More)
Here we describe the properties of CP-154,526, a potent and selective nonpeptide antagonist of corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (Ki < 10 nM) and blocks CRF-stimulated adenylate cyclase activity in membranes prepared from rat cortex and pituitary. Systemically administered CP-154,526(More)
The ability of the beta-adrenoceptor antagonist propranolol to block the effects of serotonin (5-HT) and 5-HT1A-selective agonists on the spontaneous firing of serotonergic dorsal raphe neurons was assessed. During microiontophoretic application, (-)- but not (+)-propranolol rapidly and reversibly blocked the suppressant effects of the 5-HT1A-selective(More)
It is becoming evident that the diverse electrophysiological actions of 5-HT in the central nervous system can be best formulated in terms of receptor subtypes and their respective effector mechanisms. Based on the findings described in this review, the following pattern of central 5-HT electrophysiology is emerging: 1) inhibitory effects are mediated by(More)
In low cerveau isolé transected rats, the effects of microiontophoretic application of putative serotonin 5-HT1A and 5-HT1B agonists on the spontaneous firing rate of CA1 pyramidal cells were compared to those of 5-HT. In contrast to the large current-dependent suppression of unit activity observed with 5-HT, the 5-HT1A compounds, ipsapirone, 8-OH-DPAT(More)
Neurons in the suprachiasmatic nucleus (SCN), the site of the endogenous biological clock in mammals, fire spontaneously, peaking in firing rate near ZT6 or at the midpoint of the light phase in a 12:12 light-dark cycle. In rat hypothalamic slices, tissue incubations with drugs can produce a shift in this daily rhythm, the magnitude of which is dependent(More)
In vivo microdialysis in guinea pig hypothalamus was used to study the effect of serotonin [5-hydroxytryptamine (5-HT)] subtype 1D autoreceptor blockade on the increase in extracellular 5-HT levels produced by a selective 5-HT reuptake inhibitor (SSRI). Administration of the selective 5-HT1D antagonist GR127935 at 0.3 mg/kg had no effect, but 5 mg/kg(More)
Daily variation in an organism's physiology and behaviour is regulated by the synchrony that is achieved between the internal timing mechanisms - the circadian rhythms of the biological clock - and the prevailing environmental cues. Proper synchrony constitutes an adaptive response; improper or lost synchrony may well yield maladaptation and, in the case of(More)
The effects of MDMA (3,4-methylenedioxymethamphetamine) on the activity of serotonin (5-HT)-containing dorsal raphe neurons were characterized using extracellular single-unit recording and microdialysis techniques in the in vitro midbrain slice preparation. Addition of (+)-MDMA, (-)-MDMA or p-chloroamphetamine (PCA) to the superfusate (final concentration(More)
BACKGROUND Ziprasidone (Zeldox) is a novel antipsychotic with a unique combination of antagonist activities at monoaminergic receptors and transporters and potent agonist activity at serotonin 5-HT(1A) receptors. 5-HT(1A) receptor agonism may be an important feature in ziprasidone's clinical actions because 5-HT(1A) agonists increase cortical dopamine(More)