5-HT1A antagonists

Propranolol is a medication of the beta blocker class. It is used to treat high blood pressure, some types of irregular heart rate, thyrotoxicosis, capillary hemangiomas, akathisia, performance anxiety, and essential tremors, as well as to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks. It can be taken orally, rectally, or by intravenous injection. The formulation that is taken orally comes in short-acting and long-acting versions. Propranolol appears in the blood after 30 minutes and has a maximum effect between 60 and 90 minut

Pindolol, sold under the brand name Visken among others, is a non-selective beta blocker which is used in the treatment of 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 therapy to various antidepressants, such as clomipramine and the selective serotonin reuptake inhibitors (SSRIs), in the treatment of depression and obsessive–compulsive disorder (OCD).

Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.

Oxprenolol, sold under the brand name Trasicor among others, is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure.

Alprenolol, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as a 5-HT1A and 5-HT1B receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

Penbutolol (brand names Levatol, Levatolol, Lobeta, Paginol, Hostabloc, Betapressin) is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors.

Nicergoline, sold under the brand name Sermion among others, is an ergot derivative used to treat senile dementia and other disorders with vascular origins. Internationally it has been used for frontotemporal dementia as well as early onset in Lewy body dementia and Parkinson's dementia. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Unlike many other ergolines, such as ergotamine, nicergoline is not associate

Cannabigerol (CBG) is a non-psychoactive cannabinoid and minor constituent of cannabis. It is one of more than 120identified cannabinoids found in the plant genus Cannabis. The compound is the decarboxylated form of cannabigerolic acid (CBGA), the parent molecule from which other cannabinoids are biosynthesized.

Tertatolol (Artex, Artexal, Prenalex) is a medication in the class of beta blockers, used in the treatment of high blood pressure. It was discovered by the French pharmaceutical company Servier and is marketed in Europe.

Metitepine (; developmental code names Ro 8-6837 (maleate), VUFB-6276 (mesylate)), also known as methiothepin, is a drug described as a "psychotropic agent" of the tricyclic or tetracyclic group which was never marketed.

Spiroxatrine (Spiroxamide, R5188) is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects and a relatively weak opioid action.

Iodocyanopindolol (), also known as ICYP, is a synthetic compound derived from pindolol, primarily used as a radioligand in pharmacological research. It functions as a non-selective β-adrenoceptor antagonist and a serotonin 5-HT1A and 5-HT1B receptor antagonist. Its 125I-radiolabelled derivative, [125I]-iodocyanopindolol ([125I]-ICYP), is widely employed to map the distribution and density of β-adrenoceptors and serotonin receptors in tissues, particularly in the brain, heart, and other organs. Iodocyanopindolol is not used clinically but remains a critical tool in studying receptor pharmacolo

Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.

UH-301, also known as '(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin ((S)-5-FHDPAT'), is a drug and research chemical widely used in scientific studies. It acts as a selective serotonin 5-HT1A receptor silent antagonist. It is structurally related to 8-OH-DPAT. UH-301 was found to produce a head-twitch response in mice which is usually typical of 5-HT2A agonist drugs, and has subsequently been used to investigate how 5-HT1A receptor activity modulates 5-HT2A receptors downstream.

Isamoltane (developmental code name CGP-361A) is a beta blocker (β-adrenergic receptor antagonist) with additional serotonin 5-HT1A and 5-HT1B receptor antagonist activity. It has about 5-fold higher affinity for the serotonin 5-HT1B receptor (Ki = 21nM) over the serotonin 5-HT1A receptor (Ki = 112nM). It has anxiolytic effects in rodents. The drug was under development by Novartis and AstraZeneca for the treatment of anxiety disorders in the 1990s but was never marketed.

Robalzotan (, ; developmental code names NAD-299, AZD-7371) is a selective antagonist at the serotonin 5-HT1A receptor which was under development for the treatment of major depressive disorder, anxiety disorders, gastrointestinal disorders, irritable bowel syndrome (IBS), and overactive bladder.

NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. The new finding has raised significant concerns about studies using NAN-190 as a specific serotonin receptor antagonist.

Xylamidine is a drug which acts as an antagonist of the serotonin 5-HT2A and 5-HT2C receptors, and to a lesser extent of the serotonin 5-HT1A receptor. The drug does not cross the blood–brain barrier and hence is peripherally selective, which makes it useful for blocking peripheral serotonergic responses like cardiovascular and gastrointestinal effects, without producing the central effects of 5-HT2A receptor blockade such as sedation, or interfering with the central actions of 5-HT2A receptor agonists.

Lecozotan is an investigational drug by Wyeth tested for improvement of cognitive functions of Alzheimer's disease patients. , the first Phase III clinical trial has been completed.

Pindobind is a compound developed by researchers associated with Stanford University, identified as a central nervous system depressant, which generated a response in animals reducing offensive actions such as chasing, while also notably reducing tendencies of the test animal to evade when stimulated to do so. It acts as an irreversible beta blocker and irreversible 5-HT1A receptor antagonist.