α1a

α1A/1D-Adrenoceptor antagonist-1 is a dual-targeting adrenoceptor antagonist exhibiting exceedingly high binding affinity for both alpha 1A and alpha 1D subtypes. It significantly reduces urethral resistance by specifically blocking smooth muscle contraction in the lower urinary tract and prostate, serving as an important tool for investigating benign prostatic hyperplasia (BPH) and hypertension mechanisms.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

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.

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.

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.

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.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

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.

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.

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

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).

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

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.

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.

(R)-Terazosin is an active R-enantiomer of Terazosin and a potent antagonist of α1-adrenoceptor [(α1a, α1b, and α1d-adrenoceptor] with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively).

(S)-Terazosin is an active S-enantiomer of Terazosin and acts as a potent, high-affinity antagonist of α-adrenoceptors [α1a, α1b, and α1d-adrenoceptors] with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively.

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

A 61603 is an α1A adrenergic receptor agonist that is subtype-selective for α1A receptors. A 61603 can be used to study adrenergic function and α1A adrenergic receptor regulation.

Alfuzosin (SL 77499) is an orally available, competitive α1-adrenoceptor antagonist.Alfuzosin induces smooth muscle relaxation in the bladder neck and prostate.Alfuzosin has been used to study benign prostatic hypertrophy, lower urinary tract symptoms (LUTS), and ejaculatory dysfunction (EjD).