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Endocytosis and signaling of 5-HT1A receptor

2023
The neurotransmitter serotonin (also known as 5-hydroxytryptamine, 5-HT) regulates many important physiological as well as pathological functions in the body like psychoemotional, sensation, blood circulation, food intake, autonomic, memory, sleep, pain, etc.
, Ragini   +3 more
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An Ethopharmacological Analysis of Selective Activation of 5-HT1A Receptors: The Mouse 5-HT1A Syndrome

Pharmacology Biochemistry and Behavior, 1997
The behavioral effects of 8-OH-DPAT [0.5-10 mg/kg intraperitoneally (i.p.)] and (+) S-20499 (1-20 mg/kg IP), a recently synthesized 5-HT1A receptor full agonist, were examined over a 2-h period in mice in a neutral cage and, during the peak period of effect, in a runway, 8-OH-DPAT (1 and 10 mg/kg) and (+) S-20499 (10 and 20 mg/kg) blocked vertical ...
R J, Blanchard   +5 more
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5-HT1A-mediated lower lip retraction: Effects of 5-HT1A agonists and antagonists

Pharmacology Biochemistry and Behavior, 1993
This study investigated the production of lower lip retraction (LLR) in the rat by the 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and the effect of the putative 5-HT1A antagonists pindolol and (1-(2-methoxy-phenyl)-4-[4-(2-phthalimido)-butyl]-piperazine (NAN190).
N A, Moore   +3 more
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5-HT1A Receptors in major depression

Journal of Psychopharmacology, 1990
The 5-HT 1A receptor has been studied using quantitative tritium film auto radiography in post-mortem frontal cortex of 15 cases suffering from major depression and controls matched for age, sex, post-mortem delay and storage time.
M, Yates, I N, Ferrier
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The 5-HT1A receptor: Signaling to behavior

Biochimie, 2019
The 5-HT1A receptor is highly expressed both in 5-HT neurons as a presynaptic inhibitory autoreceptor, and in many brain regions innervated by 5-HT as a post-synaptic heteroreceptor. This review examines the signaling of 5-HT1A receptors to regulate 5-HT activity and behavior. Initial findings in heterologous cell systems, neuronal cell lines, neurons,
Paul R. Albert, Faranak Vahid-Ansari
openaire   +2 more sources

Development of a presynaptic 5-HT1A antagonist

Bioorganic & Medicinal Chemistry Letters, 2003
A new 5-HT(1A) silent antagonist 14 (5-HT(1A) IC(50)=2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphé, and on 5-HT(1A) release in the raphé and hippocampus. While 14 alone was inactive in the social interaction paradigm, it completely reversed the social interaction activity
Ronald J, Mattson   +10 more
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5-HT1A behavioural models

1997
Publisher Summary 5-HT 1A receptor agonists have been tested in a wide variety of animal models indicative of CNS functions. These range from models for motion sickness and emesis to models predictive for antipsychotic drugs. In most of these tests, 5-HT 1A receptor agonists appear to be active, although the degree of specificity varies.
Mos, J., Olivier, B.
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Ligand-5-HT1A receptor interaction

Il Farmaco, 2000
In the present paper the general structure and pharmacophore of some 5-HT1A receptor ligands are described. For several compounds (approximately 15) the intrinsic activity in lower lip retraction (postsynaptic, rat) and hypothermia (presynaptic, mice) tests was determined. For the identified functional presynaptic agonists and antagonists the influence
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Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists.

The Journal of Pharmacology and Experimental Therapeutics, 1994
The novel benzodioxopiperazines [4-(benzodioxan-5-yl)1-[2- (benzocyclobutane-1-yl)ethyl]piperazine] (S 14489), [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine)] (S 15535) and [4-(benzodioxan-5-yl)1-[2(indan-1-yl)ethyl]piperazine (S15931) competitively displaced the binding of [3H]-8-OH-DPAT at serotonin (5-HT)1A receptors with affinities (pKis) of 9.2, 8.
M J, Millan   +9 more
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Development of 5-HT1A receptor antagonists

Behavioural Brain Research, 1995
The discovery that non-benzodiazepine anxiolytic agents such as buspirone bind with high affinity to the 5-HT1A receptor has stimulated the development of selective 5-HT1A receptor ligands as potential drug candidates. However, the lack of selective 5-HT1A receptor antagonists has hampered the elucidation of the mechanism of action of these agents ...
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