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*  Fenmetozole
It acts as an α2-adrenergic receptor antagonist similarly to other imidazoles like idazoxan. It was never marketed. ... "Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists". ... Fenmetozole (DH-524) is a drug which was patented as an antidepressant, but was later studied as an antagonist of the effects ...
*  Anxiolytic
The alpha1 antagonist prazosin could be effective for PTSD The Alpha2 adrenergic agonists Clonidine and guanfacine have ... Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... serotonin and adrenergic activity. Mebicar decreases the brain noradrenaline level, exerts no effect on the dopaminergic ...
*  Sympatholytic
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... ICI-118,551 Highly selective β2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ... ganglion type receptor antagonist) Peripherally acting Guanethidine (Magnesium-ATPase inhibitor) Indoramin (α1 antagonist) ...
*  Phentolamine
... (Regitine) is a reversible nonselective α-adrenergic antagonist. Its primary action is vasodilation due to α1 ... In response, the β1 adrenergic receptors on the heart increase its rate, contractility, and dromotropy, which help to offset ... as they can cause unopposed α-adrenergic mediated coronary vasoconstriction, worsening myocardial ischemia and hypertension. It ...
*  Receptor antagonist
Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... As for non-competitive antagonists and irreversible antagonists in functional assays with irreversible competitive antagonist ... A non-competitive antagonist is a type of insurmountable antagonist that may act in one of two ways: by binding to the active ... By definition, antagonists display no efficacy to activate the receptors they bind. Antagonists do not maintain the ability to ...
*  Peripherally selective drug
... a μ-opioid receptor antagonist used in the treatment of opioid-induced constipation Midodrine - an α1-adrenergic receptor ... α-Methylserotonin - a serotonin receptor agonist Alvimopan - a μ-opioid receptor antagonist used in the treatment of ... an adrenergic receptor agonist used as a cardiac stimulant and in the treatment of anaphylaxis Fenoldopam - a D1 receptor ... a D2 receptor antagonist used as an antiemetic, gastroprokinetic agent, and galactogogue Dopamine - a dopamine receptor agonist ...
*  R)-3-Nitrobiphenyline
... is a drug which acts as an α2-adrenergic agonist, selective for the α2C subtype, as well as being a weak ... antagonist at the α2A and α2B subtypes. Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, ... "Fruitful Adrenergic α2C-Agonism/α2A-Antagonism Combination to Prevent and Contrast Morphine Tolerance and Dependence". Journal ...
*  Sigma-1 receptor
... putative antagonist, selective against 5-HT1A, 5-HT6, 5-HT7, α1A and α2 adrenergic, and NMDA receptors NE-100 Positive ... Links between σ1 receptors and G-proteins have been suggested such as σ1 receptor antagonists showing GTP-sensitive high ... Antagonists: Sertraline S1RA 1-benzyl-6′-methoxy-6′,7′-dihydrospiro[piperidine-4,4′-thieno[3.2-c]pyran]: ... Brimson JM, Brown CA, Safrany ST (Sep 2011). "Antagonists show GTP-sensitive high-affinity binding to the sigma-1 receptor". ...
*  Brexpiprazole
It is also an antagonist of the serotonin 5-HT2A, 5-HT2B, and 5-HT7 receptors and the α1A-, α1B-, α1D-, and α2C-adrenergic ...
*  Hydroxyzine
In addition to its antihistamine activity, hydroxyzine has also been shown to act more weakly as an antagonist of the serotonin ... 5-HT2A receptor, the dopamine D2 receptor, and the α1-adrenergic receptor. The weak antiserotonergic effects of hydroxyzine ... Simons FE, Simons KJ, Frith EM (January 1984). "The pharmacokinetics and antihistaminic of the H1 receptor antagonist ... Paton DM, Webster DR (1985). "Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines)". Clin Pharmacokinet. ...
*  Amitriptylinoxide
... and H1 receptor antagonist, among other properties, but with approximately 60-fold lower affinity for the α1-adrenergic ...
*  Ritanserin
It has relatively low affinity for the H1, D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower ... Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in ... Ritanserin acts as a selective 5-HT2A (Ki = 0.45 nM) and 5-HT2C receptor (Ki = 0.71 nM) antagonist. ... a 5HT2A/2C antagonist, on negative symptoms of schizophrenia: A double-blind randomized placebo-controlled study". Progress in ...
*  Post-traumatic amnesia
Noradrenergic antagonists were not prescribed for the purposes of slowing the recovery of memory. Rather, these findings are ... The alpha-1 adrenergic receptor is specifically implicated. Although it has not yet been thoroughly investigated, there is ... Conversely, the administration of norpinephrine antagonists slowed recovery, and could lead to the reinstatement of deficits ...
*  Tricyclic antidepressant
In addition to their reuptake inhibition, many TCAs also have high affinity as antagonists at the 5-HT2 (5-HT2A and 5-HT2C), 5- ... HT6, 5-HT7, α1-adrenergic, and NMDA receptors, and as agonists at the sigma receptors (σ1 and σ2), some of which may contribute ... Tsai BS, Yellin TO (November 1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic ... the TCAs act as antagonists or inverse agonists of the receptors and as inhibitors of the transporters. Tianeptine is included ...
*  2C-H
It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat stomachs. It exhibits binding ... It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ...
