α1a-adrenergic receptor

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.

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

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

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

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

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.

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.

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.

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

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

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

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.

Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

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

Cirazoline hydrochloride is a competitive full agonist of the α1A-adrenergic receptor (α1A-AR; Ki: 120 nM). It is a partial agonist at α1B-AR (Ki: 960 nM) and α1D-AR (Ki: 660 nM).

Silodosin glucuronide is an active metabolite of the α1A-adrenergic receptor antagonist silodosin . It is formed from silodosin by the UDP-glucuronosyltransferase (UGT) isoform UGT2B7. Silodosin glucuronide is toxic to rats with an LD50 value of 0.347 mg/kg.

Conopeptide rho-TIA, a peptide from Conus tulipa venom, acts as a selective, noncompetitive inhibitor at the human α1B-Adrenergic Receptor and as a competitive inhibitor at the α1A and α1D-Adrenergic Receptors. Binding to these subtypes, conopeptide rho-TIA may inform the creation of new α1-Adrenergic Receptor subtype-selective drugs [1].

Buflomedil is a vasoactive compound. Buflomedil has been used for peripheral arterial diseases.

Fiduxosin hydrochloride is an alpha 1a-adrenoceptor antagonist that may be useful in the treatment of Benign Prostatic Hyperplasia.