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Results for "

hypotension

" in MedChemExpress (MCE) Product Catalog:

50

Inhibitors & Agonists

2

Biochemical Assay Reagents

8

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2

Natural
Products

3

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W702027
    Deterenol hydrochloride

    AL842

    		 Adrenergic Receptor Cardiovascular Disease
    Deterenol hydrochloride (AL842) is a selective beta-agonist. Deterenol hydrochloride causes vasodepressor, anxiety, increasing heart rate, hypotension palpitation and respiratory distress .
    Deterenol hydrochloride
  • HY-13458
    Droxidopa

    L-DOPS; DOPS; SM5688

    		 Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) .
    Droxidopa
  • HY-A0144A
    Etilefrine hydrochloride

    		AMPK Adrenergic Receptor Cardiovascular Disease
    Etilefrine hydrochloride is an orally active α adrenergic agonist. Etilefrine hydrochloride is also an AMPK activator. Etilefrine hydrochloride can be used for the research of postural hypotension .
    Etilefrine hydrochloride
  • HY-B1231
    Heptaminol hydrochloride

    RP-2831 hydrochloride

    		 Others Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels .
    Heptaminol hydrochloride
  • HY-A0144
    Etilefrine

    		Adrenergic Receptor AMPK Cardiovascular Disease
    Etilefrine (3-[2-(ethylamino)-1-hydroxyethyl]phenol) is an α adrenergic agonist . Etilefrine also is an AMPK activator . Etilefrine can be used for the research of postural hypotension .
    Etilefrine
  • HY-13458A
    Droxidopa hydrochloride

    L-DOPS hydrochloride; DOPS hydrochloride; SM5688 hydrochloride

    		 Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) .
    Droxidopa hydrochloride
  • HY-13458R
    Droxidopa (Standard)

    		Adrenergic Receptor Neurological Disease
    Droxidopa (Standard) is the analytical standard of Droxidopa. This product is intended for research and analytical applications. Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) .
    Droxidopa (Standard)
  • HY-126645
    Atelopidtoxin

    		Sodium Channel Cardiovascular Disease
    Atelopidtoxin (zetekitoxin) is a toxin (LD50=0.016 mg/kg for mice), which can be isolated from Panamanian frog Atelopus zeteki. Atelopidtoxin causes hypotension and ventricular fibrillation in rabbits. Atelopidtoxin an inhibitor for sodium channel .
    Atelopidtoxin
  • HY-105790
    Piperilate

    Pipethanate

    		 Cholinesterase (ChE) Cardiovascular Disease
    Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates .
    Piperilate
  • HY-105790A
    Piperilate hydrochloride

    		Cholinesterase (ChE) Cardiovascular Disease
    Piperilate (Pipethanate) hydrochloride is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate hydrochloride also causes hypotension and rescues mice poisoned by the organophosphates .
    Piperilate hydrochloride
  • HY-P1106A
    K41498 TFA

    		CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study .
    K41498 TFA
  • HY-B1231R
    Heptaminol hydrochloride (Standard)

    		Others Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Heptaminol (hydrochloride) (Standard) is the analytical standard of Heptaminol (hydrochloride). This product is intended for research and analytical applications. Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels .
    Heptaminol hydrochloride (Standard)
  • HY-109897
    CV-6209

    		Platelet-activating Factor Receptor (PAFR) Cardiovascular Disease
    CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats .
    CV-6209
  • HY-13575A
    Blonanserin dihydrochloride

    AD-5423 dihydrochloride

    		 5-HT Receptor Dopamine Receptor Adrenergic Receptor Sigma Receptor Cardiovascular Disease Neurological Disease
    Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension .
    Blonanserin dihydrochloride
  • HY-18734A
    Carboxy-PTIO potassium
    4 Publications Verification

    		 NO Synthase Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Carboxy-PTIO potassium is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO potassium can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model .
    Carboxy-PTIO potassium
  • HY-18734
    Carboxy-PTIO

    		NO Synthase Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Carboxy-PTIO is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model .
    Carboxy-PTIO
  • HY-P3419
    PAMP-12 (unmodified)

    		Mas-related G-protein-coupled Receptor (MRGPR) Cardiovascular Disease
    PAMP-12 (unmodified) is a potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM). PAMP-12 (unmodified) is an endogenous peptide that elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells .
    PAMP-12 (unmodified)
  • HY-13575
    Blonanserin

    AD-5423

    		 5-HT Receptor Dopamine Receptor Adrenergic Receptor Sigma Receptor Cardiovascular Disease Neurological Disease
    Blonanserin (AD-5423) is a potent?and orally active 5-HT2A?(Ki=0.812 nM) and?dopamine D2?receptor?(Ki =0.142?nM)?antagonist. Blonanserin is usually acts as an atypical antipsychotic?agent and can be used for the research of extrapyramidal symptoms, excessive?sedation, or?hypotension .
    Blonanserin
  • HY-13575R
    Blonanserin (Standard)

