Receptor, Serotonin, 5-HT1A - Antagonists & inhibitors
Research News and Information

Sunday, November 22, 2009

Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.

11 Aug 2009 On the basis of the previously reported clinical candidate, SSA-426 (1), a series of related 2-piperazin-1-ylquinoline derivatives 3-16 were synthesized and evaluated as dual-acting serotonin (5-HT) reuptake inhibitors and 5-HT1A receptor ... Read more...

Role of spinal serotonergic pathways in sneeze-induced urethral continence reflex in rats.

27 Jul 2009 To clarify the role of spinal serotonergic mechanisms in preventing stress urinary incontinence (SUI) during sneezing, we investigated the effect of intrathecal (it) application of 8-OH-DPAT (a 5-HT(1A) agonist), mCPP (a 5-HT(2B/2C) agonist), and ... Read more...

Enhancement of the function of rat serotonin and norepinephrine neurons by sustained vagus nerve stimulation.

29 Jun 2009 BACKGROUND: Vagus nerve stimulation (VNS) is a recent intervention for treatment-resistant depression. Electrophysiological recordings in the rat brain showed that VNS increases the firing rate of norepinephrine (NE) neurons after 1 day of ... Read more...

Latest indexed articles for 'Receptor, Serotonin, 5-HT1A - Antagonists & inhibitors'

These are the very latest articles for this heading:

• Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. 11 Aug 2009
• Role of spinal serotonergic pathways in sneeze-induced urethral continence reflex in rats. 27 Jul 2009
• Enhancement of the function of rat serotonin and norepinephrine neurons by sustained vagus nerve stimulation. 29 Jun 2009
• Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. 11 Jun 2009
• The contribution of serotonin 1A receptors to kappa opioid immunosuppression. 9 Jun 2009
• 5-HT1A receptor activation is necessary for 5-MeODMT-dependent potentiation of feeding inhibition. 29 May 2009
• Contribution of the striatum to the effects of 5-HT1A receptor stimulation in L-DOPA-treated hemiparkinsonian rats. 13 May 2009
• Identification of an additional supraspinal component to the analgesic mechanism of action of buprenorphine. 28 Apr 2009
• Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. 21 Apr 2009
• Memory time-course: mRNA 5-HT1A and 5-HT7 receptors. 26 Mar 2009
• Preclinical characterization of WAY-211612: a dual 5-HT uptake inhibitor and 5-HT (1A) receptor antagonist and potential novel antidepressant. 24 Mar 2009
• The selective 5-hydroxytryptamine 1A antagonist, AZD7371 [3(R)-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide (R,R)-tartrate monohydrate] (robalzotan tartrate monohydrate), inhibits visceral pain-related visceromotor, but not autonomic cardiovascular, responses to colorectal distension in rats. 24 Mar 2009
• An antihyperkinetic action by the serotonin 1A-receptor agonist osemozotan co-administered with psychostimulants or the non-stimulant atomoxetine in mice. 5 Mar 2009
• [Involvement of presynaptic 5-HT1A receptors in immunomodulation under conditions of psychoemotional state] 27 Feb 2009
• 1,3-Dioxolane-based ligands as rigid analogues of naftopidil: structure-affinity/activity relationships at alpha1 and 5-HT1A receptors. 27 Feb 2009
• WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation. 30 Jan 2009
• Synthesis and pharmacological evaluation of new arylpiperazines N-[4-[4-(aryl) piperazine-1-yl]-phenyl]-amine derivatives: putative role of 5-HT1A receptors. 22 Jan 2009
• Antagonism of 5-HT(1A) receptors uncovers an excitatory effect of SSRIs on 5-HT neuronal activity, an action probably mediated by 5-HT(7) receptors. 21 Jan 2009
• Decline in serotonergic firing activity and desensitization of 5-HT1A autoreceptors after chronic unpredictable stress. 13 Jan 2009
• Enhancement of cortical extracellular 5-HT by 5-HT1A and 5-HT2C receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. 3 Jan 2009

See a longer list of these articles.

Technical information about 'Receptor, Serotonin, 5-HT1A'

Definition: A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.

Registry Number: 112692-38-3

Descriptor UI: D044282

Alternative terms: Receptor, Serotonin, 5-HT1A; 5-HT1A Receptor; 5 HT1A Receptor; Receptor, 5-HT1A; 5-Hydroxytryptamine 1A Receptor; 1A Receptor, 5-Hydroxytryptamine; 5 Hydroxytryptamine 1A Receptor; 5-Hydroxytryptamine 1A Receptors; 1A Receptors, 5-Hydroxytryptamine; 5 Hydroxytryptamine 1A Receptors; Receptors, 5-Hydroxytryptamine 1A; Serotonin, 5-HT1a Receptor; 5-HT1a Receptor Serotonin; Receptor Serotonin, 5-HT1a; Serotonin, 5 HT1a Receptor; Serotonin 1A Receptor; 1A Receptor, Serotonin; Receptor, Serotonin 1A; Serotonin Receptor, 5-HT1A; 5-HT1A Serotonin Receptor; Receptor, 5-HT1A Serotonin; Serotonin Receptor, 5 HT1A; 5-HT(1A) Receptor; Receptor, 5-Hydroxytryptamine 1A; Receptor, 5 Hydroxytryptamine 1A;

Allowable Qualifiers: administration & dosage; analysis; antagonists & inhibitors; biosynthesis; blood; classification; deficiency; drug effects; genetics; history; immunology; isolation & purification; metabolism; physiology; radiation effects; therapeutic use; ultrastructure; chemistry; agonists;

Tree Number: D12.776.543.750.070.800.100.100; D12.776.543.750.100.800.100.100; D12.776.543.750.720.300.800.100.100;

History Note: 2004; use RECEPTOR SEROTONIN 5 HT1 SUBCLASS (NM) 1993-2003