Biomaterial Database

On the postjunctional alpha-adrenoreceptors in rat cerebral and mesenteric arteries. 1984

E D Högestätt, and K E Andersson

The contractile response to exogenously applied noradrenaline (NA) was examined in vitro in tubal segments (0.2-0.1 mm in diameter) of rat middle cerebral (MCA), basilar (BA) and mesenteric (MA) arteries. In the MCA, the maximum contractile response to NA (10(-4)M) was considerably smaller than that induced by K+ (124 mM) or 5-hydroxytryptamine (10(-5)M), whereas the inverse relationship was found in the MA. NA usually failed to elicit contraction in the BA even in the presence of propranolol and cocaine. In the MCA, propranolol (3 X 10(-7)M) enhanced the maximum contractile response to NA by approximately 100% without affecting the potency of the agonist. In the MA, propranolol had no effect on the concentration-response relationship for NA. Cocaine (10(-5)M) or 6-hydroxydopamine pretreatment increased the NA sensitivity of the MA by a factor of three, whereas these procedures failed to influence the NA sensitivity of the MCA. A marked stereoselectivity was found in the MCA, as (-)-NA was more than 100 times more potent than (+)-NA as a contractile agent. The order of potency of a series of alpha-adrenoreceptor agonists was (-)-adrenaline greater than oxymetazoline greater than (+/-)-NA approximately (-)-phenylephrine greater than methoxamine in the MCA and (+/-)-NA greater than (-)-phenylephrine in the MA. Clonidine failed to elicit contraction in concentrations lower than 3 X 10(-4)M in both types of artery. Prazosin was between three and four orders of magnitude more potent than rauwolscine in inhibiting NA-induced contractions in the MCA and MA. The pA2 values for, respectively, prazosin and rauwolscine were 9.3 and 5.4 in the MCA and 9.7 and 6.8 in the MA. The slope of the Schild plot deviated significantly from unity only for rauwolscine in the MA (0.64). It is concluded that the contractile response to exogenous NA in the MCA and MA is mediated mainly by stimulation of alpha 1-adrenoreceptors, although a small contribution of postjunctional alpha 2-adrenoreceptors in the MA cannot be excluded. In contrast to the MCA, the BA appears to lack contraction-mediating alpha-adrenoreceptors, indicating regional differences in the alpha-adrenoreceptor distribution in the rat cerebrovascular bed.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D008638	Mesenteric Arteries	Arteries which arise from the abdominal aorta and distribute to most of the intestines.	Arteries, Mesenteric,Artery, Mesenteric,Mesenteric Artery
D009119	Muscle Contraction	A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009638	Norepinephrine	Precursor of epinephrine that is secreted by the ADRENAL MEDULLA and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers, and of the diffuse projection system in the brain that arises from the LOCUS CERULEUS. It is also found in plants and is used pharmacologically as a sympathomimetic.	Levarterenol,Levonorepinephrine,Noradrenaline,Arterenol,Levonor,Levophed,Levophed Bitartrate,Noradrenaline Bitartrate,Noradrénaline tartrate renaudin,Norepinephrin d-Tartrate (1:1),Norepinephrine Bitartrate,Norepinephrine Hydrochloride,Norepinephrine Hydrochloride, (+)-Isomer,Norepinephrine Hydrochloride, (+,-)-Isomer,Norepinephrine d-Tartrate (1:1),Norepinephrine l-Tartrate (1:1),Norepinephrine l-Tartrate (1:1), (+,-)-Isomer,Norepinephrine l-Tartrate (1:1), Monohydrate,Norepinephrine l-Tartrate (1:1), Monohydrate, (+)-Isomer,Norepinephrine l-Tartrate (1:2),Norepinephrine l-Tartrate, (+)-Isomer,Norepinephrine, (+)-Isomer,Norepinephrine, (+,-)-Isomer
D011433	Propranolol	A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.	Dexpropranolol,AY-20694,Anaprilin,Anapriline,Avlocardyl,Betadren,Dociton,Inderal,Obsidan,Obzidan,Propanolol,Propranolol Hydrochloride,Rexigen,AY 20694,AY20694,Hydrochloride, Propranolol
D011919	Rats, Inbred Strains	Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.	August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D011942	Receptors, Adrenergic, alpha	One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.	Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D002536	Cerebral Arteries	The arterial blood vessels supplying the CEREBRUM.	Arteries, Cerebral,Artery, Cerebral,Cerebral Artery
D003042	Cocaine	An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.	Cocaine HCl,Cocaine Hydrochloride,HCl, Cocaine,Hydrochloride, Cocaine
D005260	Female		Females