    		5-HT Receptor Dopamine Receptor Adrenergic Receptor Sigma Receptor Neurological Disease
    Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension .
    Blonanserin (Standard)
  • HY-120476
    JNJ-39729209

    		TRP Channel Neurological Disease Inflammation/Immunology
    JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs .
    JNJ-39729209
  • HY-17416A
    Guanfacine

    		Adrenergic Receptor Cardiovascular Disease Neurological Disease Endocrinology
    Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine
  • HY-17416
    Guanfacine hydrochloride
    2 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology
    Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine hydrochloride
  • HY-17416S2
    Guanfacine-13C,d5 hydrochloride

    		Adrenergic Receptor Isotope-Labeled Compounds Cardiovascular Disease Endocrinology
    Guanfacine- 13C,d5 hydrochloride is the deuterium and 13C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine-13C,d5 hydrochloride
  • HY-17416R
    Guanfacine hydrochloride (Standard)

    		Adrenergic Receptor Cardiovascular Disease Endocrinology
    Guanfacine (hydrochloride) (Standard) is the analytical standard of Guanfacine (hydrochloride). This product is intended for research and analytical applications. Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine hydrochloride (Standard)
  • HY-17416AS1
    Guanfacine-15N3,13C2

    		Adrenergic Receptor Isotope-Labeled Compounds Neurological Disease Endocrinology
    Guanfacine- 15N3, 13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine-15N3,13C2
  • HY-12749
    Midodrine

    (±)-Midodrin

    		 Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Midodrine is an α1-receptor agonist, for the treatment of dysautonomia and orthostatic hypotension.
    Midodrine
  • HY-12749A
    Midodrine hydrochloride

    (±)-Midodrine hydrochloride

    		 Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Midodrine hydrochloride ((±)-Midodrine hydrochloride) is an α1-receptor agonist, for the treatment of dysautonomia and orthostatic hypotension.
    Midodrine hydrochloride
  • HY-117541
    Glycyl-glutamine

    Glycyl-L-glutamine

    		 Others Neurological Disease
    Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems . Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln) .
    Glycyl-glutamine
  • HY-117765
    RS-5773

    		Calcium Channel Cardiovascular Disease Neurological Disease
    RS-5773 is a calcium channel inhibitor and a diltiazem congener. RS-5773 has antianginal effect and does not cause excessive hypotension or depression of atrioventricular conduction .
    RS-5773
  • HY-119541
    Ampreloxetine

    TD-9855

    		 5-HT Receptor Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension .
    Ampreloxetine
  • HY-119541A
    Ampreloxetine TFA

    TD-9855 TFA

    		 5-HT Receptor Adrenergic Receptor Cardiovascular Disease Neurological Disease
    Ampreloxetine (TD-9855) TFA is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine TFA has the potential for the research of neurogenic orthostatic hypotension .
    Ampreloxetine TFA
  • HY-12749B
    (R)-Midodrine hydrochloride

    		Others Cardiovascular Disease
    (R)-Midodrine hydrochloride is a vasopressor used as an antihypertensive agent for the treatment of symptomatic postural hypotension, exhibiting peripheral alpha(1)-adrenoreceptor agonistic activity that induces venous and arterial vasoconstriction.
    (R)-Midodrine hydrochloride
  • HY-107037
    Tolmesoxide

    RX71107

    		 Others Cardiovascular Disease
    Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina .
    Tolmesoxide
  • HY-P1694
    B4148

    		Bradykinin Receptor Cardiovascular Disease
    B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
    B4148
  • HY-P3419A
    PAMP-12 (unmodified) (TFA)

    		Mas-related G-protein-coupled Receptor (MRGPR) Cardiovascular Disease
    PAMP-12 (unmodified) TFA is a potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM). PAMP-12 (unmodified) is an endogenous peptide that elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells .
    PAMP-12 (unmodified) (TFA)
  • HY-112071A
    Prenalterol hydrochloride

    		Adrenergic Receptor Endocrinology
    Prenalterol hydrochloride is a partial adrenal agonist with functional β1-receptor specificity and positive inotropic effects. Prenalterol hydrochloride is effective in suppressing acute heart failure, low output syndrome after myocardial infarction, shock, and reducing orthostatic hypotension in Shy-Drager syndrome .
    Prenalterol hydrochloride
  • HY-P3057
    [D-Trp11]-Neurotensin

    		Neurotensin Receptor Cardiovascular Disease Neurological Disease
    [D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension .
    [D-Trp11]-Neurotensin
  • HY-130345
    PAF (C18)

    		Platelet-activating Factor Receptor (PAFR) Cardiovascular Disease
    C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .
    PAF (C18)
  • HY-19126
    CL-184005

    		Platelet-activating Factor Receptor (PAFR) Infection Cardiovascular Disease
    CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
    CL-184005
  • HY-122489A
    (S)-Laudanosine

