receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A...
58 KB (6,181 words) - 22:24, 4 August 2024
and vortioxetine are 5-HT1A receptor partial agonists. Flibanserin, a drug used for female sexual dysfunction, is a 5-HT1A receptor partial agonist. Many...
16 KB (1,657 words) - 17:23, 8 June 2024
which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors. LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A and 5-HT6 agonist. The...
65 KB (5,263 words) - 10:40, 12 August 2024
amine-associated receptor 1 (TAAR1) agonist [12][13] Ulotaront (SEP-363856; SEP-856) – serotonin 5-HT1A receptor agonist and trace amine-associated receptor 1 (TAAR1)...
97 KB (7,819 words) - 07:20, 18 August 2024
5-HT). The 5-HT1 subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT1A, 5-HT1B...
5 KB (472 words) - 12:54, 25 December 2023
Buspirone (category 5-HT1A agonists)
generalized anxiety disorder. It is a serotonin 5-HT1A receptor agonist, increasing action at serotonin receptors in the brain. It is taken orally, and takes...
42 KB (3,631 words) - 13:44, 27 July 2024
Serotonin modulator and stimulator (category Serotonin receptor antagonists)
serotonin reuptake inhibitor (SRI), agonist of the 5-HT1A receptor, and antagonist of the 5-HT3 and 5-HT7 receptors. However, it can also technically be applied...
5 KB (568 words) - 17:03, 21 March 2024
Pindolol (category 5-HT1A antagonists)
hypertension. It is also an antagonist of the serotonin 5-HT1A receptor, preferentially blocking inhibitory 5-HT1A autoreceptors, and has been researched as an add-on...
25 KB (2,288 words) - 09:32, 25 June 2024
WAY-100635 (category Serotonin receptor antagonists)
as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. It is sometimes...
20 KB (1,933 words) - 22:02, 18 August 2023
reuptake inhibitor (SDRI) and 5-HT2A and 5-HT2C receptor antagonist Oxaflozane (Conflictan) – 5-HT1A, 5-HT2A, and 5-HT2C receptor agonist Pivagabine (Tonerg)...
17 KB (1,478 words) - 23:23, 28 July 2024
very potent and highly selective 5-HT1A receptor full agonist of the azapirone family. Its affinity for the 5-HT1A receptor was reported to be 4.8 nM (Ki)...
7 KB (730 words) - 19:56, 30 November 2023
Cariprazine (category H1 receptor antagonists)
and D2 receptor partial agonist, with a preference for the D3 receptor. Cariprazine is also a partial agonist at the serotonin 5-HT1A receptor and acts...
31 KB (2,618 words) - 06:03, 18 May 2024
– 5-HT1A receptor modulator[2] TGW00AA (FKW00GA) – 5-HT1A receptor agonist, 5-HT2A receptor antagonist [3] Darigabat (PF-06372865) – GABAA receptor positive...
7 KB (554 words) - 02:36, 15 August 2024
NBUMP (category 5-HT1A agonists)
selective 5-HT1A receptor partial agonist (Ki = 0.1 nM; IA = 40%) with an arylpiperazine structure. It is one of the highest affinity ligands for the 5-HT1A receptor...
2 KB (90 words) - 08:10, 22 August 2022
activity at the following receptors: 5-HT1A receptor (as partial or full agonists) 5-HT2A receptor (as inverse agonists) D2 receptor (as antagonists or partial...
27 KB (2,701 words) - 16:17, 8 June 2024
selective 5-HT1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT1A receptors...
15 KB (1,537 words) - 23:08, 26 July 2024
It is a potent and selective 5-HT1A receptor full agonist. In recombinant cell lines expressing human 5-HT1A receptors, befiradol exhibits high agonist...
16 KB (1,607 words) - 09:40, 27 January 2024
complex range of interactions with the 5-HT1A, GABAA, adenosine A1, AMPA, mGluR2/3, mGlu5, and OX2 receptors. In the rat cerebellum, the protein has...
87 KB (9,542 words) - 16:05, 16 August 2024
Mirtazapine (category H1 receptor antagonists)
be a functional "indirect agonist" of the 5-HT1A receptor. Increased activation of the central 5-HT1A receptor is thought to be a major mediator of efficacy...
87 KB (7,810 words) - 06:35, 18 August 2024
Gepirone (category 5-HT1A agonists)
agonist of the serotonin 5-HT1A receptor. An active metabolite of gepirone, 1-(2-pyrimidinyl)piperazine, is an α2-adrenergic receptor antagonist. Gepirone...
17 KB (1,469 words) - 19:00, 27 March 2024
Brexpiprazole (category 5-HT1A agonists)
affinity for the 5-HT1A receptor, acting as a potent antagonist at 5-HT2A receptors, and a potent partial agonist at dopamine D2 receptors with lower intrinsic...
31 KB (2,342 words) - 16:44, 31 July 2024
(December 2002). "Serotonin mechanisms in heart valve disease II: the 5-HT2 receptor and its signaling pathway in aortic valve interstitial cells". The American...
32 KB (3,396 words) - 20:01, 14 August 2024
high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has...
6 KB (518 words) - 17:39, 12 August 2023
Vilazodone (category 5-HT1A agonists)
medications and is believed to work both as an SSRI and activator of the 5-HT1A receptor. Vilazodone was approved for medical use in the United States in 2011...
22 KB (1,721 words) - 05:27, 7 May 2024
Mefway is a serotonin 5-HT1A receptor antagonist used in medical research, usually in the form of mefway (18F) as a positron emission tomography (PET)...
9 KB (937 words) - 16:28, 7 November 2022
NMDA, 5-HT3, nicotinic antagonist and NOS inhibitor) Apraclonidine Brimonidine Cannabigerol (also acts as a moderate affinity 5-HT1A receptor antagonist...
25 KB (2,231 words) - 23:55, 13 July 2024
8-OH-DPAT (category 5-HT1A agonists)
5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to have been discovered. Originally believed to be selective for the 5-HT1A...
10 KB (875 words) - 21:03, 10 March 2024
system. Over time, this leads to a downregulation of pre-synaptic 5-HT1A receptors, which is associated with an improvement in passive stress tolerance...
101 KB (10,398 words) - 08:07, 2 August 2024
acts as a 5-HT1A receptor agonist (pKi = 9.3) with high efficacy and exceptional in vivo potency, and also as a 5-HT2A and 5-HT2C receptor antagonist...
4 KB (389 words) - 06:37, 19 May 2024
Piclozotan (SUN-N4057) is a selective 5-HT1A receptor partial agonist, which has neuroprotective effects in animal studies. It has been through early...
3 KB (170 words) - 17:26, 27 December 2022