(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist

Arvidsson, L.-E.; Am, Johansson; Hacksell, Uli; Jl, Nilsson; Svensson, Kristian; Stephan, Holger; Magnusson, Tomas; Carlsson, Anna; Andersson, Bo; Wikstrom, HV

doi:10.1021/jm00394a029

Cited by 37 publications

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“…Further similarly designed experiments examined the cutaneous blood flow and SCVAR effects of drugs that interact with 5-hydroxytryptamine (5-HT) receptors, particularly the specific 5-HT 1A receptor agonist 8-OH-DPAT (Arvidsson et al 1987) and the specific 5-HT 2A receptor antagonist SR46349B (Rinaldi-Carmona et al 1992). This pattern of 5-HT receptor interaction is considered important in the manner whereby atypical antipsychotics exert their effects on dopaminergic neurotransmission (Meltzer et al 2003).…”

Section: Introductionmentioning

confidence: 99%

Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

Blessing

2005

Psychopharmacology

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Section: Introductionmentioning

confidence: 99%

Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

Blessing

2005

Psychopharmacology

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“…We have now determined whether activation of 5‐HT 1A receptors by the specific agonist 8‐hydroxy‐2‐(di‐ n ‐propylamino)tetralin (8‐OH‐DPAT) (Arvidsson et al 1987) can reduce body temperature by increasing cutaneous blood flow, thereby facilitating transfer of heat from the body. In conscious rabbits we first induced vasoconstriction of the ear pinna vascular bed by exposing the animals to a cold environment.…”

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confidence: 99%

5‐Hydroxytryptamine 1A Receptors Inhibit Cold‐Induced Sympathetically Mediated Cutaneous Vasoconstriction in Rabbits

Ootsuka

Blessing

2003

The Journal of Physiology

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Journal of PhysiologyIdentification of the different 5-hydroxytryptamine (5-HT) receptor subtypes has facilitated our understanding of the contribution of 5-HT to the regulation of body temperature. Activation of 5-HT 1A receptors decreases body temperature (Hjorth, 1985;Gudelsky et al. 1986;Cryan et al. 1999). Activation of 5-HT 2A receptors increases body temperature (Gudelsky et al. 1986;Löscher et al. 1990;Mazzola-Pomietto et al. 1995). However, the relevant neuroanatomical pathways and underlying neurotransmitter mechanisms mediating these effects remain to be elucidated. The task is especially complicated because 5-HT alters so many psychological, behavioural and physiological variables (Barnes & Sharp, 1999). Pharmacological and physiological studies of the mechanisms underlying the temperature effects of agents acting at 5-HT 1A receptors often focus on body temperature per se, without determining the relative contributions of heat production and/or heat loss to the temperature equation.Similar considerations apply to neuroanatomical studies. Interest in the role of 5-HT in temperature control has focused on upper brainstem and forebrain 5-HT-innervated regions. Much less attention has been paid to possible contributions of the thermoregulatory role of 5-HT via regulation of heat exchange with the environment through the cutaneous circulation, i.e. on heat dissipation rather than heat production. Even when temperature studies have focused on 5-HT neurons in the medullary raphe region, interpretation of the results has emphasized possible ascending projections of the cells (Dickenson, 1977;Berner et al. 1999), rather than descending projections to cutaneous sympathetic preganglionic neurons in the spinal cord. Central neuroanatomical organization of the descending central control of the cutaneous circulation includes a brainstem relay in raphe magnus/pallidus and the parapyramidal region of the medulla oblongata (Blessing & Nalivaiko, 2000;Nalivaiko & Blessing, 2001;Tanaka et al. 2002). Neurons in this medullary region include the B1-B3 bulbospinal cells that synthesize 5-HT (Loewy, 1981;Steinbusch, 1981;Skagerberg & Bjorklund, 1985;Nicholas et al. 1992). Transneuronal intra-axonal tracing experiments in rats show that 5-HT neurons are amongst

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“…In previous studies, the racemic form of 8-OH-DPAT [(6)-8-hydroxy-2-(di-n-propylamino) tertralin hydrobromide] has been widely used as a selective 5-HT 1A receptor agonist (Arvidsson et al, 1987). The present experiment was conducted with the more active enantiomer, (R)-(1)-8-hydroxy-2-(di-npropylamino)tertralin hydrobromide ((R)-8-OH-DPAT) (SigmaAldrich, Stockholm, Sweden), which, unlike the racemic form, is a full agonist at the 5-HT 1A receptor (Cornfield et al, 1991).…”

Section: Drugsmentioning

confidence: 99%

5‐HT_1A and NMDA receptors interact in the rat medial septum and modulate hippocampal‐dependent spatial learning

et al. 2009

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Cholinergic and GABAergic neurons in the medial septum/vertical limb of the diagonal band of Broca (MS/vDB) projecting to the hippocampus, constitute the septohippocampal projection, which is important for hippocampal-dependent learning and memory. There is also evidence for an extrinsic as well as an intrinsic glutamatergic network within the MS/vDB. GABAergic and cholinergic septohippocampal neurons express the serotonergic 5-HT(1A) receptor and most likely also glutamatergic NMDA receptors. The aim of the present study was to examine whether septal 5-HT(1A) receptors are important for hippocampal-dependent long-term memory and whether these receptors interact with glutamatergic NMDA receptor transmission in a manner important for hippocampal-dependent spatial memory. Intraseptal infusion of the 5-HT(1A) receptor agonist (R)-8-OH-DPAT (1 or 4 microg/rat) did not affect spatial learning in the water maze task but impaired emotional memory in the passive avoidance task at the higher dose tested (4 microg/rat). While intraseptal administration of (R)-8-OH-DPAT (4 microg) combined with a subthreshold dose of the NMDA receptor antagonist D-AP5 (1 microg) only marginally affected spatial acquisition, it produced a profound impairment in spatial memory. In conclusion, septal 5-HT(1A) receptors appears to play a more prominent role in emotional than in spatial memory. Importantly, septal 5-HT(1A) and NMDA receptors appear to interact in a manner, which is particularly critical for the expression or retrieval of hippocampal-dependent long-term spatial memory. It is proposed that NMDA receptor hypofunction in the septal area may unmask a negative effect of 5-HT(1A) receptor activation on memory, which may be clinically relevant.

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(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist

Cited by 37 publications

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Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

5‐Hydroxytryptamine 1A Receptors Inhibit Cold‐Induced Sympathetically Mediated Cutaneous Vasoconstriction in Rabbits

5‐HT_1A and NMDA receptors interact in the rat medial septum and modulate hippocampal‐dependent spatial learning

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(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist

Cited by 37 publications

References 0 publications

Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol

5‐Hydroxytryptamine 1A Receptors Inhibit Cold‐Induced Sympathetically Mediated Cutaneous Vasoconstriction in Rabbits

5‐HT1A and NMDA receptors interact in the rat medial septum and modulate hippocampal‐dependent spatial learning

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5‐HT_1A and NMDA receptors interact in the rat medial septum and modulate hippocampal‐dependent spatial learning