pressor

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

Lac repressor fragment 33-38 Lys-Arg-Glu-Lys-Val fragment from lac repressor.

p53 tumor suppressor fragment (232-240) is a peptide with the sequence H2N-Lys-Tyr-Met-Cys-Asn-Ser-Ser-Cys-Met-OH, MW= 1066.3. p53 is a tumor suppressor protein that in humans is encoded by the TP53 gene. p53 is crucial in multicellular organisms, where i

N6-Cyclohexyladenosine (CHA) is a selective agonist of A1 receptor with EC50 of 8.2 Nm. N6-Cyclohexyladenosine exerts anticonvulsant effects and protects against neuronal death. CHA was also found to inhibit the pressor effects of lumbar sympathetic nerve stimulation in rats.

Human Big ET-1 comprises residues 53-90 of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (hET-1), the peptide show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-53-7.

The big endothelins comprise residues 53-90 (human big ET-1) and 53-91 (porcine big ET-1) of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (ET-1), both peptides show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-54-8.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats.

Pentoprilat is a member of a series of l-glutarylindoline-2(S)-carboxylic acid derivatives. Pentopril was evaluated as an inhibitor of a cell-free preparation of angiotensin-converting enzyme (ACE) isolated from rabbit lung. Intravenous administration of incremental doses of pentopril to anesthetized normotensive rats produced a dose-related inhibition of angiotensin I (AI) pressor responses. The onset of inhibition of the A1 pressor response was rapid, and substantial inhibition occurred at 5 min after administration of the ACE inhibitors. Pentopril hydrolyzed in vivo to the biologically active free-acid form of CGS 13934. It was well tolerated in normal volunteers and hypertensive patients. Pentopril was developed for the treatment of both hypertension and congestive heart failure. Pentopril produced little clinical improvement and no biochemical improvement in a patients with rheumatoid arthritis.

FRAN-12 is a histamine and 5-hydroxytryptamine antagonist with pressor properties.

Quinapril-d5 is intended for use as an internal standard for the quantification of quinapril by GC- or LC-MS. Quinapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor quinaprilat. In vivo, quinapril reduces mean arterial pressure in renal hypertensive and spontaneously hypertensive rats. It inhibits angiotensin I-induced pressor responses in normotensive rats and dogs. Quinapril prevents left ventricular heart failure in CHF 14.6 cardiomyopathic hamsters. Formulations containing quinapril have been used in the treatment of hypertension, heart failure, and diabetic nephropathy.

Fosinopril-d7 is intended for use as an internal standard for the quantification of fosinopril by GC- or LC-MS. Fosinopril is a prodrug form of the angiotensin-converting enzyme inhibitor fosinoprilat. Oral administration of fosinopril inhibits angiotensin I-induced pressor responses in normotensive rats, dogs, and monkeys when administered at doses of 15, 15, and 10 µmol kg, respectively. Fosinopril reduces fractional shortening and decreases left ventricular size in a porcine model of congestive heart failure. Formulations containing fosinopril have been used in the treatment of hypertension and congestive heart failure.

Gepefrine, an orally active pressor and sympathomimetic agent, enhances the initial orthostatic regulation of arterial pressure.

Adrenomedullin (16-31), human TFA, a fragment containing amino acid residues 16-31 of human adrenomedullin (hADM), demonstrates significant CGRP1 receptor affinity and exhibits pressor activity in the rat systemic vascular bed while lacking this effect in cats [1].

EC33, a selective aminopeptidase A (APA) inhibitor, blocks the pressor response of exogenous Ang II and does not cross the blood-brain barrier, making it a potential candidate for salt-dependent hypertension research [1].

Bethanidine sulfate and its ortho-chloro derivative (BW 392C60) are potent adrenergic neuron blockers exhibiting sympathomimetic effects similar to those of bromobenzamine and guanethidine in various animal models, particularly in cats. These compounds inhibit the release of norepinephrine during neural stimulation and enhance the responsiveness of smooth muscle to epinephrine and norepinephrine. Notably, bethanidine sulfate increases the pressor response to tyramine, although this effect diminishes with higher doses. Unlike guanethidine, bethanidine sulfate does not deplete pressor amines in the iris of cats following administration. Additionally, it temporarily suppresses autonomic cholinergic mechanisms and can cause transient neuromuscular paralysis at large doses, contrasting its long-term adrenergic neuron blocking effects.

JKC 301, a selective Endothelin A receptor antagonist, attenuates the pressor effects of nicotine in rats and can be used to study cardiovascular disease caused by smoking [1] [2].