α1a

RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays.

Nicergoline (Nicergolinum) is an ergot derivative used to treat senile dementia and other disorders with vascular origins.

α1A-AR Degrader 9c is a potent, selective, and reversible PROTAC degrader targeting the α1A adrenergic receptor (α1A-AR) with a DC50 of 2.86 μM. It promotes the proteasomal degradation of the α1A-AR and exhibits anti-proliferative effects against PC-3 cells, presenting an IC50 value of 6.12 μM. This compound demonstrates antitumor activity and holds potential for prostate cancer research [1].

Tamsulosin hydrochloride (Flomax hydrochloride) is the hydrochloride salt of tamsulosin, a sulfonamide derivative with α1 adrenergic antagonist activity.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

L-771688 (SNAP 6383) is a novel potent and selective α1A-adrenoceptor antagonist with a Ki value of 0.43±0.02 nM.L-771688 KE is used for the treatment of benign prostatic hyperplasia.

Rec 15/2615 dihydrochloride is an antagonist of α1B-adrenergic receptor.

(S)-(+)-Niguldipine hydrochloride is a selective α1A-AR antagonist used in the study of depression and epilepsy.

ZY-19489 is an antimalarial compound that is a potential single-dose cure for Plasmodium falciparum and Plasmodium vivax malaria. It has received orphan drug designation from the FDA.

Ensaculin (Anseculin), a novel benzopyrone partially substituted with piperazine, showed memory-enhancing effects in passive and conditioned avoidance paradigms in normal and artificially amnesic rodents. It showed neuroprotective activity in a model of NMDA toxicity and neurotrophic effects in primary cultured rat brain cells.Ensaculin can be used for the treatment of dementia.

Nemazoline Free Base acts as an α1-adrenergic agonist and an α2-adrenergic antagonist, and may be used in the treatment of trace amine-associated receptor-related disorders.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Xylometazoline hydrochloride (Xylometazoline HCl) is an α-adrenoceptor agonist usually used as nasal decongestant.

Buflomedil hydrochloride (Fonzylane), a vasodilator, is used in therapy of claudication or the symptoms of the peripheral arterial disease.

Phenylephrine hydrochloride (NCI-c55641) is a selective agonist of the α1-adrenergic receptor.

Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Phenylephrine ((R)-(-)-Phenylephrine) is a selective α1-adrenoceptor agonist ( pKi: 5.86, 4.87 and 4.70 for α1D, α1B, and α1A receptors respectively).

Dabuzalgron (Ro 115-1240), an orally active selective alpha-1A adrenergic receptor agonist, is used to treat urinary incontinence and prevents doxorubicin-induced cardiotoxicity by maintaining mitochondrial function.

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

Tamsulosin ((R)-(-)-YM12617 free base) is an alpha1A adrenergic receptor antagonist used for the symptomatic treatment of benign prostatic hyperplasia (BPH). It treats difficulty urinating, a common symptom of an enlarged prostate, by relaxing the neck muscles of the bladder and muscle fibers in the prostate itself, easing urination.