*  Olanzapine
... is a potent antagonist of the muscarinic M3 receptor, which may underlie its diabetogenic side effects. Additionally ... Due to compensatory changes at dopamine, serotonin, adrenergic and histamine receptor sites in the central nervous system, ... high-affinity antagonist at the human dopamine D4 receptor". J. Pharmacol. Exp. Ther. 282 (2): 1011-9. PMID 9262370. Bymaster ... histamine H1 and alpha 1-adrenergic receptors in vitro". Schizophr. Res. 37 (1): 107-22. doi:10.1016/s0920-9964(98)00146-7. ...
*  Quinupramine
It has negligible affinity for the α1-adrenergic, α2-adrenergic, β-adrenergic, or D2 receptor. Clinically, quinupramine is ... and H1 receptor antagonist (antihistamine), moderate 5-HT2 receptor antagonist, and weak serotonin and norepinephrine reuptake ... Pharmacologically, quinupramine acts in vitro as a strong muscarinic acetylcholine receptor antagonist (anticholinergic) ...
*  Pharmaceutical drug
Beta2-adrenergic agonists, anticholinergics, Mast cell stabilizers. Leukotriene antagonists androgens, antiandrogens, estrogens ... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... General: adrenergic neurone blocker, astringent, ocular lubricant Diagnostic: topical anesthetics, sympathomimetics, ... H2-receptor antagonists, cytoprotectants, prostaglandin analogues Lower digestive tract: laxatives, antispasmodics, ...
*  SB-269970
2009). "5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig". Neuroreport. 20 (3): 325-330. doi ... A subsequent study in guinea pig at 10 uM showed that it also blocks the α2-adrenergic receptor activity. The significant ... Mnie-Filali O, Dahan L, Zimmer L, Haddjeri N (2007). "Effects of the serotonin 5-HT(7) receptor antagonist SB-269970 on the ... Gasbarri A, Cifariello A, Pompili A, Meneses A (2008). "Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and ...
*  Doxepin
... α1-adrenergic, and muscarinic acetylcholine receptors Moderate: 5-HT1 receptors Weak: α2-adrenergic and D2 receptors Based on ... In fact, doxepin has been said to be the most or one of the most potent H1 receptor antagonists available, with one study ... It is specifically an antagonist of the histamine H1 and H2 receptors, the serotonin 5-HT2A and 5-HT2C receptors, the α1- ... Antagonism of the H1, 5-HT2A, 5-HT2C, and α1-adrenergic receptors is thought to have sleep-promoting effects and to be ...
*  Triazoledione
Serotonin antagonist and reuptake inhibitor Alan F. Schatzberg, M.D.; Charles B. Nemeroff, M.D., Ph.D. (2017). The American ... Triazoledione shows significant affinity for the serotonin 5-HT1A and 5-HT2A receptors, the α1-adrenergic receptor, and the ...
*  Imipramine
The drug appears to work by increasing levels of serotonin and norepinephrine and by blocking certain serotonin, adrenergic, ... imipramine is an antagonist of the histamine H1 receptors. BDNF: BDNF is implicated in neurogenesis in the hippocampus, and ... Epinephrine: imipramine antagonizes adrenergic receptors, thus sometimes causing orthostatic hypotension. Sigma receptor: ... specifically an antagonist of the muscarinic acetylcholine receptors. Thus, it is prescribed with caution to the elderly and ...
*  Clorotepine
... and α1D-adrenergic receptors, and the histamine H1 receptors, where it has been it has been confirmed to act as an antagonist ( ... pharmacophore for D2 receptor antagonists. Metitepine Perathiepin Index nominum 2000: international drug directory. Taylor & ... biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists ...
*  Phenylethanolamine
... considered to be a selective β3-antagonist). Using a β2 adrenergic receptor preparation derived from transfected HEK 293 cells ... considered to be a selective β1-antagonist), and ICI 118,551 (considered to be a selective β2-antagonist), but not by SR 59230A ... These and other observations were suggested to be consistent with an action on α- and β-adrenergic receptors. Research by ... Named imprecisely as "hydroxyphenethylamine" Considered to be an antagonist of β1 and β2 receptors, and an agonist of β3 ...
*  Lurasidone
... acts as an antagonist of the dopamine D2 and D3 receptors, the serotonin 5-HT2A and 5-HT7 receptors, and the α2C- ... adrenergic receptor, and as a partial agonist of the serotonin 5-HT1A receptor. It has only low and likely clinically ...
*  Amesergide
The drug is a potent antagonist of the α2-adrenergic receptor in addition to the 5-HT2 receptors via its major active ... Amesergide acts as a selective antagonist of the serotonin 5-HT2A, 5-HT2B, 5-HT2C receptors (Ki = 1.96-15.1 nM). It is also an ... Cohen ML, Kurz KD, Fuller RW, Calligaro DO (1994). "Comparative 5-HT2-receptor antagonist activity of amesergide and its active ... Amesergide (INN, USAN; developmental code name LY-237733) is a serotonin receptor antagonist of the ergoline and lysergamide ...
*  MIN-117
... and α1B-adrenergic receptors. As of May 2015, MIN-117 is in phase II clinical trials for MDD. List of investigational ... It is described as a 5-HT1A and 5-HT2A receptor antagonist and inhibitor of serotonin and dopamine reuptake, and is also ...