mAChR1 Antagonist

mAChR1 Antagonists (20):

Cat. No.	Product Name	Effect	Purity

HY-107647

(S)-(+)-Dimethindene maleate	Antagonist	99.94%
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48).

HY-17037

Pirenzepine dihydrochloride	Antagonist	99.89%
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells.

HY-155367

mAChR antagonist 1	Antagonist	99.59%
mAChR antagonist 1 (compound 4a) is a mAChR antagonist with K_i values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively.

HY-A0082

Diphenidol hydrochloride	Antagonist	99.95%
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M₁-M₄ receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na⁺, K⁺, and Ca²⁺) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea.

HY-12100

Umeclidinium bromide	Antagonist	99.72%
Umeclidinium bromide is a novel mAChR antagonist. The affinity (K_i) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

HY-B0241

Ipratropium bromide	Antagonist	98.50%
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC₅₀s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.

HY-137976

Penehyclidine hydrochloride	Antagonist	≥99.0%
Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.

HY-14541S

Olanzapine-d₃	Antagonist	99.09%
Olanzapine-d₃ is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].

HY-I0230

Solifenacin hydrochloride	Antagonist	99.71%
Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

HY-101679

YM-58790	Antagonist	98.21%
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with K_i values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.

HY-142119

Penehyclidine	Antagonist
Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.

HY-A0002S

Solifenacin-d₅ succinate	Antagonist
Solifenacin-d₅ (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.

HY-101679A

YM-58790 free base	Antagonist
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with K_i values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.

HY-148527

LAS190792	Antagonist
LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC₅₀ 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.

HY-76570S1

5-Hydroxymethyl Tolterodine-d₁₄ formate	Antagonist
5-Hydroxymethyl Tolterodine-d₁₄ (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

HY-12100S

Umeclidinium-d₅ bromide	Antagonist
Umeclidinium-d₅ (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

HY-A0270

Diphenidol	Antagonist
Diphenidol is a non-selective muscarinic M₁-M₄ receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na⁺, K⁺, and Ca²⁺) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea.

HY-I0230S

Solifenacin-d₇ hydrochloride	Antagonist
Solifenacin-d₇ (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.

HY-12100S1

Umeclidinium-d₁₀ bromide	Antagonist
Umeclidinium-d₁₀ (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

HY-135329S

(1R,3S-)Solifenacin-d₅ hydrochloride	Antagonist
(1R,3S-)Solifenacin-d₅ (hydrochloride) is the deuterium labeled Solifenacin D5 hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively[1].

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