8-Hydroxy-2-(DI-N-propylamino)tetralin increases the activity of adenylate cyclase in the hippocampus of freely-moving rats

Sijbesma, H.; Schipper, J.; Molewijk, H.E.; Bosch, Assumpció; Kloet, E. Ronald de

doi:10.1016/0028-3908(91)90110-w

Cited by 24 publications

(5 citation statements)

References 42 publications

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“…An inverted U-shaped dose-response curve was also reported in several other studies for the effects of 8-OH-DPAT on different behaviors after systemic application (Dourish et al, 1985;Hillegaart et al, 1989;Mittman and Geyer, 1989;Papp and Willner, 1991;Shippenberg, 1991) and local application into the dorsal (DRN) and median raphe nucleus (MRN) or the dorsal hippocampus (Elliott et al, 1990;Fletcher et al, 1993;Andrews et al, 1994). At the highest dose (10 M), the low to moderate affinity of 8-OH-DPAT to non-5-HT 1A -receptor binding sites in the hippocampus (Sijbesma et al, 1991;Barnes and Sharp, 1999;Mengod et al, 1999;Koek, 1996, 2000) might possibly counteract the effects on the 5-HT 1A -receptor (Hamon, 1999).…”

Section: Discussionmentioning

confidence: 63%

Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

et al. 2004

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Cocaine induces an increase in hippocampal and nucleus accumbens (Nac) serotonin (5-HT) concentration parallel to locomotor activation. Both effects can be modulated by systemic 5-HT(1A)-receptor agonism/antagonism. Given the contribution of the hippocampus to spontaneous behavioral activity, these observations suggest a role for hippocampal 5-HT as well in the modulation of cocaine effects on behavior. To determine the role of hippocampal 5-HT(1A)-receptors in cocaine effects on behavior and hippocampal 5-HT release, we used in vivo microdialysis in freely moving rats. The 5-HT(1A)-receptor agonist, 8-OH-DPAT (0, 0.1, 1 and 10 microM), was applied locally into the hippocampus by reversed dialysis followed by a cocaine (10 mg/kg) or saline i.p. injection. The hippocampal 5-HT(1A)-receptor activation attenuated cocaine-induced hyperlocomotion and rearing behavior dose-dependently. Parallel to that, the cocaine-induced 5-HT increase was attenuated dose-dependently in the hippocampus but was left unaffected in the Nac. The intra-hippocampal application of 8-OH-DPAT affected neither behavioral activity nor 5-HT concentration in the hippocampus and in the Nac. In accord with these findings, hippocampal 5-HT(1A)-receptors may not be directly involved in the regulation of spontaneous behavior or basal 5-HT concentration in the hippocampus and Nac. However, the results indicate an inhibitory role of hippocampal 5-HT(1A)-receptors in cocaine-induced hyperactivity and in the 5-HT increase evoked by cocaine in the hippocampus but not in the Nac.

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Section: Discussionmentioning

confidence: 63%

Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

et al. 2004

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“…In 1991, Sijbesma et al examined the effects of intraperitoneal (IP) administration of 8-hydroxy-2-(di-n-propylamino) tetralin on the effl ux of cyclic adenosine monophosphate in the extracellular fl uid of the dorsal hippocampus, using in vivo microdialysis. 133 Implanting microdialysis probes into the renal cortex and measuring adenosine and inosine levels in the dialysate exiting the kidney, the researchers documented that 3-isobutyl-1-methylxanthine, a phosphodiesterase inhibitor, decreases renal cortical interstitial levels of adenosine and inosine. 134 Reverse dialysis of adenosine is capable of raising extracellular kynurenic acid in the rat striatum by interacting with postsynaptic neuronal A1 receptors.…”

Section: Other Neurotransmittersmentioning

confidence: 99%

“…A cuff was infl ated to 300 mmHg at the level of the patella to measure fl ow exclusively in the thigh. Djurhuus et al also assessed the impact of similar growth hormone (GH) and cortisol exposures on adipose tissue blood fl ow with the 133 Xe washout technique. 144 , 146 In brief, approximately 3 MBq of 133 Xe was injected into the subcutaneous adipose tissue of the abdomen ~5 cm sinistrolateral to the umbilicus.…”

Section: Analysis Of Glucose Lactate Glycerol and Local Blood Flowmentioning

confidence: 99%

“…Djurhuus et al also assessed the impact of similar growth hormone (GH) and cortisol exposures on adipose tissue blood fl ow with the 133 Xe washout technique. 144 , 146 In brief, approximately 3 MBq of 133 Xe was injected into the subcutaneous adipose tissue of the abdomen ~5 cm sinistrolateral to the umbilicus. Disappearance of 133 Xe was continuously measured starting from 30 minutes after injection by use of an NaI detector.…”