    		Others Cardiovascular Disease Neurological Disease
    (S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
    (S)-Laudanosine
  • HY-B1116A
    Metaraminol

    (-)-Metaraminol; (-)-erythro-Metaraminol; (-)-m-Hydroxynorephedrine

    		 Others Neurological Disease
    Metaraminol ((-)-Metaraminol) is a sympathomimetic compound with activity that acts primarily at alpha-1 adrenergic receptors. Metaraminol is used to inhibit hypotension due to vasodilation, particularly in critically ill patients who do not respond well to volume resuscitation. Metaraminol may also be used as an adjunct to help improve cardiac contractility. The use of metaraminol may be supported by less evidence, but its effectiveness in specific situations remains of interest .
    Metaraminol
  • HY-119200
    LY-195448 hydrochloride

    		Others Cancer
    LY-195448 hydrochloride is a phenethanolamine that exhibits anti-tumour activity across various murine tumour models. LY-195448 hydrochloride acts by blocking cells at metaphase. LY-195448 hydrochloride has demonstrated a lack of "standard" side effects commonly associated with cancer treatments, such as myelosuppression and gastrointestinal toxicity. LY-195448 hydrochloride was evaluated in a phase I trial, where it showed only mild and reversible side effects like hypotension, tachycardia, and tremor.
    LY-195448 hydrochloride
  • HY-17416AS
    Guanfacine-13C,15N3

    		Adrenergic Receptor Neurological Disease
    Guanfacine- 13C, 15N3 is the 13C and 15N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].
    Guanfacine-13C,15N3
  • HY-P3849
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)

    LMN-NKA

    		 Neurokinin Receptor Neurological Disease
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
  • HY-P1106
    K41498

    		CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study .
    K41498
  • HY-79457
    S-Methylisothiourea sulfate
    1 Publications Verification

    		 NO Synthase HSV Infection Inflammation/Immunology
    S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock .
    S-Methylisothiourea sulfate
  • HY-W328882
    3-(2-Aminopropyl)phenol

    		Others Cardiovascular Disease
    3-(2-Aminopropyl)phenol is a biologically active compound with significant blood pressure-raising activity. 3-(2-Aminopropyl)phenol can effectively improve the symptoms of orthostatic hypotension in patients. 3-(2-Aminopropyl)phenol can significantly increase blood pressure at rest and when standing after oral administration. 3-(2-Aminopropyl)phenol can help reduce pathological orthostatic adjustment disorders. 3-(2-Aminopropyl)phenol has a relatively small effect on heart rate, and no significant side effects have been observed .
    3-(2-Aminopropyl)phenol
  • HY-121354
    Hydracarbazine

    		Others Cardiovascular Disease
    Hydracarbazine is a pyridazine. Hydracarbazine can effectively lower blood pressure, it can be used for the research of high blood pressure .
    Hydracarbazine
  • HY-155297
    Nebidrazine

    FLA-136

    		 Histamine Receptor Cardiovascular Disease
    Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
    Nebidrazine
  • HY-136625
    LY134046

    		Others Neurological Disease
    LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT). Its cardiovascular activity was studied in anesthetized spontaneously hypertensive rats (SHR). Acute intraperitoneal injection of 10 and 20 mg/kg of LY134046 caused minimal cardiovascular changes, while 40 mg/kg resulted in a sustained decrease in mean arterial blood pressure and heart rate. This hypotension and bradycardia occurred rapidly and occurred when brain NMT activity was significantly inhibited. However, norepinephrine concentrations in rat brains were not significantly reduced at the time when LY134046-induced blood pressure and heart rate effects were maximal. The acute cardiovascular activity of LY134046 was not significantly affected by pretreatment of SHR with phentolamine, propranolol, or atropine, and LY134046 reduced heart rate in suspended SHR. In addition, acute or chronic administration of LY134046 did not antagonize the vasoconstrictor responses induced by sympathetic nerve stimulation or exogenous norepinephrine. These observations suggest that LY134046 does not interact with adrenergic or cholinergic receptors and that its hypotensive and bradycardic effects do not require neurogenic tension. Chronic intraperitoneal administration of LY134046 (40 mg/kg/day) resulted in a sustained and significant inhibition of hypothalamic and brainstem NMT activity, leading to central norepinephrine depletion. During chronic treatment, norepinephrine and dopamine concentrations increased in the brainstem and hypothalamus of SHR. Despite chronic inhibition of central NMT and norepinephrine depletion, cardiovascular parameters in SHR treated groups were not significantly different from those in saline-injected controls. Chronic treatment with LY134046 did not result in tolerance to its central biochemical effects or acute cardiovascular activity. The present study does not support the idea that norepinephrine-producing neurons are involved in the central regulation of cardiovascular function, because the hypotension and bradycardia induced by acute administration of LY134046 occurred before a significant decrease in hypothalamic norepinephrine concentrations, whereas chronic inhibition of central NMT and depletion of norepinephrine resulted in minimal changes in baseline cardiovascular parameters.
    LY134046

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