Section: Analysis Of Glucose Lactate Glycerol and Local Blood Flowmentioning

confidence: 99%

“…144 , 146 In brief, approximately 3 MBq of 133 Xe was injected into the subcutaneous adipose tissue of the abdomen ~5 cm sinistrolateral to the umbilicus. Disappearance of 133 Xe was continuously measured starting from 30 minutes after injection by use of an NaI detector. 146 The results indicated that coadministration of GH and cortisol does not infl uence adipose tissue blood fl ow.…”

Section: Analysis Of Glucose Lactate Glycerol and Local Blood Flowmentioning

confidence: 99%

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Microdialysis as a tool in local pharmacodynamics

Peris

Zhong

et al. 2006

AAPS J

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A BSTRACTIn many cases the clinical outcome of therapy needs to be determined by the drug concentration in the tissue compartment in which the pharmacological effect occurs rather than in the plasma. Microdialysis is an in vivo technique that allows direct measurement of unbound tissue concentrations and permits monitoring of the biochemical and physiological effects of drugs throughout the body. Microdialysis was fi rst used in pharmacodynamic research to study neurotransmission, and this remains its most common application in the fi eld. In this review, we give an overview of the principles, techniques, and applications of microdialysis in pharmacodynamic studies of local physiological events, including measurement of endogenous substances such as acetylcholine, catecholamines, serotonin, amino acids, peptides, glucose, lactate, glycerol, and hormones. Microdialysis coupled with systemic drug administration also permits the more intensive examination of the pharmacotherapeutic effect of drugs on extracellular levels of endogenous substances in peripheral compartments and blood. Selected examples of the physiological effects and mechanisms of action of drugs are also discussed, as are the advantages and limitations of this method. It is concluded that microdialysis is a reliable technique for the measurement of local events, which makes it an attractive tool for local pharmacodynamic research.

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Electrophysiological evidence for a large receptor reserve for inhibition of dorsal raphe neuronal firing by 5‐HT_1A agonists

Cox

Meller

Waszczak

1993

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Previous studies [Meller et al. (1990) Mol. Pharmacol., 37:231-237] have shown that a large receptor reserve exists for the inhibition of serotonin synthesis in rat cortex and hippocampus by the 5-HT1A agonist 8-hydroxy-2(di-n-propylamino)tetralin (8-OH-DPAT), whereas little or no reserve exists for the lower efficacy agonists ipsapirone and BMY 7378. The current studies were undertaken to determine if the above drugs exhibit similar relative efficacies and receptor reserves in an electrophysiological model of 5-HT1A receptor activation, i.e., the inhibition of dorsal raphe cell firing. Intravenous dose-response curves were constructed in untreated control rats, or in rats which received an injection of the irreversible receptor inactivator N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ, 6 mg/kg, s.c.) 24 hours before recording. All three drugs fully inhibited dorsal raphe cell firing in control rats (ED50's: 1.5 micrograms/kg, 8-OH-DPAT; 30.0 micrograms/kg, ipsapirone; 17.5 micrograms/kg, BMY 7378). However, unlike effects on serotonin synthesis, EEDQ treatments caused no depression of the maximal inhibitory response for any of the agonists, although all dose-response curves were shifted to the right (ED50's: 10.1 micrograms/kg, 6.7-fold shift, 8-OH-DPAT; 139.9 micrograms/kg, 4.7-fold shift, ipsapirone; 53.8 micrograms/kg, 3.1-fold shift, BMY 7378). Although the order of agonist efficacies was similar for both inhibition of serotonin synthesis and dorsal raphe cell firing (8-OH-DPAT > ipsapirone > BMY 7378), a large (> 50%) receptor reserve was estimated for all three drugs in this electrophysiological system.(ABSTRACT TRUNCATED AT 250 WORDS)

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8-Hydroxy-2-(DI-N-propylamino)tetralin increases the activity of adenylate cyclase in the hippocampus of freely-moving rats

Cited by 24 publications

References 42 publications

Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Microdialysis as a tool in local pharmacodynamics

Electrophysiological evidence for a large receptor reserve for inhibition of dorsal raphe neuronal firing by 5‐HT_1A agonists

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8-Hydroxy-2-(DI-N-propylamino)tetralin increases the activity of adenylate cyclase in the hippocampus of freely-moving rats

Cited by 24 publications

References 42 publications

Hippocampus 5‐HT1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Hippocampus 5‐HT1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Microdialysis as a tool in local pharmacodynamics

Electrophysiological evidence for a large receptor reserve for inhibition of dorsal raphe neuronal firing by 5‐HT1A agonists

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Product

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Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Hippocampus 5‐HT_1A‐receptors attenuate cocaine‐induced hyperlocomotion and the increase in hippocampal but not nucleus accumbens 5‐HT

Electrophysiological evidence for a large receptor reserve for inhibition of dorsal raphe neuronal firing by 5‐HT_1A agonists